ALBERT

All Library Books, journals and Electronic Records Telegrafenberg

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
Filter
  • Organic Chemistry  (68,935)
  • Life and Medical Sciences  (30,791)
  • Chemical Engineering  (17,976)
  • pharmacokinetics  (2,095)
  • Wiley-Blackwell  (117,703)
  • Springer  (2,026)
  • MDPI - Multidisciplinary Digital Publishing Institute  (42)
Collection
Keywords
Publisher
Language
Years
  • 1
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-01-08
    Description: This Special Issue provides an update on the state of the art and current trends in polymeric drug delivery systems specifically designed for improving drug bioavailability. The multiple contributions received further strengthen the role of polymers in modern drug delivery and targeting, illustrating the different approaches possible and unveiling what the future may bring.
    Keywords: Histoplasma capsulatum ; PLGA ; Itraconazole ; macrophage ; functionalized nanoparticle ; F4/80 receptor ; rutin ; nanocrystals ; anti-inflammatory ; hydroxypropyl beta-cyclodextrin ; nanoparticles ; budesonide ; chitosan ; colon delivery ; eudragit ; pellets ; ferrisilicate ; PEG ; insulin ; encapsulation ; diabetic mellitus ; polypeptides ; drug delivery ; doxorubicin ; cancer ; topology of poly-l-cystein ; antimicrobial ; antifouling ; pH sensitivity ; zwitterionic polymers ; gamma radiation ; copolyester ; SPION ; cysteine ; bioconjugation ; and enzymatic release ; polymeric nanoparticles ; drug delivery and targeting ; ocular posterior segment ; oxidative stress ; retinal degeneration ; nerve growth factor ; peanut agglutinin ; zebrafish ; molecular dynamics simulation ; interaction energy ; hydrogen bonding ; solid dispersion ; hot melt extrusion ; amorphous formulation ; tacrolimus ; sucrose acetate isobutyrate ; amorphous solid dispersion ; dissolution ; stability ; pharmacokinetics ; phytomedicine ; nanosponges ; lactoferrin ; bioavailability ; MDA-MB-231 cells ; caspase-3 ; cyclin-D1 ; dendrimers ; Janus nanoparticles ; biocompatibility ; nanoformulation ; pharmaceuticals ; 3D printing ; hybrid scaffold ; polycaprolactone ; vancomycin ; mesenchymal stem cells ; tissue engineering ; drug delivery systems (DDSs) ; osteomyelitis ; n/a ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PS Biology, life sciences ; bic Book Industry Communication::P Mathematics & science::PS Biology, life sciences::PSB Biochemistry
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 2
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-01-08
    Description: Lipid-based nanosystems, including solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC), cationic lipid nanoparticles, nanoemulsions, and liposomes, have been extensively studied to improve drug delivery through different administration routes. The main advantages linked to these systems are the ability to protect, transport, and control the release of lipophilic and hydrophilic molecules (either small molecular weight or macromolecules); the use of generally recognized as safe (GRAS) excipients that minimize the toxicity of the formulations; and the possibility to modulate pharmacokinetics and enable the site-specific delivery of encapsulated payloads. In addition, the versatility of lipid-based nanosystems has been further demonstrated through the delivery of vaccines, protection of cosmetic actives, or improvement in the moisturizing properties of cosmetic formulations. Currently, lipid-based nanosystems are well established, and there are already different commercially approved formulations for different human disorders. This success has actually paved the way to diversifying the pipeline of development, upon addressing unmet medical needs for several indications, such as cancer; neurological disorders; and autoimmune, genetic, and infectious diseases. This Special Issue aims to update readers on the latest research on lipid-based nanosystems, both at the preclinical and clinical levels.
    Keywords: design of experiment ; porcine mucous membrane ; ophthalmic tissues ; permeation ; nanostructured lipid carriers ; gentiopicroside ; phospholipid complex ; self-nanoemulsion drug delivery system ; oral bioavailability ; pharmacokinetics ; antioxidants ; marine bio-waste ; bioactive compounds ; neurodegenerative diseases ; NLC ; solid lipid nanoparticles ; SLN ; intranasal administration ; nose-to-brain ; exosome ; drug loading ; exosomal delivery ; large-scale production ; lipid nanoparticles ; mucoadhesion ; ocular bioavailability ; surface modification ; liposomes ; baricitinib ; JAK-inhibitor ; transepidermal delivery ; skin permeation ; lipid NPs ; breast cancer ; siRNA delivery ; gene silencing ; personalized therapy ; bimatoprost ; central composite design ; glaucoma ; HET-CAM test ; solid lipid nanoparticles (SLNs) ; perillyl acid ; biodistribution ; empty lipid nanoparticles ; reactogenicity ; xenobiotics ; ionizable lipids ; isoniazid ; in vivo pharmacokinetics ; drug release profile ; histopathological toxicity ; mannosylation ; nanocarriers ; Chagas disease ; Trypanosoma cruzi ; in vivo assays ; quality by design ; plumbagin ; diabetes ; in vitro ; niosomes ; levosulpiride ; antidepressant ; acute toxicity ; in vivo imaging ; bioavailability ; cisplatin ; co-encapsulation ; mifepristone ; synergism ; gefitinib ; lipid ; surfactant ; stability ; breast cancer cell ; MTT assay ; anticancer ; n/a ; bic Book Industry Communication::T Technology, engineering, agriculture::TB Technology: general issues
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 3
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-04-05
    Description: Model-informed precision dosing (MIPD) is an advanced quantitative approach focusing on individualized treatment optimization. MIPD integrates mathematical models of drugs and diseases combined with individual patient characteristics (e.g., genotype, anthropometric factors, and organ function). MIPD has been highlighted as a useful tool for drug dosage selection in both the drug development process and clinical practice and it is a rapidly growing discipline that is supported by the main drug regulatory agencies. Despite the potential benefits of this methodology toward personalized medicine, its application is still limited. The Special Issue presented here includes several PKPD and PBPK models focused on improving the current state of art regarding the PK behaviour of different drugs with the aim of improving the efficacy/safety balance of these treatments and their clinical outcome; the Special Issue is intended to be of particular interest for clinical pharmacologists, pharmacometricians, and specific clinicians who routinely use the considered drugs.
    Keywords: model-informed precision dosing (MIPD) ; efficacy PKPD indexes ; pharmacokinetics ; pharmacodynamics ; PKPD modeling and simulation ; dosing algorithms ; nomograms ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::K Economics, finance, business & management::KN Industry & industrial studies::KND Manufacturing industries::KNDP Pharmaceutical industries
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 4
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-03-28
    Description: Nowadays, diet-related non-communicable diseases and their complications are one of the most important public health problems worldwide. Food supplements and functional foods are considered food products which contribute to the achievement of optimal nutritional well-being, health status, and quality of life through reducing the risk of diseases and promoting the appropriate function of human organs and systems. Nowadays, the assessment of these functional foods and the study of their implications in nutrition and health are important challenges in societies of developed countries where consumers increasingly demand foods with added value beyond the provision of nutrients and the satisfaction of appetite. In this reprint, the characterization of the nutritional composition and phytochemicals of functional foods and food supplements as well as the evaluation of their potential health benefits in different disorders and diseases through clinical trials or preliminary studies are addressed.
    Keywords: food supplement ; folic acid ; pregnancy ; food safety ; health claims ; nutrition ; Amazonian fruits ; composition ; metabolic effects ; royal jelly ; acetylcholine ; fatty acid ; ophthalmology ; dry eye ; magnesium ; pharmacy ; food supplements ; drugstore ; functional foods ; healthy eating ; credibility ; extrinsic attributes ; conjoint analysis ; Mediterranean diet ; phytonutrients ; dietary recommendations ; healthy diet ; polyphenols ; flavonoids ; carotenoids ; organosulfur ; caffeine ; antidiabetic activity ; antioxidant activity ; inhibition of α-glucosidase ; inhibition of α-amylase ; inhibition of collagenase ; kombucha ; bacteria ; yeast ; metagenome ; metabolome ; tea polyphenols ; antioxidants ; Glossogyne tenuifolia ; exercise ; forelimb grip strength ; lactate ; ammonia ; creatine kinase ; medium-chain triglycerides (MCTs) ; obesity ; energy expenditure ; diet-derived fat ; postprandial resting metabolism ; sedentary ; octanoic acid ; decanoic acid ; creatine ; magnetic resonance spectroscopy ; cost-effectiveness ; brain ; muscle ; healthcare ; anthocyanins ; organosulfur compounds ; tannins ; phenolic acids ; Persea americana ; non-alcoholic liver disease ; liver enzymes ; inflammation ; oxidative stress ; novel foods ; novel ingredients ; extracts ; risk assessment ; dietary supplements ; HPLC ; food authenticity ; neural tube defects ; food ; food analysis ; food ingredients ; infant formula ; kynurenic acid ; (poly)phenol-based supplement ; pharmacokinetics ; urinary excretion ; bioavailability ; inter-individual variability ; non-invasive brain stimulation ; TMS ; a-tDCS ; indicaxanthin ; brain food ; cortical excitability ; homeostatic plasticity ; trans-resveratrol ; regulation ; labels ; nutrition claims ; high-performance thin-layer chromatography ; HPTLC ; glutamine ; intestinal stem cells ; crypt ; proliferation ; burns ; micronutrient ; health claim ; labeling ; European legislation ; thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general ; thema EDItEUR::P Mathematics and Science::PS Biology, life sciences ; thema EDItEUR::J Society and Social Sciences::JB Society and culture: general::JBC Cultural and media studies::JBCC Cultural studies::JBCC4 Cultural studies: food and society
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 5
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-04-05
    Description: This Special Issue is a collection of research topics on developing analytical and bioanalytical methods for isolation, identification, and determination of substances in biomedical and pharmaceutical matrices. Special attention is given to advancements in sample preparation, separation techniques and novel detection methods of small molecules, peptides, and monoclonal antibodies. The presented analytical methods exhibit several applications, including pharmacokinetic studies, therapeutic drug monitoring, microdialysis, toxicology, disease screening or drug stability study. Two comprehensive review articles were also presented on applying capillary electrophoresis to analyze bioactive compounds in herbal matrices.
    Keywords: CNS ; sulfasalazine ; brain to plasma ratio ; LC-ESI-TOF-MS ; rituximab ; quadripolar mass spectrometer ; albumin depletion ; pharmacokinetics ; orbitrap mass spectrometer ; IgG-immunocapture ; bubble-generating magnetic liposomes ; bionic membrane ; permeable compounds ; herbal medicines ; LC–MS ; capillary electrophoresis ; herbal ; raw material ; tea ; polyphenols ; flavonoids ; amino acids ; coumarins ; alkaloids ; chlorambucil and valproic acid ; HPLC-UV and GC-MS methods ; optimization and validation ; determination in plasma ; combined anticancer therapy ; herbal drugs ; medicinal plants ; quality control ; quantitative analysis ; pharmaceutical analysis ; 4-acetamidobenzoic acid ; validation ; pharmacokinetic ; pigs ; LC-MS/MS ; iron determination ; spectrophotometry ; flow analysis ; direct injection detector ; multi-pumping flow system ; medical errors ; hospital workflow ; patient safety ; Raman spectroscopy ; IV drugs ; piperacillin ; tazobactam ; non-invasively ; vildagliptin ; remogliflozin ; ratio derivative spectrophotometry ; determination ; formulation ; ecofriendly ; confidence interval ; stability ; retrospective analysis ; sample size ; regulatory bioanalysis ; bioanalytical method validation ; heparin ; metal–organic framework ; zeolite imidazolate framework-8 ; kinetic ; thermodynamic ; Oncheong-eum ; traditional herbal prescription ; method development ; method validation ; high-performance liquid chromatography ; thalassemia ; human hemoglobin ; wooden-tip electrospray ionization ; multiply charged ions ; mass spectrometry ; multiply charged ion ; GC–MS ; analytical QbD ; genotoxic impurity ; alkyl halide ; (Q)SAR ; analytical method development ; tyrosine kinase inhibitor ; liquid chromatography–mass spectrometry ; active metabolite ; therapeutic drug monitoring ; chronic lymphocytic leukemia ; assay error equation ; oral anticancer drug ; IWR-1-endo ; Wnt signaling inhibitor ; solid-phase extraction ; cerebral microdialysis ; bioanalysis ; Tafamidis ; polymorphs ; crystal structure ; powder diffraction ; thermal stability ; blood collection tubes ; citrate anticoagulant ; direct spectrometric determination ; quality control method ; anticoagulant concentration ; draw volume ; anticoagulant volume ; magnesium contamination ; potassium contamination ; Agrimonia pilosa ; apigenin-7-O-glucuronide ; cream ; HPLC-DAD ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PN Chemistry ; bic Book Industry Communication::P Mathematics & science::PN Chemistry::PNF Analytical chemistry
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 6
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-03-28
    Description: This Special Issue published one editorial, eight articles and four reviews from approximately one hundred authors. It aimed to provide cutting-edge research on pre-clinical development and the clinical translation of radiopharmaceuticals within the molecular imaging community. The Special Issue covered radioligand development, existing radiotracer optimization, imaging agent evaluation in animal models, the clinical production of radiopharmaceuticals, and investigative research on the use of molecular imaging probes in human subjects. We appreciate all the authors’ significant contributions to this Special Issue and hope the readers will enjoy the content.
    Keywords: nanoparticle ; multimodal imaging ; photoacoustic ; heterobivalent peptide ; Alzheimer’s disease ; amyloid-beta ; animal model ; astrocyte ; blood–brain barrier ; imaging ; metabolism ; microglia ; neuroinflammation ; neurotransmitter receptors ; positron emission tomography ; synaptic density ; vascular imaging ; FDG ; PET/CT ; microvasculature imaging ; ABC-transporter ; drug-induced liver injury ; hepatotoxicity ; organic anion-transporting polypeptide ; pharmacokinetics ; liver function ; SLC-transporter ; V/Q PET/CT ; [68Ga]Ga-MAA ; 68Ga-labelled carbon nanoparticles ; glioblastoma ; fluorescence guided surgery ; 5-ALA ; fluorescein ; NIR-AZA ; magnetic resonance imaging ; high resolution ; hybrid imaging ; psychiatric disorders ; extracellular vesicles (EVs) ; umbilical cord mesenchymal stem cell (UCMSC) ; diabetes ; I-124 ; positron emission tomography (PET) ; intravenous (I.V.) administration ; intra-arterial (I.A.) administration ; biodistribution ; fluorine-18 ; PET ; oxime ; PSMA ; lipophilicity ; radiometals ; copper-61 ; liquid targets ; post-processing ; [61Cu]Cu-DOTA-NOC ; [61Cu]Cu-DOTA-TOC ; [61Cu]Cu-DOTA-TATE ; FAP ; 99mTc-FAP inhibitor ; 99mTc-labeled iFAP ; tumor microenvironment ; SPECT ; GluN1/2B receptors ; NMDA ; [3H]ifenprodil ; σ1 and σ2 receptors ; receptor occupancy ; PET imaging ; drug development ; neurodegenerative diseases ; n/a ; thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general ; thema EDItEUR::P Mathematics and Science::PS Biology, life sciences
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 7
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-02-02
    Description: This reprint covers a wide range of topics including, but not limited to, new analytical and bioanalytical methods relevant to the separation, identification, and determination of substances in pharmaceutics, pharmacokinetics, nanobiotechnology, clinical chemistry, and related disciplines; methods for the identification of bioactive compounds in functional foods and medicinal plants; applications of chromatography and allied techniques in biomedical sciences.
    Keywords: wild rice ; antioxidant ; macroporous resins ; LC-MS/MS ; phenolics ; procyanidins ; osimertinib ; UPLC-TOF-MS ; rat ; pharmacokinetics ; carbonyl derivatization ; phenylhydrazine ; phenylenediamine ; hydroxylamine ; water analysis ; lipoxidation ; lisdexamfetamine dimesylate ; impurities ; structural elucidation ; forced degradation ; HPLC validation ; chemical constituent profiles of Sinisan ; chinese medicine processing ; chinese medicinal formula compatibility ; Dendropanax morbifera leaf ; xanthine oxidase ; hyperuricemia ; HPLC ; advanced glycation end-products (AGEs) ; Nε-(carboxymethyl) lysine (CML) ; Nε-(carboxyethyl) lysine (CEL) ; antler velvet processing ; UPLC-MS/MS ; Cinnamomum yabunikkei leaf ; elastase ; Citrus junos Seib ex TANAKA ; rhKGF-1 ; rhKGF-2 ; bioactivity ; cell-based bioassay ; method validation ; CYP450 enzyme ; cocktail probe drug ; RT-PCR ; galangin ; affecting factors ; amadori compound ; furosine ; Maillard reaction ; velvet antler processing ; Brazilian green propolis ; phenolic acids ; UPLC-ESI-QTOF-MS ; quantitation ; methodological verification ; Glycyrrhizae Radix extract ; glycyrrhizin ; isoliquiritigenin ; liquiritigenin ; liquiritin ; LC–MS/MS analysis ; desoxo-narchinol A ; Nardostachys jatamansi ; bioavailability ; silybin ; silymarin product ; comparative pharmacokinetics ; ginsenosides ; red ginseng extract ; human ; acanthus ilicifolius herb ; phenylethanoid glycosides ; C.tricuspidata Bureau ; tyrosinase ; dialyzable leukocyte extract ; Transferon® ; complex mixture of peptides ; quality specifications ; biological potency ; development and validation ; Dioscorea nipponica Makino ; steroidal saponin ; HPLC-UV ; UPLC-QTOF/MS ; validation ; osteosarcoma ; apoptosis ; epinastine ; comparison ; SH-1242 ; 2-(3,4-dimethoxyphenyl)-1-(5-methoxy-2,2-dimethyl-2H-chromen-6-yl)ethanone ; HPLC-MS/MS ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PN Chemistry ; bic Book Industry Communication::P Mathematics & science::PN Chemistry::PNF Analytical chemistry
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 8
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-04-05
    Description: This reprint is an excellent collection of articles that deal with difficult-to-treat infections in the ICU environment. Multiresistant bacteria and fungi create severe treatment problems to the physician charged with their care. We hope that this book will help everyday dilemmas and add useful information on difficult topics.
    Keywords: Acinetobacter ; pandrug-resistant ; antimicrobial combinations ; synergy ; renal replacement therapy ; Monte Carlo simulation ; antibiotics ; pharmacokinetics ; pharmacodynamics ; microbiome ; probiotics ; intensive care unit ; dysbiosis ; ventilator-associated pneumonia ; extracorporeal membrane oxygenation ; ECMO ; critical illness ; antibiotic choices ; HAP ; VAP ; colonization ; antibiotic pressure ; bloodstream infection ; bacteraemia ; sepsis ; septic shock ; empirical ; probabilistic antibiotics ; source control ; de-escalation ; ICU ; intensive care ; antimicrobial stewardship ; COVID-19 ; procalcitonin ; C-reactive protein ; presepsin ; infection ; biomarker ; guided antimicrobial therapy ; APACHE II score ; bacteremia ; broth microdilution ; colistin ; colistin-resistant ; Gram-negative ; mortality ; SOFA score ; candidemia ; incidence ; epidemiology ; Candida species ; non-albicans Candida species ; fluconazole resistance ; critically ill ; beta-lactam antibiotics ; Acinetobacter baumannii ; antibiotic optimisation ; antibiotic stewardship (AMS) ; aspiration pneumonia ; hospital-acquired pneumonia (HAP) ; multidrug-resistance (MDR) ; non-fermentative Gram-negative bacilli (GNB) ; polymicrobial ; pneumonia resolution ; ventilator-associated pneumonia (VAP) ; carbapenem-resistant A. baumannii (CRAb) ; infection control ; antimicrobial agents ; carbapenems ; antibiotic resistance ; clinical pharmacy services ; Klebsiella pneumoniae ; Pseudomonas aeruginosa ; salvage treatment ; double carbapenem ; newer β-lactam-β-lactamase inhibitors ; cefiderocol ; eravacycline ; SARS-CoV-2 infection ; mechanical ventilation ; risk factors ; blood stream infection ; defined daily dose ; antibiotics utilization ; empiric ; n/a ; bic Book Industry Communication::M Medicine
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 9
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-06-23
    Description: The aim of this second Eng Special Issue is to collect experimental and theoretical re-search relating to engineering science and technology. The general topics of Eng are as follows: electrical, electronic and information engineering; chemical and materials engineering; energy engineering; mechanical and automotive engineering; industrial and manufacturing engineering; civil and structural engineering; aerospace engineering; biomedical engineering; geotechnical engineering and engineering geology; and ocean and environmental engineering. Therefore, the following editorial is a selection of representative works of these topics.
    Keywords: &nbsp ; Environment Management ; Environmental Engineering ; Chemical Engineering ; Materials Engineering&nbsp ; bic Book Industry Communication::T Technology, engineering, agriculture::TB Technology: general issues ; bic Book Industry Communication::T Technology, engineering, agriculture::TB Technology: general issues::TBX History of engineering & technology
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 10
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-02-02
    Description: Advanced Blood-Brain Barrier Drug Delivery is a reprint with a summary editorial, followed by 16 chapters that cover five areas of brain drug delivery, including receptor-mediated transport (RMT), carrier-mediated transport (CMT), active efflux transport (AET), Trojan horse lipid nanoparticles (LNP), and in vivo methods for measurement of drug transport across the blood–brain barrier (BBB).
    Keywords: blood–brain barrier (BBB) ; brain drug delivery ; prodrugs ; solute carriers (SLCs) ; lysosomal storage disease ; neuronopathic mucopolysaccharidosis ; blood–brain barrier ; neurodegeneration ; enzyme replacement therapy ; receptor-mediated transcytosis ; transferrin receptor ; insulin receptor ; endothelium ; receptor-mediated transport ; carrier-mediated transport ; genetic engineering ; IgG fusion proteins ; nanoparticles ; liposomes ; TrkB ; agonist antibody ; variable new antigen receptor (VNAR) ; neuroprotection ; transferrin receptor 1 (TfR1) ; blood-brain barrier (BBB) ; 6-OHDA ; Parkinson’s disease ; bispecific antibody ; alpha-synuclein (αSYN) ; Parkinson’s disease (PD) ; immunotherapy ; monoclonal antibody ; transferrin receptor (TfR) ; receptor-mediated transcytosis (RMT) ; single domains antibody ; IGF1R ; neurotensin ; protein-based therapy ; lysosomal storage disorders ; fusion proteins ; Alzheimer’s disease ; neurotrophic factors ; decoy receptors ; ATP-binding cassette transporters ; drug delivery ; ischemic stroke ; SLC transporters ; lipid nanoparticle ; ssPalm ; mRNA transfection ; hCMEC/D3 cells ; cell toxicity ; SWATH-MS ; translation ; chaperonin-containing TCP-1 ; proton-coupled organic cation antiporter ; photo-affinity labeling ; proteomics ; SWATH-MS (sequential window acquisition of all theoretical-mass spectra) ; pharmacokinetics ; compartmental models ; physiologically based PK models ; blood-brain barrier ; antibody ; cavernous sinus ; BBB–peptide shuttle ; brain delivery ; solute carrier (SLC) transporters ; amyotrophic lateral sclerosis (ALS) ; NSC-34 cell lines ; taurine transporter (Taut) ; large amino acid transporter 1 (LAT1) ; monocarboxylate transporters (MCTs) ; organic cation transporters (OCTNs) ; choline transporter-like protein-1 (CTL1) ; TNF-α inhibitor ; molecular Trojan horse ; endosomal ; liposome ; nanoparticle ; targeting ; transferrin ; n/a ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::M Medicine::MM Other branches of medicine::MMG Pharmacology
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 11
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-11-30
    Description: Research in ophthalmic drug delivery has developed significant advances in the few last years, and efforts have been made to develop more effective topical formulations to increase drug bioavailability, efficiency, and safety. Drug delivery to the posterior segment of the eye remains a great challenge in the pharmaceutical industry due to the complexity and particularity of the eye's anatomy and physiology. Some advances have been made with the purpose of maintaining constant drug levels in the site of action. The anatomical ocular barriers have a great impact on drug pharmacokinetics and, subsequently, on the pharmacological effect.Despite the increasing interest in efficiently reaching the posterior segment of the eye with reduced adverse effects, there is still a need to expand the knowledge of ocular pharmacokinetics that allow the development of safer and more innovative drug delivery systems. These novel approaches may greatly improve the lives of patients with ocular pathologies.
    Keywords: ocular ; drug delivery ; pharmacokinetics ; tissue isolation ; rat ; eye ; drug concentration ; method ; pigment ; melanin ; aniridia ; ataluren ; ophthalmic solution ; rare disease ; stability ; tacrolimus ; hydroxypropyl-β-cyclodextrin ; topical ophthalmic administration ; eye drops ; uveitis ; PET/CT imaging ; ocular implants ; electrospinning technique ; glaucoma ; sustained drug release ; poly ε-caprolactone ; electrospun fibers ; permeability ; retina ; retinal pigment epithelium ; Ussing chamber ; intravitreal half-life ; posterior capsule opacification ; pathophysiology ; wound healing ; lens epithelial cells ; intraocular lenses ; experimental models ; clinical studies ; gold nanoparticles ; anterior chamber ; distribution ; intracameral injection ; trabecular meshwork ; hyaluronic acid ; liposomes ; intravitreal ; ocular drug delivery ; retinal explants ; amantadine ; blood–retinal barrier ; retinal disease ; NMDA receptor ; inner BRB ; retinal capitally endothelial cells ; outer BRB ; retinal pigment epithelial cells ; transporter ; rivoceranib ; drug repositioning ; microsphere ; subfoveal choroidal neovascularization ; macular degeneration ; endotoxin-induced uveitis ; interleukins ; immunosuppressants ; physicochemical stability ; container-content interaction ; leachable compound ; nanoparticles ; PLGA ; lactoferrin ; nanoprecipitation ; protein nanocarriers ; keratoconus ; corneal ecstatic disorder ; posterior capsular opacification ; intraocular lens ; surface modification ; photothermal therapy ; photodynamic therapy ; micro-pattern ; anti-biofouling ; ocular hypertension ; prostaglandin analogues ; aqueous solubility ; chemical stability ; intraocular pressure ; cystinosis ; ophthalmic administration ; cysteamine ; compounded formulation ; PET ; nanocrystals ; conjunctivitis ; besifloxacin ; Povacoat® ; fluoroquinolones ; acanthamoeba keratitis ; controlled drug delivery ; contact lens ; miltefosine ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::K Economics, finance, business & management::KN Industry & industrial studies::KND Manufacturing industries::KNDP Pharmaceutical industries
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 12
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-11-30
    Description: In this Special Issue, our aim was to collect studies on clinical pharmacology and pharmacy of antimicrobial agents from both human and veterinary medicine as the complex problem of AMR requires actions taken within the One Health approach that involve both fields. Studies covered here are about new or optimized usage of already authorized antimicrobials, as well as discoveries about new agents, new combinations of drugs, and drug repositioning. Pharmacodynamic, pharmacokinetic, and toxicological aspects of individual and combinational drug use are areas covered in this Special Issue.
    Keywords: antibiotic combination ; minimum inhibitory concentration ; Monte Carlo ; synergistic effect ; antibiotics ; combination therapy ; multi-drug resistant infection ; meta-analysis ; pan-genome ; Campylobacter ureolyticus ; UDP-3-O-acyl-N-acetylglucosamine deacetylase ; LpxC ; campylobacteriosis ; self-medication ; students ; habits ; cystic fibrosis ; P. aeruginosa ; transporters ; Escherichia coli ; suture ; antimicrobial ; pharmacodynamics ; triclosan ; surgical site infection ; time-kill ; contact killing ; translational modelling ; antifungals ; adverse drug reaction (ADR) ; drug-drug interaction (DDI) ; polypharmacy ; multimorbidity ; intensive care patients ; traumatology ; elderly patients ; organ failure ; multi-organ failure ; drug safety ; patient safety ; nonlinear mixed-effects modeling ; glomerular filtration rate ; dosing regimen ; oxacillin ; Monte Carlo simulations ; adsorption ; desorption ; doxycycline ; pH dependence ; small ruminant feed ; heterocyclic compounds ; phenolic compounds ; pyran ; food microbiology ; microbial pathogen ; serum/plasma concentrations ; interstitial concentrations ; tissue concentrations ; pharmacokinetics ; macrolide antibiotics ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::M Medicine::MM Other branches of medicine::MMG Pharmacology
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 13
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-09-11
    Keywords: drug design and discovery ; drug&ndash ; protein interactions ; drug response ; drug solubility ; antimicrobial drugs ; antiviral drugs ; antibiotics ; anticancer drugs ; cancer prevention ; molecular modeling ; molecular mechanisms ; crystallography ; preclinical study ; pharmacokinetics ; pharmacodynamics ; pharmacognosy ; nuclear receptors ; receptor agonist and antagonist ; activity profiling, markers and diagnostics ; drug carriers ; dosage form ; nanoparticles ; dissolution testing ; bic Book Industry Communication::M Medicine::MB Medicine: general issues::MBG Medical equipment & techniques
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 14
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-04-05
    Description: Novel Anticancer Strategies reviews important findings and updates within the cancer therapy field, of great interest to those in academic research studying the development and validation of novel anticancer approaches. The Editor invited preeminent specialists to contribute to original and review articles devoted to key areas of major progress and expectations. Key features: Nanoparticle-based drug delivery in cancer therapy; Extracellular vesicles for anticancer drug delivery; Peptide-based drug conjugates; Cancer stem cells as a valuable target to eradicate tumor relapse; Spheroids in preclinical model for cancer research; and cancer immunotherapy.
    Keywords: tumor-homing extracellular vesicles ; pH-sensitive extracellular vesicles ; doxorubicin ; tumor therapy ; pancreatic cancer ; targeted tumor therapy ; homing peptide ; antitumor peptide conjugates ; daunomycin ; oxime linkage ; combinatorial immunotherapy ; cytotoxics ; biomarkers ; precision medicine ; immunotherapy ; anti-PD-L1 ; ionizing irradiation ; pharmacokinetics ; tumor-immune interaction ; global sensitivity ; immuno-oncology ; mathematical modeling ; glycol chitosan nanoparticle ; high-intensity focused ultrasound ; deep tumor penetration ; dense ECM ; cancer treatment ; prostate cancer ; gastrin-releasing peptide receptor ; RM26 ; albumin-binding domain ; targeted therapy ; gastrin-releasing peptide receptors (GRPR) antagonist ; cervical cancer ; tetraarsenic hexoxide ; patient-derived xenograft ; autophagy ; cisplatin ; fenbendazole ; micelle solubilization ; Soluplus® polymeric micelles ; toxicity test ; sonoporation ; microbubbles ; ultrasound ; intracellular signaling ; phosphorylation ; ultrasound contrast agents ; drug delivery ; cellular stress ; tumour microenvironment ; cancer stem cells ; extracellular vesicles ; drug delivery systems ; liposomes ; immunoliposomes ; antisense oligonucleotides ; 3D cultures ; tumor microenvironment ; tumor spheroids ; efficacy analysis ; drug resistance ; cancer therapy ; glioblastoma ; receptor tyrosine kinases ; epidermal growth factor receptor ; small molecule inhibitors ; nanoformulations ; breast cancer ; micelles ; dendrimers ; anticancer drugs ; platinum drug ; methotrexate ; lung metastasis ; liver metastasis ; cancer treatments and progression biomarkers ; mesoporous silica nanoparticles ; controlled release ; anticancer natural prodrugs ; natural products ; cancer targeting ; nanoformulations/nanomedicine applications ; n/a ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::M Medicine::MJ Clinical & internal medicine::MJC Diseases & disorders::MJCL Oncology
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 15
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-03-31
    Description: Recently, microfluidic, nanofluidic and lab-on-a-chip devices have gained particular attention in biomedical applications. Due to their advantages, such as miniaturization, versatility, ease of use, cost-effectiveness, and the potential to replace animal models for drug development and testing, these devices hold tremendous potential to revolutionize the research of more effective treatments for several diseases that threaten human life. With integrated biosensors, these devices allow the development and design of micro- and nanoparticles to be studied in detail, modelling human physiology, investigating the molecular and cellular mechanisms underlying disease formation and progression, and gaining insights into the performance and long-term effects of responsive drug delivery nanocarriers. This Special Issue gathered research papers, and review articles focusing on novel microfluidic, nanofluidic and lab-on-a-chip devices for biomedical applications, addressing all steps related to fabrication, biosensor integration and development, characterization, numerical simulations and validation of the devices, optimization and, the translation of these devices from research labs to industry settings.
    Keywords: protein biomarker ; microarray ; microfluidic cassette ; multiplex measurement ; immunoassay ; point-of-care testing ; microfluidic device ; small intestine ; ex vivo ; histology ; embedded resin ; sectioning ; peptide biosensor ; lab-on-a-chip ; label-free detection ; peptide aptamers ; protein biomarkers ; microfluidic biochip ; troponin T ; computational simulations ; drug discovery ; organ-on-a-chip ; microfluidic devices ; preclinical models ; numerical simulations ; automation ; non-enzymatic ; DNA amplification ; L-DNA ; microfluidic ; fluorescence ; paper microfluidics ; sweat ; sensing ; hydrogels ; lactate ; osmotic pumping ; evaporation ; capillary ; wicking ; biochemical assay ; microfluidics ; cell trap ; RBC ; evolutionary algorithm ; generative design ; artificial intelligence ; organ-on-chip ; liver-on-chip ; liver disease ; multi-level microfluidic device ; live cell imaging ; long-term microscopy imaging ; focus drifting ; immersion oil viscosity ; bacterial population dynamics ; single-cell studies ; E. coli ; mother machine ; computational fluid dynamics ; cancer-on-chip ; xenograft ; colorectal cancer ; pharmacodynamics ; pharmacokinetics ; drug efficacy ; oxaliplatin ; microfabrication ; microphysiological system ; biophysical stimuli ; biochemical stimuli ; in vitro cell culture ; cortical neurons ; hippocampal neurons ; electrical stimulation ; Micro-Electrode Arrays ; engineered neuronal networks ; polydimethylsiloxane ; microchannels ; in vivo micro bioreactor ; additive manufacturing ; poly-(ethylene glycol)-diacrylate ; biocompatibility ; COVID-19 ; diagnosis ; image analysis ; PCR ; SARS-CoV-2 ; n/a ; thema EDItEUR::M Medicine and Nursing
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 16
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-09-11
    Description: It has been known that cellular glutathione content and its speciation play a role, among others, in redox homeostasis, cell cycle control, immunological defense, and pathological abnormalities. Furthermore, it plays a significant role in the biotransformation of drugs and other endogenous or exogenous electrophilic species. Most of these cellular functions are related to the thiol function of the cysteine moiety.This reprint presents the publications that appeared in the Special Issue of Molecules, “Glutathione: Chemistry and Biochemistry.” The first three contributions review the present-day knowledge of the GSH/GSSG system and the most important GSH-related proteins involved in regulating various cellular events. The subsequent four contributions present selected interventions that modulate the GSSG/2GSH system. One of the contributions to this session describes a new HPLC method to quantify the reduced and oxidized glutathione levels. The third session involves three contributions demonstrating the role of GSH in the metabolism of different candidate and clinically used anticancer drugs. One of the contributions, a theoretical work, provides helpful information for developing GSH analogs with high ACE inhibitor activity.By purpose and content, this Special Issue is addressed to the vast number of life science researchers (academic and industrial) and medical professionals who are interested in or already engaged in research that involves glutathione.
    Keywords: cyclophosphamide ; autoimmune diseases ; glutathione ; glutathione-S-transferase ; polymorphism ; glutaredoxin ; iron-sulfur cluster ; iron ; S-glutathionylation ; S-nitrosylation ; GSH ; nitrosoglutathione ; redox-regulation ; polymerized whey protein ; physicochemical properties ; pharmacokinetics ; toxicity ; chalcone ; cysteine ; thiols ; Michael addition ; diastereoselective addition ; reactive oxygen species ; oxidative stress ; nanotoxicity ; cell injury ; fluorescence probes ; brain ; liquid chromatography ; diode array detector ; anticancer drugs ; mechanisms of glutathione conjugation reaction ; detoxification ; bioactivation ; sulodexide ; endothelial cells ; ischemia ; apoptosis ; GSSG ; GCLc ; GSS ; redox potential ; supramolecular arrangement ; M06-2X/6-311++G(d,p) ; DFT ; molecular docking ; angiotensin-converting enzyme ; cell ; redox homeostasis ; glutathionylation ; glutathione system ; glutathione enzyme ; n/a ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PS Biology, life sciences
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 17
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-09-11
    Keywords: iron oxide magnetic nanoparticles ; silica coating ; magnetic hyperthermia ; cancer cells ; alamar blue ; neutral red ; A549 ; A35 ; BJ ; ultrasmall magnetic iron oxide nanoparticles ; inflammatory pain ; analgesia ; pro-inflammatory cytokines ; neurotoxicity ; long-term potentiation ; solid lipid nanoparticles ; magnetic nanoparticles ; magnetic solid lipid nanoparticles ; cancer theranostics ; MRI-contrast agents ; pulsed laser ablation in liquids ; multimodal imaging ; MRI ; CT ; photothermal therapy ; iron-gold nanoparticles ; pharmacokinetics ; magnetic targeting ; micro-systems ; nano-systems ; drug delivery ; nanoparticles ; microparticles ; targeted delivery ; magnetic guidance ; theranostics ; imaging ; AC biosuceptometry ; cirrhosis-associated rat hepatocarcinogenesis ; nanotechnology ; magnetoresponsive nanocomposite ; functional coating ; particle targeting ; particle aggregation ; stent targeting ; nanomedicine ; MRI technology ; patient-centred healthcare ; iron oxide nanoparticles ; paramagnetic salinomycin complexes ; bacterial ghosts ; gadolinium ; manganese ; lectin ; PLGA ; ConA ; magnetic polymer nanoparticles ; MPQ ; allografts ; photodynamic therapy ; IR775 ; image-guided therapy ; n/a ; bic Book Industry Communication::T Technology, engineering, agriculture::TB Technology: general issues
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 18
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-05-06
    Description: The gastrointestinal tract (GIT) can be broadly divided into several regions: the stomach, the small intestine (which is subdivided to duodenum, jejunum, and ileum), and the colon. The conditions and environment in each of these segments, and even within the segment, are dependent on many factors, e.g., the surrounding pH, fluid composition, transporters expression, metabolic enzymes activity, tight junction resistance, different morphology along the GIT, variable intestinal mucosal cell differentiation, changes in drug concentration (in cases of carrier-mediated transport), thickness and types of mucus, and resident microflora. Each of these variables, alone or in combination with others, can fundamentally alter the solubility/dissolution, the intestinal permeability, and the overall absorption of various drugs. This is the underlying mechanistic basis of regional-dependent intestinal drug absorption, which has led to many attempts to deliver drugs to specific regions throughout the GIT, aiming to optimize drug absorption, bioavailability, pharmacokinetics, and/or pharmacodynamics. In the book "Regional Intestinal Drug Absorption: Biopharmaceutics and Drug Formulation" we aim to highlight the current progress and to provide an overview of the latest developments in the field of regional-dependent intestinal drug absorption and delivery, as well as pointing out the unmet needs of the field.
    Keywords: bioequivalence ; Biopharmaceutics Classification System ; in vitro ; dissolution test ; pravastatin ; oral absorption ; in silico modeling ; GastroPlus ; Phoenix WinNonlin ; pharmacokinetics ; clinical studies ; ibuprofen ; manometry ; gastrointestinal ; mechanistic modeling ; PBPK ; PBBM ; disintegration ; dissolution ; enteric-coated ; ICH ; quality control ; regional intestinal permeability ; permeation enhancers ; absorption-modifying excipients ; oral peptide delivery ; intestinal perfusion ; pharmaceutical development ; controlled release drug product ; biopharmaceutics classification system ; drug solubility ; drug permeability ; location-dependent absorption ; segregated flow intestinal model (SFM) ; traditional model (TM) ; route-dependent intestinal metabolism ; first-pass effect ; drug-drug interactions ; DDI ; in vitro in vivo extrapolations ; IVIVE ; zero-order absorption ; first-order absorption ; combined zero- and first-order absorption ; transit compartment absorption model ; in situ perfusion ; microdevices ; shape ; mucoadhesion ; colon absorption ; nutrient digestion ; nutrient absorption ; gastrointestinal hormone ; postprandial glycaemia ; energy intake ; region of the gut ; obesity ; type 2 diabetes ; Franz–PAMPA ; BCS drugs ; biomimetic membrane ; Franz cell ; passive drug transport ; BCS class IV drugs ; segmental-dependent intestinal permeability ; intestinal absorption ; oral drug delivery ; biopharmaceutics ; physiologically-based pharmacokinetic (PBPK) modeling ; furosemide ; intestinal permeability ; human colon carcinoma cell layer (Caco-2) ; hierarchical support vector regression (HSVR) ; drug absorption ; drug solubility/dissolution ; regional/segmental-dependent permeability and absorption ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::K Economics, finance, business & management::KN Industry & industrial studies::KND Manufacturing industries::KNDP Pharmaceutical industries
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 19
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-03-21
    Description: This book is a compendium of scientific articles submitted to a Special Issue of International Journal of Molecular Sciences, fostered by MDPI and curated by Dr. Annamaria Sandomenico and Dr. Menotti Ruvo from the Institute of Biostructure and Bioimaging of the National Research Council. All articles underwent a rigorous peer review and were selected to highlight the properties that make monoclonal antibodies and their functional fragments some of the most useful and versatile assets in therapy and diagnosis.
    Keywords: porcine deltacoronavirus ; nucleocapsid ; monoclonal antibodies ; neurodegenerative disorders ; affibody molecules ; blood–brain barrier ; receptor-mediated transcytosis ; transferrin receptor ; AL amyloidosis ; CD38 ; anti-CD38 MoAb ; Daratumumab ; Isatuximab ; myeloma ; BCMA ; bispecific T-cell engager ; antibody-drug conjugates ; chimeric antigen receptor T-cells ; belantamab mafodotin ; idecabtagene vicleucel ; JNJ-68284528 ; Mabs ; Antibody-Drug Conjugate ; cancer therapy ; drug targeting ; payload ; cross-linking ; antibody fragment ; Fab ; scFv ; E. coli ; YKL-40 ; CHI3L1 ; monoclonal antibody ; phage display ; lung metastasis ; prostate-specific membrane antigen ; in vivo imaging ; prostate cancer ; glutamate carboxypeptidase II ; NAALADase ; immunization ; antibody ; protocol ; guinea pig ; cDNA ; chimeric antigen receptor (CAR T) ; universal CAR T ; modular CAR T ; universal immune receptor ; CAR adaptor ; adoptive immunotherapy ; split CAR ; bispecific ; polyspecificity ; pharmacokinetics ; solubility ; aggregation ; viscosity ; developability ; stability ; affinity ; specificity ; protein engineering ; self-association ; non-specific binding ; immunogenicity ; antibody fragments ; single chain ; amyloid ; oligomer ; neurotoxicity ; NUsc1 ; bic Book Industry Communication::T Technology, engineering, agriculture::TB Technology: general issues
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 20
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-06-21
    Description: Derivatization is one of the most widely used sample pretreatment techniques in Analytical Chemistry and Chemical Analysis. Reagent-based or reagent-less schemes offer improved detectability of target compounds, modification of the chromatographic properties and/or the stabilization of sensitive compounds until analysis. Either coupled with separation techniques or as a “stand alone” analytical procedure, derivatization offers endless possibilities in all aspects of analytical applications.
    Keywords: tyrosine kinase inhibitors ; chloranilic acid ; charge-transfer reaction ; 96-microwell spectrophotometric assay ; high-throughput pharmaceutical analysis ; biogenic amines ; Lycium barbarum L. ; HPLC ; derivatization ; amino acids ; esterification ; GC–MS ; pentafluoropropionic anhydride ; stability ; toluene ; pigment ; linseed oil ; derivatisation ; quantification ; P/S ratio ; A/P ratio ; ∑D ; GC-MS ; ureide ; BSTFA ; creatine ; creatinine ; silylation ; TMS ; validation ; low-molecular-weight thiols ; human serum albumin ; α-lipoic acid ; blood plasma ; monobromobimane ; reduction ; sodium borohydride ; high-performance liquid chromatography ; fluorescence detection ; taurine ; glutamine ; clams ; high-resolution mass spectrometry ; nerve agents ; methylation ; chemical warfare agents ; sarin ; Novichoks ; 2-naphthalenethiol ; sulforaphane ; HPLC-UV/Vis ; pharmacokinetics ; acetonitrile-related adducts ; acetylenic lipids ; double and triple bond localization ; in-source derivatization ; mass spectrometry ; acetazolamide ; carbonic anhydrase ; enhancement ; inhibition ; pentafluorobenzyl bromide ; chiral metabolomics ; rice water ; d-amino acids ; enantiomer separation ; dimethyl labeling ; homocysteine thiolactone ; homocysteine ; zone fluidics ; o-phthalaldehyde ; fluorosurfactant-modified gold nanoparticles ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PN Chemistry ; bic Book Industry Communication::P Mathematics & science::PN Chemistry::PNF Analytical chemistry
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 21
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-03-27
    Description: This book covers the most recent research trends and applications of Pharmaceutical Analytical Chemistry. The included topics range from the adulteration of dietary supplements, to the determination of drugs in biological samples with the aim to investigate their pharmacokinetic properties.
    Keywords: growth hormone ; long-acting Fc-fusion recombinant human growth hormone ; method validation ; cell-based bioassay ; reporter gene assay ; pharmacokinetics ; tissue distribution ; alnustone ; rats ; LC-MS/MS ; inflammatory bowel disease ; fixed-dose combination ; biomimetic chromatography ; thiopurine immunosuppressants ; folic acid ; doxorubicin ; hernandezine ; pharmacokinetic study ; drug–drug interaction ; gardneramine ; monoterpenoid indole alkaloid ; memantine ; rimantadine ; amantadine ; zone fluidics ; o-phthalaldehyde ; derivatization ; stopped-flow ; quality control ; anwuligan ; rat ; optode ; polyhexamethylene biguanide hydrochloride ; lactone-rhodamine B ; contact-lens detergent ; dietary supplement ; adulteration ; low-field NMR ; multivariate analysis ; steroids ; Partial Least Squares regression ; in vitro permeability ; predictive model ; ketamine ; norketamine ; high throughput bar adsorptive microextraction ; LVI-GC-MS(SIM) ; urine ; baricitinib ; UPLC-MS/MS ; irbersartan ; n/a ; thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 22
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-03-31
    Description: This book serves to highlight the pharmacokinetics/drug–drug interactions and mechanistic understanding in relation to the drug-metabolizing enzymes and drug transporters.This book presents a series of drug metabolism and transport mechanisms that govern the pharmacokinetic features of therapeutic drugs as well as natural herbal medicines. It also covers the pharmacokinetic interactions caused by inhibiting or inducing the metabolic or transport activities under disease states or the coadministration of potential inhibitors. It also deals with microenvironmental pharmacokinetic profiles as well as population pharmacokinetics, which gives new insights regarding the pharmacokinetic features with regard to drug metabolism and transporters.
    Keywords: tofacitinib ; dose-dependent pharmacokinetics ; hepatic and intestinal first-pass effect ; rats ; catalposide ; in vitro human metabolism ; UDP-glucuronosyltransferase ; sulfotransferase ; carboxylesterase ; celecoxib ; drug–drug interaction ; fluorescence ; HPLC ; metabolism ; repaglinide ; HSG4112 ; anti-obesity agent ; stereoselectivity ; pharmacokinetics ; compound K ; protopanaxadiol (PPD) ; biliary excretion ; intestinal metabolism ; Carthamus tinctorius extract ; notoginseng total saponins ; comparative pharmacokinetic study ; large volume direct injection ; compatibility mechanism ; mertansine ; human hepatocytes ; cytochrome P450 ; UDP-glucuronosyltransferases ; sodium-glucose cotransporter 2 (SGLT2) inhibitors ; DWP16001 ; kidney distribution ; inhibition mode ; diabetes ; transporter-enzyme interplay ; influx transporter ; efflux transporter ; physiologically based pharmacokinetic model ; cytochrome P450 enzymes ; tiropramide ; healthy Korean subjects ; modeling ; population pharmacokinetic ; quercetin ; breast cancer resistance protein ; inhibitor ; prazosin ; sulfasalazine ; kinetic analysis ; food–drug interactions ; Caco-2 ; EpiIntestinal ; first-pass ; P-gp ; BCRP ; drug transporter ; CYP3A4 ; oral availability ; automatization ; drug absorption ; drug dosing ; head-and-neck cancer ; real-time measurements ; taxanes ; tissue engineering ; UHPLC-MS/MS ; metformin ; verapamil ; drug interaction ; organic cation transporter 2 ; renal excretion ; acute renal failure ; gentamicin ; cisplatin ; hepatic CYP3A1(23) ; creatinine clearance ; renal clearance ; nonrenal clearance ; thema EDItEUR::M Medicine and Nursing ; thema EDItEUR::K Economics, Finance, Business and Management::KN Industry and industrial studies::KND Manufacturing industries
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 23
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-02-24
    Description: The book broadly deals with therapeutic monoclonal antibodies (mAbs) and various relevant topics, including different antibody formats such as Antibody–Drug Conjugates (ADC), bispecifics, nanoparticle-based mAbs and HER2+ cancers, immune checkpoint inhibitors and other closely related topics. Each paper was written by leading active research groups in their fields both from academia and industry. The book should be of interest to those scientists and researchers who develop or use biologics, biotherapeutics, biosimilars and biobetters in cancer treatment.
    Keywords: monoclonal antibody ; NSCLC ; immunotherapy ; ELISA ; pharmacokinetics ; pharmacogenetics ; anti-PD-1 monoclonal antibodies ; anti-acetylcholine receptor (AChR) antibody ; B cell ; immune checkpoint blockade ; immune-related adverse events (irAEs) ; myasthenia gravis (MG) ; non-small-cell lung cancer (NSCLC) ; nivolumab ; programmed cell death ligand 1 (PD-L1) ; T cell ; tetraspanins ; cancer ; Tspan8 ; radioimmunotherapy ; immune-checkpoint inhibitors ; LDH ; biomarkers ; Ang-2 ; antiangiogenic therapy ; in vivo imaging ; radio- and chemotherapy ; VEGF-A ; cancer therapy ; neovascularization ; angiogenesis ; tumor microenvironment ; colorectal cancer ; antibody ; NK cells ; ADCC ; CD133 ; prominin-1 ; gold nanoparticles ; antibody-drug conjugates ; cell penetrating peptide ; HIV-1 TAT ; active-targeting ; targeted delivery ; trastuzumab ; MMAE ; valine-citrulline ; affibody ; drug conjugates ; hepatic uptake ; DM1 ; dermatooncology ; immune checkpoints ; monoclonal antibodies ; passive immunotherapy ; canine B-cell lymphoma ; DLA-DR ; HLA-DR ; antibody-drug conjugate ; ADC ; methotrexate ; tumor immunity ; combination therapy ; multiple myeloma (MM) ; monoclonal antibodies (mAbs) ; antibody products ; B cell maturation antigens (BCMAs) ; bispecific T cell engagers (BiTEs®) ; checkpoint inhibitors 1 ; protein structure 2 ; pharmacokinetics 3 ; drug optimization 4 ; HER2-positive breast cancer ; metastatic disease ; neoadjuvant and adjuvant therapy ; targeted therapy ; acute myeloid leukemia ; CD123 ; IL3RA ; kinesin spindle protein inhibitor ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::K Economics, finance, business & management::KN Industry & industrial studies::KND Manufacturing industries::KNDP Pharmaceutical industries
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 24
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-11-17
    Description: Caffeine is present in coffee and many other beverages and is the most widely used central nervous system stimulant. Coffee drinking or caffeine supplementation may have a role in preventing cardiometabolic and endocrine disease, neuroinflammation, cancer, and even all-cause mortality. Other aspects are either less known or controversial, including the effects on the brain–gut axis, neurodevelopment, behavior, pain, muscle–skeletal health, skin or sexual function. Studies focusing on special populations (neonates, children, adolescents, athletes, elderly, pregnant and nonpregnant women), or interactions with other drugs and foods, are relatively scarce but of obvious interest. Other compounds present in coffee and other caffeinated food stuffs may affect caffeine´s physiological effects with a tremendous impact on health. This Special Issue, which contains twenty-one manuscripts, has focused on some of these varied topics, providing further evidence of the multiple health benefits that coffee/caffeine intake may exert in humans, at least in specific populations (with a particular genetic profile or suffering from specific diseases). However, the specific effects in the different organs and systems, as well as the mechanisms involved are not yet clear. Furthermore, within the current context aiming to sustainable development, the coffee plant Coffee sp. and its so-far relatively neglected by-products are expected to become soon a source of ingredients for new functional foods whose properties will need to be precisely determined. We hope the readers of this Special Issue will find inspiration for new studies on the topic.
    Keywords: pharmacokinetics ; energy drink ; exercise ; elite athlete ; performance ; football ; RPE ; DOMS ; sport performance ; supplementation ; ergogenic aids ; consumer ; behavior ; perception ; coffee ; health ; consumption motives ; coffee/caffeine ; systematic review and meta-analysis ; prospective studies ; epidemiology ; cancer prevention ; colorectal cancer ; individual responses ; responders ; exercise performance ; caffeine ; tea ; energy drinks ; pregnancy ; newborn ; ergogenic aid ; resistance training ; isokinetic testing ; adrenal gland ; corticosterone ; puberty ; rat ; sex-difference ; fatigue ; mood state ; supplement ; resistance exercise ; speed ; repetition ; n/a ; metabolome ; skeletal muscle ; muscle contraction ; ergogenic effect ; bench press ; upper limb ; ergogenic substances ; time under tension ; 1RM test ; metabolites ; phenotyping ; CYP450 ; NAT ; xanthine oxidase ; actigraphy ; athletic ; anaerobic ; CMJ ; nutrition ; sport supplement ; Wingate ; electromyography ; efficiency ; sport ; expectancy ; belief ; perceptions ; placebo effect ; recovery ; strength ; power ; sprint performance ; menstrual cycle ; placebo ; ergogenic ; EEG–EMG coherence ; women ; exercise training ; velocity ; muscle function ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PS Biology, life sciences ; bic Book Industry Communication::J Society & social sciences::JF Society & culture: general::JFC Cultural studies::JFCV Food & society
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 25
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-02-24
    Description: The book deals with therapeutic monoclonal antibodies (mAbs) broadly, and relevant topics such as challenges and opportunities, next-generation antibody products, Antibody-Drug-Conjugates (ADC), bispecifics, glycosylation, and T-cell engagers are covered. Each topic has been written by leading groups around the world and the book should be of interest to researchers from both academia and industry.
    Keywords: therapeutic antibody ; stability ; aggregation ; manufacture challenges ; formulation ; antibodies ; site-specific conjugation ; bioconjugates ; ADC ; antibody-drug conjugates ; payloads ; linkers ; nucleic acids ; ADME ; developability ; glycosylation ; post-translational modifications ; pharmacokinetics ; effector functions ; antibody-dependent cell-mediated cytotoxicity ; complement-dependent cytotoxicity ; immunogenicity ; pharmacodynamics ; glycoengineering ; type III secretion system ; prophylaxis ; antibacterials ; antibiotics ; HIV/AIDS ; co-formulation ; high concentration ; analytical characterization ; antibody (s) ; T-cell engagers ; bispecific antibodies ; immunotherapy ; oncology ; antibody engineering ; immunological synapse ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::K Economics, finance, business & management::KN Industry & industrial studies::KND Manufacturing industries::KNDP Pharmaceutical industries
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 26
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-08-12
    Description: This colligated Special Issue of Pharmaceutics on Precision Medicine: Applied Concepts of Pharmacogenomics in Patients with Various Diseases and Polypharmacy offers to the reader a series of articles that describe the concept of Precision Medicine, discuss its implementation process and limitations, demonstrate its value by illustrating some clinical cases, and open the door to new and more sophisticated techniques and applications.
    Keywords: fibromyalgia (FM) ; myalgic encephalomyelitis/chronic fatigue syndrome (ME/CFS) ; microRNA ; miRNome ; pharmacogenomics ; pharmacoepigenomics ; SM2miR ; Pharmaco-miR ; repoDB ; ME/CFS Common Data Elements (CDEs) ; dihydropyrimidine dehydrogenase ; DPYD ; 5-fluorouracil ; fluoropyrimidine ; therapeutic drug monitoring ; orthotopic liver transplant ; busulfan ; glutathione S-transferase ; genetic polymorphism ; limited sampling strategy ; pharmacokinetics ; clinical pharmacogenetics ; pharmacogenetic testing ; adverse drug reactions ; genotype ; phenotype ; pharmacogene ; barriers to pharmacogenetics implementation ; Sub-Saharan Africa ; chronic low back pain (cLBP) ; genetics ; personalized treatment ; polymorphism ; CYP450 ; tacrolimus ; CYP3A5 ; liver transplant ; pharmacogenomic ; minority ; data collection ; drug ; biomarker ; pharmacogenetics ; pharmacogenetic test ; personalized medicine ; gene expression ; infliximab ; adalimumab ; ulcerative colitis ; Crohn disease ; inflammatory bowel disease ; n/a ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::M Medicine::MJ Clinical & internal medicine
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 27
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-09
    Description: The use of lipid-based nanosystems, including lipid nanoparticles (solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)), nanoemulsions, and liposomes, among others, is widespread. Several researchers have described the advantages of different applications of these nanosystems. For instance, they can increase the targeting and bioavailability of drugs, improving therapeutic effects. Their use in the cosmetic field is also promising, owing to their moisturizing properties and ability to protect labile cosmetic actives. Thus, it is surprising that only a few lipid-based nanosystems have reached the market. This can be explained by the strict regulatory requirements of medicines and the occurrence of unexpected in vivo failure, which highlights the need to conduct more preclinical studies.Current research is focused on testing the in vitro, ex vivo, and in vivo efficacy of lipid-based nanosystems to predict their clinical performance. However, there is a lack of method validation, which compromises the comparison between different studies.This book brings together the latest research and reviews that report on in vitro, ex vivo, and in vivo preclinical studies using lipid-based nanosystems. Readers can find up-to-date information on the most common experiments performed to predict the clinical behavior of lipid-based nanosystems. A series of 15 research articles and a review are presented, with authors from 15 different countries, which demonstrates the universality of the investigations that have been carried out in this area.
    Keywords: nanostructured lipid carriers (NLC) ; formulation optimization ; rivastigmine ; quality by design (QbD) ; nasal route ; nose-to-brain ; N-alkylisatin ; liposome ; urokinase plasminogen activator ; PAI-2 ; SerpinB2 ; breast cancer ; liposomes ; target delivery nanosystem ; FZD10 protein ; colon cancer therapy ; supersaturation ; silica-lipid hybrid ; spray drying ; lipolysis ; lipid-based formulation ; fenofibrate ; mesoporous silica ; oral drug delivery ; hyaluronic acid ; drug release ; light activation ; stability ; mobility ; biocorona ; dissolution enhancement ; phospholipids ; solid dosage forms ; porous microparticles ; nanoemulsion(s) ; phase-behavior ; DoE ; D-optimal design ; vegetable oils ; non-ionic surfactants ; efavirenz ; flaxseed oil ; nanostructured lipid carriers ; nanocarrier ; docohexaenoic acid ; neuroprotection ; neuroinflammation ; fluconazole ; Box‒Behnken design ; nanotransfersome ; ulcer index ; zone of inhibition ; rheological behavior ; ex vivo permeation ; nanomedicine ; cancer ; doxorubicin ; melanoma ; drug delivery ; ultrasound contrast agents ; phospholipid coating ; ligand distribution ; cholesterol ; acoustic response ; microbubble ; lipid phase ; dialysis ; ammonia ; intoxication ; cyanocobalamin ; vitamin B12 ; atopic dermatitis ; psoriasis ; transferosomes ; lipid vesicles ; skin topical delivery ; oligonucleotide ; self-emulsifying drug delivery systems ; hydrophobic ion pairing ; intestinal permeation enhancers ; Caco-2 monolayer ; clarithromycin ; solid lipid nanoparticles ; optimization ; permeation ; pharmacokinetics ; follicular targeting ; dexamethasone ; alopecia areata ; lipomers ; lipid polymer hybrid nanocapsules ; biodistribution ; skin ; ethyl cellulose ; n/a ; thema EDItEUR::T Technology, Engineering, Agriculture, Industrial processes::TB Technology: general issues
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 28
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-06-24
    Description: Drug–drug interactions (DDIs) cause a drug to affect other drugs, leading to reduced drug efficacy or increased toxicity of the affected drug. Some well-known interactions are known to be the cause of adverse drug reactions (ADRs) that are life threatening to the patient. Traditionally, DDI have been evaluated around the selective action of drugs on specific CYP enzymes. The interaction of drugs with CYP remains very important in drug interactions but, recently, other important mechanisms have also been studied as contributing to drug interaction including transport- or UDP-glucuronyltransferase as a Phase II reaction-mediated DDI. In addition, novel mechanisms of regulating DDIs can also be suggested. In the case of the substance targeted for interaction, not only the DDIs but also the herb–drug or food–drug interactions have been reported to be clinically relevant in terms of adverse side effects. Reporting examples of drug interactions on a marketed drug or studies on new mechanisms will be very helpful for preventing the side effects of the patient taking these drugs. This Special Issue aims to highlight current progress in understanding both the clinical and nonclinical interactions of commercial drugs and the elucidation of the mechanisms of drug interactions.
    Keywords: tadalafil ; ticagrelor ; drug-drug interaction ; pharmacokinetics ; plasma concentration ; CYP3A4 ; Loxoprofen ; CYP3A ; Dexamethasone ; Ketoconazole ; CYP2D6 ; O-desmethyltramadol ; physiologically-based pharmacokinetics ; tramadol ; (‒)-sophoranone ; CYP2C9 ; potent inhibition ; in vitro ; in vivo ; drug interaction ; low permeability ; high plasma protein binding ; biflavonoid ; cytochrome P450 ; drug interactions ; selamariscina A ; uridine 5′-diphosphoglucuronosyl transferase ; tissue-specific ; systemic exposure ; P-glycoprotein (P-gp) ; organic anion transporting polypeptide 1A2 (OATP1A2) ; Rumex acetosa ; fexofenadine ; chronic kidney disease ; drug–drug interactions ; polypharmacy ; adverse drug reactions ; Lexicomp ; subset analysis ; signal detection algorithms ; spontaneous reporting systems ; mechanism-based inhibition ; competitive inhibition ; non-competitive inhibition ; substrate ; inhibitor ; cytochromes P450 ; OATP1B1 ; OATP1B3 ; tyrosine kinase inhibitors ; drug-drug interactions ; migraine ; lasmiditan ; gepants ; monoclonal antibodies ; CYP1A1 ; CYP1A2 ; drug–drug interaction ; expression ; metabolism ; regulation ; drug transporter ; ubiquitination ; ixazomib ; DDI ; computational prediction ; in silico ; QSAR ; drug metabolism ; ADME ; CYP ; metabolic DDI ; P450 ; 1A2 ; 2B6 ; 2C19 ; 2C8 ; 2C9 ; 2D6 ; 3A4 ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PS Biology, life sciences
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 29
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-08-12
    Description: This book collects contributions published in the Special Issue “From a Molecule to a Drug: Chemical Features Enhancing Pharmacological Potential” and dealing with successful stories of drug improvement or design using classic protocols, quantum mechanical mechanistic investigation, or hybrid approaches such as QM/MM or QM/ML (machine learning). In the last two decades, computer-aided modeling has strongly supported scientists’ intuition to design functional molecules. High-throughput screening protocols, mainly based on classical mechanics’ atomistic potentials, are largely employed in biology and medicinal chemistry studies with the aim of simulating drug-likeness and bioactivity in terms of efficient binding to the target receptors. The advantages of this approach are quick outcomes, the possibility of repurposing commercially available drugs, consolidated protocols, and the availability of large databases. On the other hand, these studies do not intrinsically provide reactivity information, which requires quantum mechanical methodologies that are only applicable to significantly smaller and simplified systems at present. These latter studies focus on the drug itself, considering the chemical properties related to its structural features and motifs. Overall, such simulations provide necessary insights for a better understanding of the chemistry principles that rule the diseases at the molecular level, as well as possible mechanisms for restoring the physiological equilibrium.
    Keywords: SARS-CoV-2 ; benzoic acid derivatives ; gallic acid ; molecular docking ; reactivity parameters ; selenoxide elimination ; one-pot ; imine-enamine ; reaction mechanism ; DFT calculations ; selenium ; anti-inflammatory drugs ; QSAR ; pain management ; cyclooxygenase ; multitarget drug ; cannabinoid ; neuropathic pain ; clopidogrel ; NMR study ; oxone ; peroxymonosulfate ; sodium halide ; thienopyridine ; drug discovery ; precision medicine ; pharmacodynamics ; pharmacokinetics ; coronavirus SARS-CoV-2 ; COVID-19 ; 3-chymotrypsin-like protease ; pyrimidonic pharmaceuticals ; molecular dynamics simulations ; binding free energy ; β-carrageenan ; antioxidant activity ; Box-Behken ; extraction ; Eucheuma gelatinae ; physic-chemistry ; rheology ; quercetin ; quercetin 3-O-glucuronide ; cisplatin ; nephrotoxicity ; cytoprotection ; lithium therapy ; neurocytology ; toxicology ; neuroprotection ; chemoinformatics ; big data ; methadone hydrochloride ; pharmaceutical solutions ; drug compounding ; high performance liquid chromatography ; stability study ; microbiology ; fucoidan ; alginate ; L-selectin ; E-selectin ; MCP-1 ; ICAM-1 ; THP-1 macrophage ; monocyte migration ; protein binding ; breast milk ; M/P ratio ; statistical modeling ; molecular descriptors ; chromatographic descriptors ; affinity chromatography ; anti-ACE ; anti-DPP-IV ; gastrointestinal digestion ; in silico ; molecular dynamics ; paramyosin ; seafood ; target fishing ; n/a ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::M Medicine::MM Other branches of medicine::MMG Pharmacology
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 30
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-07-06
    Description: Since first receiving approval in 1986, antibody-based therapeutics have been the most successful modality for the treatment of various diseases. This Special Issue of IJMS, “Recent Advances in Antibody Therapeutics”, presents leading-edge articles and reviews for discovery, development, and clinical applications of therapeutic antibodies, covering antibody drug conjugates (ADCs), GPCR-targeting antibodies, a functional antibody screening, bioassay of bispecific antibodies, antibody applications for cardiovascular diseases, antibody delivery to CNS, etc. The excellent studies in this Special Issue would valuable insight for scientists and clinicians in the field of therapeutic antibodies
    Keywords: interleukin 33 ; ST2 receptor ; scFv ; C2_2E12 ; bladder cancer ; antibodies ; immune checkpoint inhibitors ; antibody-drug conjugates ; sacituzumab govitecan ; enfortumab vedotin ; erdafitinib ; cost-effectiveness ; G protein-coupled receptor ; membrane protein ; antigen ; therapeutic antibody ; anti-angiogenesis ; delta-like ligand ; irinotecan ; paclitaxel ; VEGF ; SARS-CoV-2 ; spike protein ; receptor-binding domain ; phage display ; monoclonal antibody ; cytomegalovirus ; peptide/major histocompatibility complex class I complex ; T-cell-receptor-like antibody ; affinity maturation ; yeast surface display ; combinatorial antibody library ; agonist antibody ; cell fate ; bispecific antibodies ; bioassays ; mechanisms of action ; binding assays ; potency assays ; atherosclerosis ; inflammation ; antibody therapy ; blood–brain barrier ; antibody ; pharmacokinetics ; disposition ; biochemical and physicochemical properties ; Fc binding ; receptor-mediated transcytosis ; brain shuttle ; molecular Trojan horse ; transferrin ; anti-cancer antibody ; antibody engineering ; biophysical properties ; computational methods ; research cell bank ; antibody therapeutics ; recombinant antibodies ; intracellular antibodies ; single-chain antibody fragment ; nanobody ; Human papillomaviruses ; HPV oncoproteins ; HPV-associated cancer ; HPV cancer therapy ; asthma ; refractory asthma ; biomarker ; n/a ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PN Chemistry
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 31
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-10-25
    Description: Functional nutrition is deeply connected with healthy lifestyle and sustainable food production, due to its positive health benefits and the use of economically underexplored and natural raw materials. Expectedly, it appeals to large number of interested consumers while becoming lucrative segment of the food industry with a fast-growing market fueled by new sociodemographic trends. Accordingly, functional juices and beverages made of indigenous fruits are interesting niche for various food market stakeholders. Here, biologically active compounds (BACs) and probiotics that have positive health effects in functional foods (juices) are mostly thermolabile. This is especially important for industry that still employs classical heat treatments (e.g., pasteurization), while being concerned with degradation of food quality in the final products. To prevent this, focus is on designing economic and ecological technologies that are able to preserve nutritional and sensory quality while maintaining microbiological stability in products. Such approaches are based on low-energy consumption and low-impact processing, e.g. “hurdle technology” that combines advanced and conventional methods (e.g., high-power ultrasound, pulse electric field). Food design is another important focus point for consumers’ sensory appeal and economic success of foods. Hence, technologies as 3D food printing can be particularly useful for manufacturing. Based on the above, presented topics are relevant to sustainable functional food production, functional fruit juices, BACs, “hurdle technology,” advanced food processing, 3D food printing, and authentic fruits.
    Keywords: dehydration ; conserving vegetables ; improving shelf-life ; rehydrated pepper ; histological preparation ; green practices ; meat analogue ; liquid additives ; soy protein isolate ; lecithin ; emulsion ; functional fruit juice ; hurdle technology ; non-thermal processing ; preservation ; quality ; probiotic ; fruit by-products ; lulo bagasse powder ; fiber ; antioxidant properties ; carotenoids ; cocoa shell ; high voltage electrical discharge ; tannin ; dietary fiber ; water binding capacity ; grindability ; traditional ; slow ; pressure and microwave cooking ; polyphenols ; antioxidant activity ; faba bean ; lentil ; pea ; probiotic safety ; toxicity ; pathogenicity ; functional food industry ; pharmacological interactions ; functional fruit juices ; mushroom ; vitamin D ; reducing capacity ; glycation ; Lactuca sativa ; metabolomics ; antioxidants ; eustress ; total soluble solids ; particle size distribution ; total anthocyanin content ; antioxidant capacity ; non-dairy beverages ; pulses ; chickpea ; lupin ; flow behavior ; animal and plant proteins ; computer vision system ; nutritional value ; texture ; water activity ; viscosity ; microstructure ; heavy metals ; amino acids ; pesticide ; fruit wastes ; vegetable wastes ; drying ; extraction ; intensification technologies ; phenolic acids ; food processing ; minimally processed foods ; UHLPC-MS/MS ; sous-vide cooking ; vegetables ; seafood ; cephalopods ; safety ; nutritive quality ; beetroot ; convective drying ; infrared drying ; purée ; Fourier-transform infrared spectroscopy ; confocal scanning microscopy ; fruit juice ; interaction ; drug ; phytochemical ; pharmacokinetics ; ginger ; pineapple ; turmeric ; juice mix ; physicochemical properties ; microbiological quality ; sensory attributes ; Diospyros kaki ; post-harvest losses ; dehydrated persimmon ; thin-layer modeling ; drying rate ; old apple cultivar ; biologically active compounds ; functional food ; agriculture ; extensive farming ; bisphosphonates ; SERMs ; food ; supplements ; bioavailability ; meal ; coffee ; juice ; mineral water ; edible mushroom ; nutrition ; phenolic compounds ; vacuum ; poria cubes ; optimization ; stage drying ; n/a ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PS Biology, life sciences ; bic Book Industry Communication::T Technology, engineering, agriculture
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 32
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-10-25
    Description: In this Topical Collection, ten articles (one review and nine research articles) are published in a time span of 2021–2022. All articles are written by experts in the field of Separation Techniques who were invited to contribute to the presentation of the current status in separation science. The authors were invited to answer the questions: What is the state-of-the-art in Separation Sciences? What advances have been reported recently? Last but not least, what are the future perspectives? The Editor and authors hope that the readers will find valuable information in the topic.
    Keywords: protein-based chiral stationary phase ; alpha 1-acid glycoprotein ; chiral recognition mechanism ; molecular docking ; proteomics ; high-performance liquid chromatography ; mass spectrometry ; gout ; uric acid ; Salvia miltiorrhiza ; HPLC-MS/MS ; pharmacokinetics ; wine-processed ; hydrophilic interaction liquid chromatography ; chromatography ; oligopeptides ; acetyl hexapeptide-8 ; acetyl hexapeptide-3 ; Argireline ; cosmetics ; SARS-CoV-2 ; virus particles ; air filtering ; aerosols ; probability distributions ; rotational particle separator ; air separation ; steam methane reforming ; water gas shift ; alternative fluids ; gas turbine ; Senecio anteuphorbium ; response factors ; true quantitation ; allelopathy ; herbicide ; chlorpropham ; potato ; μQuEChERS/UHPLC-PDA ; validation ; cooking ; methyl nicotinate ; methyl salicylate ; ethyl salicylate ; 2-hydroxyethyl salicylate ; pain relief spray ; Tulasnellaceae sp. ; Gymnadenia orchidis ; mdium-pressure liquid chromatography ; reversed-phase liquid chromatography ; ergosterol ; bic Book Industry Communication::G Reference, information & interdisciplinary subjects::GP Research & information: general ; bic Book Industry Communication::P Mathematics & science::PN Chemistry
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 33
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2022-06-21
    Description: There have been recent significant improvements in the short-term survival of solid organ transplantation patients due to advances in immunosuppression and transplant techniques. However, long-term graft survival has still lagged behind other outcomes and has now become one of the main problems in solid organ transplantation.For this Special Issue, we invited researchers and clinicians to submit studies on solid organ transplantation. These have provided us with additional knowledge and skills that will ultimately help us to improve outcomes after solid organ transplantation.
    Keywords: living donation ; nephrectomy ; hand-assisted laparoscopic nephrectomy ; body composition ; complications ; simultaneous pancreas-kidney transplantation ; immunosuppression ; graft order ; sequence ; outcome ; survival ; kidney transplantation ; hydrogen ; diarrhea ; small intestinal bacterial overgrowth ; sickle cell disease ; sickle cell ; transplantation ; outcomes ; big data ; tacrolimus ; metabolism ; C/D ratio ; cholesterol ; dyslipidemia ; LDL-C ; liver transplantation ; hematuria ; chronic kidney disease ; tocilizumab ; clazakizumab ; desensitization ; anti-HLA alloantibody ; post traumatic growth ; psychiatric morbidity ; network analysis ; ESAS ; MINI ; CPC ; DCPR ; distress ; demoralization ; alexithymia ; anxiety ; antibody-mediated rejection ; recurrent primary disease ; renal transplantation ; pancreas transplantation ; cold ischemia time ; delayed graft function ; Eurotransplant Senior Program ; end-stage renal disease ; intensive care unit ; bioimpedance analysis ; drug dosing ; lean body mass index ; pharmacokinetics ; tacrolimus C/D ratio ; mineral bone disorder ; parathyroidectomy ; parathyroid hormone ; osteoporosis ; bone fractures ; Contrast-enhanced ultrasound ; kidney perfusion ; kidney function ; kidney donation ; n/a ; bic Book Industry Communication::M Medicine ; bic Book Industry Communication::M Medicine::MM Other branches of medicine::MMG Pharmacology
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 34
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-12-21
    Description: Development of strategies to assist the movement of poorly permeable molecules across biological barriers has long been the goal of drug delivery science. In the last three decades, there has been an exponential increase in advanced drug delivery systems that aim to address this issue. However, most proprietary delivery technologies that have progressed to clinical development are based on permeation enhancers (PEs) that have a history of safe use in man. This Special Issue entitled “Transmucosal Absorption Enhancers in the Drug Delivery Field” aims to present the current state-of-the-art in the application of PEs to improve drug absorption. Emphasis is placed on identification of novel permeation enhancers, mechanisms of barrier alteration, physicochemical properties of PEs that contribute to optimal enhancement action, new delivery models to assess PEs, studies assessing safety of PEs, approaches to assist translation of PEs into effective oral, nasal, ocular and vaginal dosage forms and combining PEs with other delivery strategies.
    Keywords: R5-920 ; RM1-950 ; chitosan ; intestinal epithelial cells ; ocular delivery ; amphiphilic polymers ; cornea ; tight junction modulator ; cyclodextrin ; permeability ; gemini surfactant ; transferrin ; compound 48/80 ; epithelial permeability ; cervicovaginal tumors ; nanoparticles ; confocal laser scanning microscopy ; safety ; formulation ; salcaprozate sodium ; intestinal absorption ; FITC-dextran ; curcumin ; block copolymers ; nasal vaccination ; whole leaf ; brush border ; ocular drug delivery ; vaccine adjuvant ; nanoparticle ; nasal delivery ; efflux ; permeation enhancers ; absorption enhancers ; nose to brain delivery ; small intestine ; epithelium ; CNS disorders ; absorption modifying excipients ; insulin ; absorption enhancer ; gel ; intestinal delivery ; thermogel system ; Caco-2 ; biocompatibility studies ; absorption enhancement ; man ; PN159 ; poorly absorbed drug ; tryptophan ; tight junction ; oral macromolecule delivery ; penetration enhancer ; intestinal permeation enhancers ; nanocrystals ; simvastatin ; nanomedicine ; enterocyte ; N-dodecyl-?-D-maltoside (DDM) ; cell-penetrating peptide ; quaternization ; KLAL ; nasal ; nasal permeability ; transmucosal drug delivery ; Caco-2 cells ; mast cell activator ; penetration enhancers ; drug delivery ; nose-to-brain ; bioenhancer ; polymeric micelles ; mucoadhesion ; cell-penetrating peptide (CPP) ; simulated intestinal fluid ; vaginal delivery ; nasal formulation ; pharmacokinetic interaction ; sodium caprate ; clinical trial ; transmucosal permeation ; drug absorption enhancer ; sugar-based surfactants ; nanocapsules ; imatinib ; teriparatide ; osteoporosis ; hydrophobization ; F-actin ; combined microsphere ; transepithelial electrical resistance ; oral delivery ; ocular conditions ; metabolism ; antimicrobial peptide ; permeation enhancer ; drug administration ; antiepileptic drug ; amino acid ; in vivo studies ; sodium cholate (NaC) ; epithelial transport ; preclinical ; nose to brain transport ; pharmacokinetics ; chitosan derivatives ; ophthalmology ; tight junctions ; sheep ; cationic functionalization ; GLP-1 ; pulmonary ; and liposome ; cytochrome P450 ; claudin ; P-glycoprotein ; in situ hydrogel ; mucoadhesiveness ; PTH 1-34 ; Aloe vera ; oral peptides ; bic Book Industry Communication::M Medicine
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 35
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-05
    Description: The year 2019 has been prolific in terms of new evidence regarding the effects of coffee and caffeine consumption on diverse aspects of human functioning. This book collects 20 high-quality manuscripts published in Nutrients that include original investigation or systematic review studies of the effects of caffeine intake on human performance and health. The diversity of the articles published in this Special Issue highlights the extent of the effects of coffee and caffeine on human functioning, while underpinning the positive nature of most of these effects. This book will help with understanding why the natural sources of caffeine are so widely present in the nutrition behaviors of modern society.
    Keywords: QH301-705.5 ; Q1-390 ; TX341-641 ; NAT ; n/a ; supplementation ; EEG–EMG coherence ; muscle function ; tea ; fatigue ; ergogenic ; adrenal gland ; skeletal muscle ; xanthine oxidase ; placebo ; CMJ ; efficiency ; colorectal cancer ; rat ; pregnancy ; coffee/caffeine ; Wingate ; 1RM test ; supplement ; actigraphy ; athletic ; systematic review and meta-analysis ; women ; consumption motives ; resistance training ; cancer prevention ; sport supplement ; exercise ; DOMS ; placebo effect ; sprint performance ; power ; behavior ; belief ; health ; perceptions ; exercise performance ; ergogenic aid ; electromyography ; ergogenic effect ; corticosterone ; metabolome ; mood state ; muscle contraction ; strength ; energy drink ; repetition ; responders ; perception ; anaerobic ; CYP450 ; puberty ; energy drinks ; isokinetic testing ; individual responses ; phenotyping ; nutrition ; time under tension ; menstrual cycle ; exercise training ; RPE ; ergogenic substances ; upper limb ; elite athlete ; recovery ; speed ; epidemiology ; caffeine ; sex-difference ; bench press ; pharmacokinetics ; sport performance ; ergogenic aids ; expectancy ; consumer ; football ; newborn ; velocity ; metabolites ; performance ; coffee ; prospective studies ; resistance exercise ; sport ; thema EDItEUR::P Mathematics and Science::PS Biology, life sciences
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 36
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-05
    Description: The amide bond represents a privileged motif in chemistry. The recent years have witnessed an explosion of interest in the development of new chemical transformations of amides. These developments cover an impressive range of catalytic N–C bond activation in electrophilic, Lewis acid, radical, and nucleophilic reaction pathways, among other transformations. Equally relevant are structural and theoretical studies that provide the basis for chemoselective manipulation of amidic resonance. This monograph on amide bonds offers a broad survey of recent advances in activation of amides and addresses various approaches in the field.
    Keywords: QD1-999 ; Q1-390 ; QD450-801 ; N-heterocyclic carbene ; non planar amide ; ruthenium (Ru) ; physical organic chemistry ; gemcitabine prodrug ; pyramidal amides ; bridged sultams ; catalysis ; dipeptides ; N-(1-naphthyl)acetamide ; C-N ? bond cleavage ; steric effects ; peptide bond cleavage ; transition-metal-free ; palladium ; N-heterocyclic carbenes (NHCs) ; addition reaction ; C–O activation ; rhodium ; metal complexes ; carbanions ; thioamidation ; amide bond ; intramolecular catalysis ; antiviral activity ; additivity principle ; pre-catalysts ; C–N bond cleavage ; bridged lactams ; C–H acidity ; arynes ; twisted amides ; organic synthesis ; amination ; Suzuki-Miyaura ; tert-butyl ; cyclopentadienyl complexes ; C-S formation ; enzymes ; DFT study ; sulfonamide bond ; N ; HERON reaction ; primaquine ; entropy ; amide activation ; amidation ; synthesis ; amide hydrolysis ; carbonylicity ; amide bond activation ; amide bond resonance ; aminosulfonylation ; molecular dynamics ; model compound ; in situ ; amide ; homogeneous catalysis ; heterocycles ; anomeric effect ; multi-component coupling reaction ; kinetic ; excited state ; C–H bond cleavage ; palladium catalysis ; amides ; thiourea ; formylation ; alkynes ; cis/trans isomerization ; amide C–N bond activation ; intein ; C-H functionalization ; succindiamide ; amide bonds ; crown ether ; aminoacylation ; directing groups ; cytostatic activity ; reaction thermodynamics ; acyl transfer ; transition metals ; N-dimethylformamide ; DMAc ; acylative cross-coupling ; C-H/C-N activation ; nickel catalysis ; antibacterial screening ; sodium ; aryl thioamides ; Winkler-Dunitz parameters ; catalyst ; N-dimethylacetamide ; base-catalyed hydrolysis ; nitrogen heterocycles ; cross-coupling ; insertion ; amidicity ; nitro-aci tautomerism ; activation ; carbonylation ; transamidation ; amine ; distortion ; Pd-catalysis ; rotational barrier energy ; hypersensitivity ; N–C activation ; metabolic stability ; [2+2+2] annulation ; twisted amide ; protease ; cyanation ; amide resonance ; trialkylborane ; catalysts ; biofilm eradication ; pharmacokinetics ; pancreatic cancer cells ; DMF ; aryl esters ; Michael acceptor ; fumardiamide ; water solvation ; ester bond activation ; cyclization ; nuclear magnetic resonance ; secondary amides ; reaction mechanism ; density functional theory ; density-functional theory ; amino acid transporters ; thema EDItEUR::P Mathematics and Science::PN Chemistry
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 37
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-12-21
    Description: Drug metabolism/pharmacokinetics and drug interaction studies have been extensively carried out in order to secure the druggability and safety of new chemical entities throughout the development of new drugs. Recently, drug metabolism and transport by phase II drug metabolizing enzymes and drug transporters, respectively, as well as phase I drug metabolizing enzymes, have been studied. A combination of biochemical advances in the function and regulation of drug metabolizing enzymes and automated analytical technologies are revolutionizing drug metabolism research. There are also potential drug–drug interactions with co-administered drugs due to inhibition and/or induction of drug metabolic enzymes and drug transporters. In addition, drug interaction studies have been actively performed to develop substrate cocktails that do not interfere with each other and a simultaneous analytical method of substrate drugs and their metabolites using a tandem mass spectrometer. This Special Issue has the aim of highlighting current progress in drug metabolism/pharmacokinetics, drug interactions, and bioanalysis.
    Keywords: R5-920 ; RM1-950 ; human liver microsomes ; alcohol addiction ; UGT ; ultra-high-pressure liquid chromatography ; adalimumab ; procainamide ; LC-MS/MS ; DA-9805 ; paeonol ; LC-QTOF-MS/MS ; YRA-1909 ; chlorogenic acid ; immunoprecipitation ; Eurycoma longifolia ; CYP ; caffeic acid ; rat ; pharmaceutical excipient ; Korean red ginseng extract ; Stauntonia hexaphylla leaf extract ; bioanalysis ; HPLC-MS/MS ; B6 ; eurycomanone ; bioavailability ; drying technology ; GB3 ; diclofenac ; 129-Glatm1Kul/J ; aglycone ; caffeic acid O-glucuronides ; organic anion transporting polypeptide ; protein precipitation ; metabolic stability ; Fabry disease ; biopharmaceuticals ; imperatorin ; neochlorogenic acid ; gastric ulcer ; saikosaponin a ; hair ; anthraquinone ; acetyl tributyl citrate ; pharmacokinetics ; brain distribution ; mematine ; ethyl glucuronide ; pharmacokinetic ; loxoprofen ; liquid chromatography-quadrupole TOF MS ; glucuronidation ; esomeprazole ; metformin ; cytochrome P450 ; glycoside ; AUDIT score ; protein stability ; efficacy ; LC-HR/MS ; cryptochlorogenic acid ; aceclofenac ; drug interaction ; liquid chromatography-tandem mass spectrometry ; Osthenol ; plasma ; N-acetylprocainamide ; diabetes ; bic Book Industry Communication::M Medicine
    Language: English
    Format: image/jpeg
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 38
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-03-27
    Description: Sprouted grains are food ingredients widely appreciated for their improved nutritional, functional, organoleptic, and textural properties compared with non-germinated grains. In recent years, sprouting has been explored as a promising green food engineering strategy to improve the nutritional value of grains and the formation of secondary metabolites with potential application in the functional food, nutraceutical, pharmaceutical, and cosmetic markets. However, little attention has been paid to the impact of sprouting on the chemical composition, safety aspects, and technofunctional and chemopreventive properties of sprouted seeds and their derived flours and byproducts. The six articles included in this Special Issue present insightful findings on the most recent advances regarding new applications of sprouted seeds or products derived thereof, evaluations of the nutritional value and phytochemical composition of sprouts during production or storage, and explorations of their microbiological, bioactive, and technofunctional properties.
    Keywords: biochemical characteristic ; enzymatic browning ; inhibitory profile ; lentil ; sprouts ; polyphenol oxidase ; purification ; germinated oat ; avenanthramides ; colorectal cancer ; chemoprevention ; bran ; cell walls ; sprouting ; dough rheology ; bread-making ; microstructure ; barley ; germination ; flour ; RSM ; nutritional properties ; bioactive compounds ; quality ; melatonin ; bioavailability ; lentil sprouts ; phenolic compounds ; antioxidant status ; pharmacokinetics ; food safety ; legumes ; microbial contamination ; protein ; mineral ; seed germination ; nutritional value ; phytochemicals ; bioactivity ; health ; technological properties ; food development ; functional foods ; thema EDItEUR::G Reference, Information and Interdisciplinary subjects::GP Research and information: general
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 39
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-05
    Description: Throughout most of history, medicinal plants and their active metabolites have represented a valuable source of compounds used to prevent and to cure several diseases. Interest in natural compounds is still high as they represent a source of novel biologically/pharmacologically active compounds. Due to their high structural diversity and complexity, they are interesting structural scaffolds that can offer promising candidates for the study of new drugs, functional foods, and food additives.Plant extracts are a highly complex mixture of compounds and qualitative and quantitative analyses are necessary to ensure their quality. Furthermore, greener methods of extraction and analysis are needed today.This book is based on articles submitted for publication in the Special Issue entitled “Qualitative and Quantitative Analysis of Bioactive Natural Products” that collected original research and reviews on these topics.
    Keywords: QH301-705.5 ; Q1-390 ; Scorzonera ; capsaicinoids ; artificial neural network ; cerebral ischemia reperfusion injury ; antioxidant activity ; quality evaluation ; chemometrics ; secondary metabolites ; identification ; antioxidant capacity ; Moroccan region ; volatile compounds ; HPLC-Q-Exactive-Orbitrap-MS ; quantitative analysis ; amino acids content ; HPLC-ELSD ; antioxidant ; autophagy ; quantification ; sugars ; 1-triacontanol ; hemp seed oil ; Alzheimer’s disease ; macrodiolides ; extraction ; recycling preparative high performance liquid chromatography ; HPLC methods ; GC-MS ; Myristica fragrans ; Rossa da inverno sel. Rojo Duro onion cultivar ; fruit powders ; decursin ; food traceability ; ionic liquids ; separation optimisation ; Spondias spp. ; C-glycosylflavone ; wine ; UPLC-MS ; scutellarein ; saffron ; carotenoids ; red cabbage ; hydrodistillation ; Ginkgo biloba Extract (GBE) ; gas chromatography ; organic acids ; olive leaves ; crocins ; CBD oil ; Bolbostemma paniculatum ; UPLC-ESI-MS/MS ; geographical origin ; HPLC ; traditional Chinese medicine decoction ; liquid chromatography ; bioactive natural compounds ; Podospermum ; metabolic profiling ; SPME-GC/MS ; LTQ-Orbitrap ; oral administration ; UPLC ; bioactive compounds ; Erigeron breviscapus extract ; terrain conditions ; nutmeg ; antibacterial activity ; method validation ; ShenFu prescription decoction ; chili ; decursinol angelate ; statistical evaluations ; stereoselective and simultaneous analysis ; curcuminoids ; Talaromyces pinophilus ; talarodiolide ; HPLC-Q-TOF-MS/MS ; Olea europaea L. ; triterpenes ; chromatogram-bioactivity correlation ; essential oil ; stability ; Staphylococcus aureus ; Iris lactea Pall. var. chinensis (Fisch.) Koidz. ; endothelial function ; anthocyanins ; HPLC analysis ; liquid chromatography-mass spectrometry ; nodakenin ; turmerone ; UHPLC-MS/MS ; Quercus acuta leaf ; Curcuma longa ; UHPLC analysis ; ginseng berry extract ; geographical variation ; qualitative analysis ; Sorbus ; free radical-scavenging ; ginsenosides ; flavonoids ; biostimulant ; GC/MS ; terpenes ; aleuritolic acid ; phenolic compounds ; apoptosis ; response surface methodology ; phenolic acids ; pharmacokinetics ; mass spectrometry ; scutellarin ; multivariate statistical analysis ; phenolics ; MODDE experimental design ; proanthocyanidins ; UFLC-QQQ-MS ; rice ; cannabidiol ; odor-activity values ; UPLC-QTOF-MS ; turmeric ; decursinol ; thema EDItEUR::P Mathematics and Science::PS Biology, life sciences
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 40
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-05
    Description: This book entitled “Cocoa, Chocolate, and Human Health” presents the most recent findings about cocoa and health in 14 peer-reviewed chapters including nine original contributions and five reviews from cocoa experts around the world. Bioavailability and metabolism of the main cocoa polyphenols, i.e., the flavanols like epicatechin, are presented including metabolites like valerolactones that are formed by the gut microbiome. Many studies, including intervention studies or epidemiological observations, do not focus on single compounds, but on cocoa as a whole. This proves the effectiveness of cocoa as a functional food. A positive influence of cocoa on hearing problems, exercise performance, and metabolic syndrome is discussed with mixed results; the results about exercise performance are contradictive. Evidence shows that cocoa flavanols may modulate some risk factors related to metabolic syndrome such as hypertension and disorders in glucose and lipid metabolism. However, several cardiometabolic parameters in type 2 diabetics were not affected by a flavanol-rich cocoa powder as simultaneous treatment with pharmaceuticals might have negated the effect of cocoa. The putative health-promoting components of cocoa are altered during processing like fermentation, drying, and roasting of cocoa beans. Chocolate, the most popular cocoa product, shows remarkable losses in polyphenols and vitamin E during 18 months of storage.
    Keywords: QH301-705.5 ; Q1-390 ; TX341-641 ; n/a ; lipids ; theobromine ; colonic bacteria ; ?-glucosidase inhibition ; cacao ; tinnitus ; antioxidant capacity ; metabolomics ; methylxanthines ; lipid status ; physical exercise ; skeletal muscle ; functional volatile compounds ; soluble cocoa products ; blood pressure ; flavanols ; functional food ; classification ; monitoring ; cocoa ; yeast ; quality ; flavanols bioavailability ; fermentation ; cocoa processing ; hearing loss ; Italian chocolate ; chocolate ; (?)-catechin ; extraction and characterization methods ; heath potentials ; CREB ; inflammation ; flavanol-rich cocoa ; behavior ; (?)-epicatechin ; BDNF ; plasma appearance ; flavan-3-ol stereoisomers ; fermentation-related enzymes ; angiotensin-converting enzyme (ACE) inhibitory activity ; type 2 diabetes ; CaMKII ; exercise performance ; anti-inflammatory properties ; (+)-catechin ; bioactive compounds ; chiral separation ; plasma ; oxidative stress ; antidiabetic capacity ; polyphenols ; oligopeptides ; urine ; protein–phenol interactions ; postprandial ; working memory ; procyanidins ; simulated gastrointestinal digestion ; cocoa-based ingredients ; one-compartment model ; cocoa beans ; athlete ; biomarkers ; polyphenol ; metabolic syndrome ; nutrition ; bioavailability ; roasting ; glucose metabolism ; cohort study ; plasma nutrikinetics ; pharmacokinetics ; human ; cocoa proteins ; metabolites ; cocoa by-product ; meal ; bioactive peptides ; performance ; liquid chromatography coupled to electrospray ionisation and quadrupole time-of-flight mass spectrometry (LC-ESI-QToF-MS) ; starter culture ; thema EDItEUR::P Mathematics and Science::PS Biology, life sciences
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 41
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2024-04-05
    Description: Carotenoids are a group of natural pigments, consisting of more than 750 compounds. They are mostly yellow, orange, or red in color, due to the system of conjugated double bonds. This structural element is also responsible for the good antioxidant properties of many carotenoids. Carotenoids have shown numerous biological activities (not only as provitamin A), e.g., preventive properties of fruits and vegetables. As lipophilic compounds, their uptake and storage in the body are dependent on various conditions. In vitro and in vivo data showed stimulating and inhibitory effects of matrix compounds on bioaccessibility and bioavailability of carotenoids.
    Keywords: QH301-705.5 ; Q1-390 ; singlet-triplet annihilation ; silicon carotenoids ; dye-sensitized solar cells ; spent coffee grounds ; astaxanthin ; antioxidant antagonism ; carotenoid and chlorophyll derivatives ; fluorocarotenoids ; RNS ; feed processing ; ?-carotene ; iodocarotenoids ; hydrophilic ; selenium carotenoids ; free radical kinetics ; mechanisms ; stability ; free radicals ; antioxidant ; soil amendment ; pressurized fluid extraction ; extraction ; metal ions ; lutein ; lettuce ; lycopene ; antioxidant synergism ; iron carotenoids ; ROS ; solubility ; flavonoids ; bromocarotenoids ; sulfur carotenoids ; marine carotenoids ; cationic lipid ; carotenoids ; antioxidants ; nelfinavir ; fruit ; SK-Hep-1 ; carotenoid ; storage ; vegetables ; ethanol ; exon skipping ; inflammation ; xanthophylls ; Duchenne muscular dystrophy ; pharmacokinetics ; carrots ; chlorocarotenoids ; chelating compound ; cardiovascular disease ; ageing ; accelerated solvent extraction ; nitrogen carotenoids ; VEGF ; chlorophyll ; liquid chromatography ; antiradical ; PEG conjugates ; injection solvent ; cycloaddition ; HIV ; esterification ; antisense oligonucleotide ; B16F10 ; interaction ; cancer chemoprevention ; antireductant ; PC-3 ; oxidative stress ; thema EDItEUR::P Mathematics and Science::PS Biology, life sciences
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 42
    facet.materialart.
    Unknown
    MDPI - Multidisciplinary Digital Publishing Institute
    Publication Date: 2023-12-21
    Description: Canada continues to have a rich history of ground-breaking research in drug delivery within academic institutions, pharmaceutical industry and the biotechnology community.
    Keywords: R5-920 ; RM1-950 ; encapsulation ; biodistribution ; pharmaceutics ; targeted therapies ; gambogic acid ; GE11 peptide ; formulation and dosage form development ; transient modulation ; ROESY NMR spectroscopy ; bioaccessibility ; polymeric micelle ; pharmacological Inhibitors of HIF-1 and STAT3 ; nanoparticles ; Vitamin D ; drug discovery ; EGFR-targeted therapy ; translational research ; clinical trials ; doxorubicin ; dissolution ; drug development ; permeation enhancers ; Canada ; plant ; primary central nervous system lymphomas ; photostabilizers ; head and neck squamous cell carcinoma ; mouse models ; drug delivery systems ; melphalan ; hypoxia-induced chemoresistance ; skin ; virus ; circadian clock ; child friendly formulation ; adenanthin ; co-delivery ; canola oil deodorizer distillate ; Metaplex ; innovation ; controlled drug delivery ; nifedipine ; radiolabeling ; amphotericin B ; biological barriers ; blood-brain barrier (BBB) ; biologicals ; lipid nanoparticles ; oral formulation ; phytosterols ; medical devices ; chronotherapy ; oral ; cationic gemini surfactant ; route of administration ; drug delivery ; intra-arterial chemotherapy ; developing world ; sustained delivery ; water miscible solvents ; combination therapy ; antibodies ; throughput ; magnetic fields ; liposomes ; medulloblastoma ; drug-resistant melanoma ; rosmarinic acid ; topical formulation ; TNO gastrointestinal model ; gastrointestinal simulator ; malignant gliomas ; transdermal drug delivery ; oral delivery ; precision medicine ; 3D spheroid ; flavonoids ; staurosporine ; DOX-Vit D ; loading gradients ; bacteriophage ; phospholipid complex ; triggered drug release ; HIF-1 ; phage display ; pharmacokinetics ; emulsion ; quercetin ; cisplatin ; parasitic infections ; remote loading ; HAV6 cadherin peptide ; blood-brain barrier ; inclusion complex ; tocopherols ; STAT3 ; ultrasound ; liposome ; fungal infections ; magnetic resonance imaging (MRI) ; MG63 ; model orange juice ; radiation ; cancer ; mefloquine ; small molecules ; bic Book Industry Communication::M Medicine
    Language: English
    Format: application/octet-stream
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 43
    Keywords: Biomass conversion ; Biotechnology ; Chemical Engineering ; Chemistry industry ; Industrial Chemistry ; Kent ; Riegel ; biochemical engineering
    Description / Table of Contents: Substantially revising and updating the classic reference in the field, this handbook offers a valuable overview and myriad details on current chemical processes, products, and practices. No other source offers as much data on the chemistry, engineering, economics, and infrastructure of the industry. The Handbook serves a spectrum of individuals, from those who are directly involved in the chemical industry to others in related industries and activities. It provides not only the underlying science and technology for important industry sectors, but also broad coverage of critical supporting topics. Industrial processes and products can be much enhanced through observing the tenets and applying the methodologies found in chapters on Green Engineering and Chemistry (specifically, biomass conversion), Practical Catalysis, and Environmental Measurements; as well as expanded treatment of Safety, chemistry plant security, and Emergency Preparedness. Understanding these factors allows them to be part of the total process and helps achieve optimum results in, for example, process development, review, and modification. Important topics in the energy field, namely nuclear, coal, natural gas, and petroleum, are covered in individual chapters. Other new chapters include energy conversion, energy storage, emerging nanoscience and technology. Updated sections include more material on biomass conversion, as well as three chapters covering biotechnology topics, namely, Industrial Biotechnology, Industrial Enzymes, and Industrial Production of Therapeutic Proteins.
    Pages: Online-Ressource (XIV, 1562 pages)
    ISBN: 9780387278438
    Language: English
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 44
    Electronic Resource
    Electronic Resource
    Springer
    Investigational new drugs 18 (2000), S. 373-381 
    ISSN: 1573-0646
    Keywords: clinical pharmacology ; dihydropyrimdine dehydrogenase ; eniluracil ; oral 5-FU ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacological inactivation of dihydropyrimidine dehydrogenase (DPD)represents one strategy to improve 5-FU therapy, which historically hasbeen associated with unpredictable pharmacological behavior andtoxicity. This is principally due to high interpatientdifferences in the activity of DPD, the enzyme that mediates theinitial and rate-limiting step in 5-FU catabolism. Byinactivating DPD and suppressing the catabolism of 5-FU,eniluracil has dramatically altered the pharmacological profileof 5-FU. The maximum tolerated dose of oral 5-FU given with oraleniluracil (1.0 to 25 mg/m2) is substantially lower thanconventional 5-FU doses. In the presence of eniluracil,bioavailability of 5-FU has increased to approximately 100%, thehalf-life is prolonged to 4 to 6 hours, and systemic clearanceis reduced 〉 20-fold to values comparable the glomerularfiltration rate (46 to 58 mL/min/m2). Renal excretion(∼ 45% to 75%), instead of DPD-related catabolism, is theprincipal route of elimination of oral 5-FU given witheniluracil. Chronic daily administration of oral 5-FU 1.0mg/m2 twice daily with eniluracil 20 mg twice dailyproduces 5-FU steady-state concentrations (8–38 ng/mL) similarto those achieved with protracted intravenous administration onclinically relevant dose-schedules. On a daily × 5regimen, higher 5-FU AUC values are related to neutropenia,whereas elevated 5-FU AUC and steady-state concentrations arerelated to diarrhea when oral 5-FU is given daily with eniluracilon a chronic schedule. The pharmacokinetic behavior of oraleniluracil is similar to that for oral 5-FU. Administration ofeniluracil 10 to 20 mg twice daily completely inactivates DPDactivity both in peripheral blood mononuclear cells and incolorectal tumor tissue, and prolonged inhibition of DPD afterdiscontinuation of eniluracil treatment has been noted. In thepresence of eniluracil, oral administration of 5-FU is feasibleand variation in 5-FU exposure is reduced, with the anticipationof further reduction in variation as dosing guidelines based onrenal function are formulated.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 45
    ISSN: 1573-904X
    Keywords: allometric scaling ; interspecies scaling ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To evaluate (1) allometric scaling of systemic clearance (CL)using unbound drug concentration, (2) the potential usage of brainweight (BRW) correction in allometric scaling of both CL and oralclearance (CL/F). Methods. Human clearance was predicted allometrically (CLu = a ·Wbiv) using unbound plasma concentration for eight Parke-Daviscompounds and 29 drugs from literature sources. When the exponent bivwas higher than 0.85, BRW was incorporated into the allometricrelationship (CLu*BRW = a · Wbiv). This approach was also applied tothe prediction of CLu/F for 10 Parke-Davis compounds. Human oralt1/2, Cmax, AUC, and bioavailability were estimated based onallometrically predicted pharmacokinetic (PK) parameters. Results. Human CL and CL/F were more accurately estimated usingunbound drug concentration and the prediction was further improvedwhen BRW was incorporated into the allometric relationship. ForParke-Davis compounds, the predicted human CL and CL/F werewithin 50-200% and 50-220% of the actual values, respectively. Theestimated human oral t1/2, Cmax, and AUC were within 82-220%,56-240%, and 73-190% of the actual values for all 7 compounds,suggesting that human oral PK parameters of those drugs could bereasonably predicted from animal data. Conclusions. Results from the retrospective analysis indicate thatallometric scaling of free concentration could be applied to orallyadministered drugs to gain knowledge of drug disposition in man, and to helpdecision-making at early stages of drug development.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 46
    ISSN: 1573-904X
    Keywords: pharmacokinetics ; recombinant human interleukin-11 ; absorption ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 47
    ISSN: 1573-904X
    Keywords: (R,S)-Ifosfamide ; R2-, R3-, S2-, S3-DCE-IFF ; iterative-two stage analysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To describe the pharmacokinetics of R- andS-Ifosfamide (IFF), and their respective 2 and 3 N-dechloroethylated (DCE)metabolites (R2-, R3-, S2, S3-DCE-IFF) in cancer patients. Methods. (R,S)-IFF was administered (1.5 g/m2)daily for 5 days in 13 cancer patients. Plasma and urine samples were collectedand analyzed using an enantioselective GC-MS method. An average of 97observations per patient were simultaneously fitted using apharmacokinetic-metabolism (PK-MB) model. A population PK analysis was performedusing an iterative 2-stage method (IT2S). Results. Auto-induction of IFF metabolism was observed over the 5day period. Increases were seen in IFF clearance (R: 4 vs 7 L/h; S: 5vs 10 L/h), and in the formation of DCE (R: 7 vs 9%; S: 14 vs 19%)and active metabolites (4-OHM-IFF; R: 71 vs 77%; S: 67 vs 71%). Anovel finding of this analysis was that the renal excretion of the DCEmetabolites was also induced. Conclusions. This population PK-MB model for (R,S)-IFF may beuseful in the optimization of patient care, and gives new insight intothe metabolism of (R,S)-IFF.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 48
    ISSN: 1573-904X
    Keywords: stealth and remote loading proliposome ; doxorubicin ; pharmacokinetics ; acute toxicity ; anticancer effect
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The aim of the study was to prepare stealth and remoteloading proliposome (SRP-L) to carry doxorubicin (DXR) and evaluatethe pharmacokinetics, acute toxicity, and anticancer effect of DXRcarried with SRP-L. Methods. SRP-L was transparent solution. When SRP-L was injectedinto 0.9% NaCl aqueous solution containing DXR, liposomes formedand automatically loaded DXR (SRP-L-DXR). The long circulation ofSRP-L-DXR was evaluated using the pharmacokinetics ofSRP-L-DXR, cardiolipin liposomal DXR (CL-DXR) and free DXR (F-DXR).The acute toxicity and anticancer effect of SRP-L-DXR were evaluatedin C57BL/6 mice and murine hystocytoma M5076 tumor model. Results. The average diameter of SRP-L-DXR in pure water was112.9 ± 8.6 (nm) and the encapsulation efficiency of SRP-L-DXRwas 96.5 ± 0.2% in pure water, 95.5 ± 0.1% in 5% glucose and 98.01± 0.6% in 0.9% NaCl. The plasma concentration of SRP-L-DXR wasmuch higher than those of F-DXR and CL-DXR. Compared with thatof F-DXR, the SRP-L-DXR had lower acute toxicity and its anticancereffects depended upon the therapeutic treatment. Conclusions. A novel proliposome (SRP-L) was developed, whichcould automatically load DXR and form SRP-L-DXR with excellentcharacteristics. SRP-L-DXR had lower acute toxicity but was notalways more effective for the treatment of the ascitic M5076 thanF-DXR.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 49
    ISSN: 1573-904X
    Keywords: morphine ; nociceptive effect ; electrical stimulation vocalisation method ; microdialysis ; retrodialysis by drug ; pharmacokinetics ; pharmacodynamics ; modelling ; blood-brain barrier transport
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To quantify the contribution of distributional processes across the blood-brain barrier (BBB) to the delay in antinociceptive effect of morphine in rats. Methods. Unbound morphine concentrations were monitored in venous blood and in brain extracellular fluid (ECF) using microdialysis (MD) and in arterial blood by regular sampling. Retrodialysis by drug was used for in vivo calibration of the MD probes. Morphine was infused (10 or 40 mg/kg) over 10 min intravenously. Nociception, measured by the electrical stimulation vocalisation method, and blood gas status were determined. Results. The half-life of unbound morphine in striatum was 44 min compared to 30 min in venous and arterial blood (p 〈 0.05). The BBB equilibration of morphine, expressed as the ratio of areas under the curve between striatum and venous blood, was less than unity (0.28 ± 0.09 and 0.22 ± 0.17 for 10 and 40 mg/kg), respectively, indicating active efflux of morphine across the BBB. The concentration-effect relationship exhibited a clear hysterisis with an effect delay half-life of 32 and 5 min based on arterial blood and brain ECF concentrations, respectively. Conclusions. Eighty five percent of the effect delay was caused by morphine transport across the BBB, indicating possible involvement of rate limiting mechanisms at the receptor level or distributional phenomena for the remaining effect delay of 5 min.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 50
    ISSN: 1573-904X
    Keywords: bioequivalence ; dose proportionality ; mixed effects model ; pharmacokinetics ; power model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The aim of this work was a pragmatic, statistically sound and clinically relevant approach to dose-proportionality analyses that is compatible with common study designs. Methods. Statistical estimation is used to derive a (1-α)% confidence interval (CI) for the ratio of dose-normalized, geometric mean values (Rdnm) of a pharmacokinetic variable (PK). An acceptance interval for Rdnm defining the clinically relevant, dose-proportional region is established a priori. Proportionality is declared if the CI for Rdnm is completely contained within the critical region. The approach is illustrated with mixed-effects models based on a power function of the form PK = β0 • Doseβ1; however, the logic holds for other functional forms. Results. It was observed that the dose-proportional region delineated by a power model depends only on the dose ratio. Furthermore, a dose ratio (ρ1) can be calculated such that the CI lies entirely within the pre-specified critical region. A larger ratio (ρ2) may exist such that the CI lies completely outside that region. The approach supports inferences about the PK response that are not constrained to the exact dose levels studied. Conclusion. The proposed method enhances the information from a clinical dose-proportionality study and helps to standardize decision rules.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 51
    ISSN: 1573-904X
    Keywords: SK&F 107647 ; peptide ; pharmacokinetics ; hematore gulatory ; adenocarcinoma ; cytokines
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To describe the pharmacokinetics of SK&F 107647, a synthetichematoregulatory peptide, in healthy volunteers and in patientswith adenocarcinoma.Methods. SK&F 107647 pharmacokinetics were evaluated in 2dose-escalation studies. Volunteers received SK&F 107647 as single15-minute iv infusion doses of 1, 10, 100, 500, and 1000 μg/kg. Cancerpatients received 2-hour iv infusions of 0.001, 0.01, 0.1 and 1μg/kg once daily for 10 days. Drug concentrations were quantified in plasmaand urine of healthy volunteers and on days 1 and 10 in plasma ofcancer patients receiving the two top dose levels.Results. In volunteers, mean clearance (CL) ranged from 76.7 to 101ml/hour/kg; mean volume of distribution at steady-state (Vss)rangedfrom 175 to 268 ml/kg. Most of the administered dose was renallyexcreted as intact peptide within 24 hours postinfusion. In patients,mean CL was 57.6 ml/hour/kg, mean Vss ranged from 128 to 150ml/kg and terminal half-life from 2.1 to 3.4 hours. There was littleaccumulation of drug. In both studies, linear pharmacokinetics wasobserved. Clearance approached normal glomerular filtration rate(GFR) in volunteers and correlated with creatinine clearance incancer patients.Conclusions. SK&F 107647 exhibits linear pharmacokinetics, a smallVss, and clearance, primarily renal, approaching normal GFR.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 52
    ISSN: 1573-904X
    Keywords: glycyrrhizic acid ; modeling ; enterohepatic cycling ; PBPK ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To analyze the role of the kinetics of glycyrrhizic acid (GD) in its toxicity. A physiologically-based pharmacokinetic (PBPK) model that has been developed for humans. Methods. The kinetics of GD, which is absorbed as glycyrrhetic acid (GA), were described by a human PBPK model, which is based on a rat model. After rat to human extrapolation, the model was validated on plasma concentration data after ingestion of GA and GD solutions or licorice confectionery, and an additional data derived from the literature. Observed interindividual variability in kinetics was quantified by deriving an optimal set of parameters for each individual. Results. The a-priori defined model successfully forecasted GA kinetics in humans, which is characterized by a second absorption peak in the terminal elimination phase. This peak is subscribed to enterohepatic cycling of GA metabolites. The optimized model explained most of the interindividual variance, observed in the clinical study, and adequately described data from the literature. Conclusions. Preclinical information on GD kinetics could be incorporated in the human PBPK model. Model simulations demonstrate that especially in subjects with prolonged gastrointestinal residence times, GA may accumulate after repeated licorice consumption, thus increasing the health risk of this specific subgroup of individuals.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 53
    ISSN: 1573-904X
    Keywords: luteinising hormone-releasing hormone (LH-RH) antagonist ; cetrorelix ; pharmacokinetics ; population PK/PD-modeling ; testosterone ; rat ; dog
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Population models for thepharmacokinetic-pharmacodynamic relationship for cetrorelix (CET), a luteinising hormone-releasinghormone (LH-RH) antagonist, and the pharmacodynamic response ontestosterone production were investigated in rats and dogs. Methods. The plasma concentrations of CET and testosterone weredetermined after intravenous and subcutaneous injections. Thepopulation PK/PD-models were developed using P-PHARM software. Results. Absolute bioavailability of cetrorelix was 100% in rats and97% in dogs. In rats, the pharmacokinetics was explained by atwo-compartment model with saturable absorption, while athree-compartment model was used in dogs. Testosterone suppression in both specieswas described by a sigmoid Emax model with maximum effect (Emax)considered as total hormonal suppression. The duration of testosteronesuppression in rats was longer at higher doses. The populationelimination half-lifes after iv-dose were 3.0 h in rats and 9.3 h in dogs.Population mean estimates of IC50 were 1.39 and 1.24 ng/ml in ratsand dogs, respectively. Conclusions. A population pharmacokinetic model was developed toexplain the dissolution rate limited absorption from the injection site.The suppression of testosterone could be described by an indirectinhibitory sigmoid Emax model. In both species 1-2 ng/ml CET inplasma was necessary to suppress testosterone production.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 54
    ISSN: 1573-904X
    Keywords: methylphenidate ; average bioequivalence ; individual bioequivalence ; human ; pharmacokinetics ; replicated design
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To determine the relative bioavailability of two marketed,immediate-release methylphenidate tablets. The study used a replicatedstudy design to characterize intrasubject variability, and determinebioequivalence using both average and individual bioequivalencecriteria. Methods. A replicated crossover design was employed using 20subjects. Each subject received a single 20 mg dose of the reference tableton two occasions and two doses of the test tablet on two occasions.Blood samples were obtained for 10 hr after dosing, and plasma wasassayed for methylphenidate by GC/MS. Results. The test product was more rapidly dissolved in vitro and morerapidly absorbed in vivo than the reference product. The mean Cmaxand AUC(0 − ∞) differed by 11% and 9%, respectively. Using anaverage bioequivalence criterion, the 90% confidence limits for theLn-transformed Cmax and AUC(0 − ∞), comparing the two replicatesof the test to the reference product, fell within the acceptable range of80–125%. Using an individual bioequivalence criterion the test productfailed to demonstrate equivalence in Cmax to the reference product. Conclusions. The test and reference tablets were bioequivalent usingan average bioequivalence criterion. The intrasubject variability of thegeneric product was greater and the subject-by-formulation interactionvariance was borderline high. For these reasons, the test tablets werenot individually bioequivalent to the reference tablets.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 55
    ISSN: 1573-904X
    Keywords: 1,4-dihydropyridine calcium channel antagonist ; (+)-[3H]PN 200-110 ; senescence-accelerated prone mouse ; brain concentration ; pharmacokinetics ; in vivo receptor binding
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To characterize the in vivo specific binding andpharmacokinetics of a 1,4-dihydropyridine (DHP) calcium channel antagonist, PN200-110, in the senescent brain, using senescence-accelerated pronemice (SAMP8) and senescence-resistant mice (SAMR1). Methods. Blood, brain, and heart samples were taken periodically fromSAMR1 and SAMP8 following intravenous injection of (+)-[3H]PN200-110, and the concentration of (+)-[3H]PN 200-110 in the plasmaand tissues was determined. In addition, the in vivo specific bindingof (+)-[3H]PN 200-110 in the brains of SAMR1 and SAMP8 wasmeasured periodically after intravenous injection of the radioligand. Results. There was very little significant difference between SAMR1and SAMP8 in terms of the half-life (t1/2), total body clearance (CLtot),steady-state volume of distribution (Vdss), and AUC for the plasmaconcentration of (+)-[3H]PN 200-110 after intravenous injection ofthe radioligand. The brain concentration (AUCbrain) for (+)-[3H]PN200-110 and the brain/plasma AUC ratio (AUCbrain/AUCplasma) weresignificantly lower in SAMP8 than in SAMR1, and the heartconcentration (AUCheart) and the heart/plasma AUC ratio (AUCheart/AUCplasma)were similar in both strains. Also, the brain/plasma unbound AUCratio (AUCbrain/AUCplasma-free) for (+)-[3H]PN 200-110 wassignificantly lower in SAMP8 than in SAMR1. The in vivo specific binding(AUCspecific binding, maximal number of binding sites: Bmax) of(+)-[3H]PN 200-110 was significantly lower in brain particulate fractionsof SAMP8 than SAMR1. Conclusions. The concentration and in vivo specific binding of(+)-[3H]PN 200-110 was significantly reduced in the senescent brain. Thesimultaneous analysis of the concentrations of centrally acting drugsand the in vivo specific binding in the brain in relation to theirpharmacokinetics may be valuable in evaluating their CNS effects.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 56
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 17 (2000), S. 903-905 
    ISSN: 1573-904X
    Keywords: P-glycoprotein ; hepatic metabolism ; pharmacokinetics ; first-pass metabolism ; drug interaction
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 57
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 17 (2000), S. 127-134 
    ISSN: 1573-904X
    Keywords: in-situ head perfusion ; pharmacokinetics ; red blood cells ; water
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To develop a viable, single pass rat head perfusion modeluseful for pharmacokinetic studies. Methods. A viable rat head preparation, perfused with MOPS-bufferedRinger's solution, was developed. Radiolabelled markers (red bloodcells, water and sucrose) were injected in a bolus into the internalcarotid artery and collected from the posterior facial vein over 28minutes. The double inverse Gaussian function was used to estimatethe statistical moments of the markers. Results. The viability of the perfusion was up to one hour, with optimalperfusate being 2% bovine serum albumin at 37°C, pH 7.4. Thedistribution volumes for red blood cells, sucrose and water (from all studies,n = 18) were 1.0 ± 0.3ml, 6.4 ± 4.2ml and 18.3 ± 11.9ml, respectively.A high normalised variance for red blood cells (3.1 ± 2.0) suggestsa marked vascular heterogeneity. A higher normalised variance forwater (6.4 ± 3.3) is consistent with additional diffusive/permeabilitylimitations. Conclusions. Analysis of the physiological parameters derived fromthe moments suggested that the kinetics of the markers were consistentwith distribution throughout the head (weight 25g) rather than justthe brain (weight 2g). This model should assist in studying solutepharmacokinetics in the head.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 58
    ISSN: 1573-904X
    Keywords: α1-acid glycoprotein ; protein binding ; dissociation rate ; species difference ; physiological model ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The extremely low clearance and small distribution volumeof UCN-01 in humans could be partly due to the high degree of bindingto hAGP (1,2). The quantitative effects of hAGP on the pharmacokineticsof UCN-01 at several levels of hAGP and UCN-01 were estimatedin rats given an infusion of hAGP to mimic the clinical situation anda physiological model for analysis was developed. Methods. The plasma concentrations of UCN-01 (72.5–7250 nmol/kgiv) in rats given an infusion of hAGP, 15 or 150 nmol/h/kg, weremeasured by HPLC. Pharmacokinetic analysis under conditionsassuming rapid equilibrium of protein binding and incorporating thedissociation rate was conducted. Results. The Vdss and CLtot of UCN-01 (725 nmol/kg iv) in ratsgiven an infusion of hAGP, 150 nmol/h/kg, fell to about 1/250 and 1/700that in control rats. The Vdss and CLtot following 72.5–7250nmol/kg UCN-01 to rats given 150 nmol/h/kg hAGP were 63.9–688ml/kg and 3.18–32.9 ml/h/kg, respectively, indicating non-linearitydue to saturation of UCN-01 binding. The CLtot estimated by thephysiological model assuming rapid equilibrium of UCN-01 bindingto hAGP, was six times higher than the observed value while the CLtotestimated by the model incorporating koff, measured using DCC, wascomparable with the observed value. Conclusions. These results suggest that the slow dissociation ofUCN-01 from hAGP limits its disposition and elimination.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 59
    ISSN: 1573-904X
    Keywords: IVIVC ; racemate ; enantiomers ; metoprolol ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To investigate the ability of an IVIVC developedwith a racemate drug as well as each enantiomer in predicting the invivo enantiomer drug performance. Methods. Dissolution of metoprolol extended releasetablets with different release characteristics (e.g., fast (F),moderate (M), and slow (S)) was performed using USP ApparatusI, pH 1.2, 50 rpm. Metoprolol racemate tablets (S, M, and F, 100 mg) and 50mg oral solution were administered to healthy volunteers, blood samples werecollected over 24 (solution) and 48 (tablet) hours and assayed. IVIVC modelsdeveloped were: (1) Racemate-fraction of drug dissolved (FRD) vsRacemate-fraction of drug absorbed (FRA), (2) R-FRD vs R-FRA, and (3) S-FRDvs S-FRA for combinations of formulations (S/M/F, S/M, S/F, and M/F).Enantiomer Cmax and AUC prediction errors (PEs) were estimated for modelevaluation after convolution of in vivo release rates. Results. The R-IVIVC and S-IVIVC accurately predicted theR- and S-metoprolol pharmacokinetic profiles, respectively. The averagedprediciton errors (PE) for the enantiomer Cmax and AUC were less than10% for S/M/F, M/F, and S/F IVIVC models. Racemate-IVIVC (M/F) wasable to predict S-enantiomer with an average %PE of 2.52 for S-Cmaxand 4.3 for S-AUC. However, the racemate-IVIVC was unable to predict theR-enantiomer pharmacokinetic profile. Conclusions. Metoprolol racemate data cannot be used toaccurately predict R-enantiomer drug concentrations. However, the racematedata was predictive of the active stereoisomer.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 60
    Electronic Resource
    Electronic Resource
    Springer
    Fish physiology and biochemistry 23 (2000), S. 225-232 
    ISSN: 1573-5168
    Keywords: methylisoborneol ; catfish ; cytochrome P450 ; biotransformation ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract 2-Methylisoborneol (MIB) and structurally related terpenoid compounds are responsible for millions of dollars of lost revenue to catfish farmers. In an attempt to determine enzymatic pathways of biotransformation and elimination of MIB, the in vitro metabolism of MIB was examined in the Ulvade strain of channel catfish (Ictalurus punctatus). Although cytochrome P450 (CYP) activities were observed and correlated with expression of specific isoforms (i.e. steroid hydroxylation and CYP3A expression), no metabolites of MIB were observed. To determine whether extrahepatic biotransformation may be occurring the in vivo metabolism and disposition of 14C-MIB was examined in Uvalde, USDA-103 channel catfish, and a channel catfish X blue catfish (Ictalurus furcatus) hybrid species. Confirming in vitro hepatic studies, no metabolites were observed in plasma from animals treated with an intra-arterial dose of 14C-MIB. 14C-MIB elimination was predicted using a two compartment model in each strain of fish. There was no significant difference in terminal half-lives between strains but possible differences in total body clearance and apparent volumes of distribution which may be related to higher lipid content in the hybrids. Results of these studies indicate biotransformation has no involvement in MIB elimination and that other physiological processes may play a more significant role in MIB disposition within Ictalurid fish species.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 61
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 17 (2000), S. 1426-1431 
    ISSN: 1573-904X
    Keywords: eplerenone ; selective aldosterone receptor antagonist ; dog ; pharmacokinetics ; absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The present study was conducted to characterize the pharmacokinetics of eplerenone (EP), a selective aldosterone receptor antagonist, and its open lactone ring form in the dog. Methods. Pharmacokinetic studies of EP were conducted in dogs following i.v., oral, and rectal dosing (15 mg/kg) and following intragastric, intraduodenal, intrajejunal, and intracolonic dosing (7.5 mg/kg). Results. After oral administration, the systemic availability of EP was 79.2%. Systemic availabilities following administration via other routes were similar to that following oral administration. The half-life and plasma clearance of EP were 2.21 hr and 0.329 l/kg/hr, respectively. Plasma concentrations of the open lactone ring form were lower than EP concentrations regardless of the route of administration. The C-14 AUC in red blood cells was approximately 64% and 68% of the plasma AUC for i.v. and oral doses. Percentages of the dose excreted as total radioactivity in urine and feces were 54.2% and 40.6%, respectively, after i.v. administration, and 40.7% and 52.3%, respectively, after oral administration. The percentages of the dose excreted in urine and feces as EP were 13.7% and 2.5%, respectively, after i.v. administration, and 2.1% and 4.6% after oral administration, respectively. Approximately 11% and 15% of the doses were excreted as the open form following i.v. and oral doses. Conclusions. EP was rapidly and efficiently absorbed throughout the gastrointestinal tract, resulting in a good systemic availability. The drug did not preferentially accumulate in red blood cells. EP was extensively metabolized; however, first-pass metabolism after oral and rectal administration was minimal. EP and its metabolites appear to be highly excreted in the bile.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 62
    ISSN: 1573-904X
    Keywords: amphotericin B ; liposomes ; pharmacokinetics ; toxicokinetics ; tissue distribution ; toxicity
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Amphotericin B in small, unilamellar liposomes (AmBisome) is safer and produces higher plasma concentrations than other formulations. Because liposomes may increase and prolong tissue exposures, the potential for drug accumulation or delayed toxicity after chronic AmBisome was investigated. Methods. Rats (174/sex) received intravenous AmBisome (1, 4, or 12 mg/kg), dextrose, or empty liposomes for 91 days with a 30-day recovery. Safety (including clinical and microscopic pathology) and toxicokinetics in plasma and tissues were evaluated. Results. Chemical and histopathologic changes demonstrated that the kidneys and liver were the target organs for chronic AmBisome toxicity. Nephrotoxicity was moderate (urean nitrogen [BUN] ≤51 mg/dl; creatinine unchanged). Liposome-related changes (vacuolated macrophages and hypercholesterolemia) were also observed. Although plasma and tissue accumulation was nonlinear and progressive (clearance and volume decreased, half-life increased with dose and time), most toxic changes occurred early, stabilized by the end of dosing, and reversed during recovery. There were no delayed toxicities. Concentrations in liver and spleen greatly exceeded those in plasma; kidney and lung concentrations were similar to those in plasma. Elimination half-lives were 1-4 weeks in all tissues. Conclusions. Despite nonlinear accumulation, AmBisome revealed predictable hepatic and renal toxicities after 91 days, with no new or delayed effects after prolonged treatment at high doses that resulted in plasma levels 〉200 μg/ml and tissue levels 〉3000 μg/g.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 63
    ISSN: 1573-904X
    Keywords: aspergillosis ; pharmacokinetics ; amphotericin B ; biodistribution ; liposomes ; cholesterol hemisuccinate
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. This study compared the biodistribution of two amphotericin B formulations in normal and Aspergillus infected mice. Amphotericin B cholesterol hemisuccinate vesicles (ABCV) which reduces the toxicity of amphotericin B and thereby enhances its therapeutic efficacy in a murine model of aspergillosis was compared with conventional amphotericin B deoxycholate suspension (AmBDOC). Methods. ABCV (12 mg/kg wt) and AmBDOC (2 mg/kg wt) were intravenously administered to normal and A.fumigatus infected mice. The concentration of amphotericin B in plasma and other organs was determined at different time points. Results. It was observed that ABCV had a significantly different pharmacokinetic profile compared to conventional amphotericin B. In comparison to AmBDOC significantly lower levels of amphotericin B were observed in kidneys and plasma, the major target organs of toxicity. Animals receiving ABCV demonstrated high levels of amphotericin B in liver (38% retention till 48 h) and spleen (2.6% retention till 48 h) in comparison to AmBDOC (7.3% and 0.21% retention in liver and spleen respectively till 48 h). Biodistribution studies of ABCV in infected mice demonstrated that there was a moderate enhancement in levels of amphotericin B in liver, spleen, lungs and kidneys as compared to normal mice and the plasma levels were reduced. However, such observations were not made after AmBDOC administration to infected mice except for kidneys in which there was a marked increase in uptake as compared to normal mice. Conclusions. Our results suggest that prolonged retention of high concentrations of ABCV in reticuloendothelial system organs is the reason for its reduced toxicity. Enhanced localization of the drug at the infected site may lead to improvement in therapeutic efficacy.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 64
    ISSN: 1573-904X
    Keywords: oral absorption ; humans ; dogs ; rats ; interspecies scale-up ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To conduct a retrospective evaluation of using dog as ananimal model to study the fraction of oral dose absorbed (F) of 43drugs in humans and to briefly discuss potential factors that mighthave contributed to the observed differences in absorption. Methods. Mean human and dog absorption data obtained under fastedstate of 43 drugs with markedly different physicochemical andpharmacological properties and with mean F values ranging from 0.015 to1.0 were obtained from the literature. Correlation of F values betweenhumans and dogs was studied. Based on the same references, additionalF data for humans and rats were also obtained for 18 drugs. Results. Among the 43 drugs studied, 22 drugs were virtuallycompletely absorbed in both dogs and humans. However, the overallcorrelation was relatively poor (r2 = 0.5123) as compared to the earlier ratvs. human study on 64 drugs (r2 = 0.975). Several drugs showed muchbetter absorption in dogs than in humans. Marked differences in thenonliner absorption profiles between the two species were found forsome drugs. Also, some drugs had much longer Tmax values andprolonged absorption in humans than in dogs that might be theoreticallypredicted. Data on 18 drugs further support great similarity in F betweenhumans and rats reported earlier from our laboratory. Conclusions. Although dog has been commonly employed as ananimal model for studying oral absorption in drug discovery anddevelopment, the present study suggests that one may need to exercise cautionin the interpretation of data obtained. Exact reasons for the observedinterspecies differences in oral absorption remain to be explored.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 65
    ISSN: 1573-904X
    Keywords: benzodiazepines ; pharmacokinetics ; EEG ; operational model of agonism ; receptor binding ; muscimol-induced Cl−uptake
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. A mechanism-based model is applied to analyse adaptivechanges in the pharmacodynamics of benzodiazepines upon chronictreatment in rats. Methods. The pharmacodynamics of midazolam was studied in ratswhich received a constant rate infusion of the drug for 14 days, resultingin a steady-state concentration of 102 ± 8 ng·ml−1. Vehicle treated ratswere used as controls. Concentration-EEG effect data were analysed onbasis of the operational model of agonism. The results were comparedto data obtained in vitro in a brain synaptoneurosomal preparation. Results. The relationship between midazolam concentration and EEGeffect was non-linear. In midazolam pre-treated rats the maximum EEGeffect was reduced by 51 ± 23 μV from the original value of 109 ±15 μV in vehicle treated group. Analysis of this change on basis ofthe operational model of agonism showed that it can be explained bya change in the parameter tissue maximum (Em) rather than efficacy(τ). In the in vitro studies no changes in density, affinity or functionalityof the benzodiazepine receptor were observed. Conclusions. It is concluded that the observed changes in theconcentration-EEG effect relationship of midazolam upon chronic treatmentare unrelated to changes in benzodiazepine receptor function.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 66
    ISSN: 1573-8221
    Keywords: acylprolyldipeptide ; GVS-111 ; pharmacokinetics ; blood-brain barrier permeability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Pharmacokinetics of GVS-111, a new acylprolyldipeptide with nootropic properties and its penetration across the blood-brain barrier were studied in rats using HPLC. It was found that the dipeptide is absorbed in the gastrointestinal tract, enters the circulation, and penetrates through the blood-brain barrier in an umodified state.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 67
    Electronic Resource
    Electronic Resource
    Springer
    Risk analysis 19 (1999), S. 711-726 
    ISSN: 1539-6924
    Keywords: variability ; exposure ; susceptibility ; risk assessment ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Energy, Environment Protection, Nuclear Power Engineering
    Notes: Abstract This paper reviews existing data on the variability in parameters relevant for health risk analyses. We cover both exposure-related parameters and parameters related to individual susceptibility to toxicity. The toxicity/susceptibility data base under construction is part of a longer term research effort to lay the groundwork for quantitative distributional analyses of non-cancer toxic risks. These data are broken down into a variety of parameter types that encompass different portions of the pathway from external exposure to the production of biological responses. The discrete steps in this pathway, as we now conceive them, are: •Contact Rate (Breathing rates per body weight; fish consumption per body weight) •Uptake or Absorption as a Fraction of Intake or Contact Rate •General Systemic Availability Net of First Pass Elimination and Dilution via Distribution Volume (e.g., initial blood concentration per mg/kg of uptake) •Systemic Elimination (half life or clearance) •Active Site Concentration per Systemic Blood or Plasma Concentration •Physiological Parameter Change per Active Site Concentration (expressed as the dose required to make a given percentage change in different people, or the dose required to achieve some proportion of an individual's maximum response to the drug or toxicant) •Functional Reserve Capacity–Change in Baseline Physiological Parameter Needed to Produce a Biological Response or Pass a Criterion of Abnormal Function Comparison of the amounts of variability observed for the different parameter types suggests that appreciable variability is associated with the final step in the process–differences among people in “functional reserve capacity.” This has the implication that relevant information for estimating effective toxic susceptibility distributions may be gleaned by direct studies of the population distributions of key physiological parameters in people that are not exposed to the environmental and occupational toxicants that are thought to perturb those parameters. This is illustrated with some recent observations of the population distributions of Low Density Lipoprotein Cholesterol from the second and third National Health and Nutrition Examination Surveys.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 68
    ISSN: 1539-6924
    Keywords: MeHg ; pharmacokinetics ; PBPK model ; variability ; risk assessment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Energy, Environment Protection, Nuclear Power Engineering
    Notes: Abstract An analysis of the uncertainty in guidelines for the ingestion of methylmercury (MeHg) due to human pharmacokinetic variability was conducted using a physiologically based pharmacokinetic (PBPK) model that describes MeHg kinetics in the pregnant human and fetus. Two alternative derivations of an ingestion guideline for MeHg were considered: the U.S. Environmental Protection Agency reference dose (RfD) of 0.1 μg/kg/day derived from studies of an Iraqi grain poisoning episode, and the Agency for Toxic Substances and Disease Registry chronic oral minimal risk level (MRL) of 0.5 μg/kg/day based on studies of a fish-eating population in the Seychelles Islands. Calculation of an ingestion guideline for MeHg from either of these epidemiological studies requires calculation of a dose conversion factor (DCF) relating a hair mercury concentration to a chronic MeHg ingestion rate. To evaluate the uncertainty in this DCF across the population of U.S. women of child-bearing age, Monte Carlo analyses were performed in which distributions for each of the parameters in the PBPK model were randomly sampled 1000 times. The 1st and 5th percentiles of the resulting distribution of DCFs were a factor of 1.8 and 1.5 below the median, respectively. This estimate of variability is consistent with, but somewhat less than, previous analyses performed with empirical, one-compartment pharmacokinetic models. The use of a consistent factor in both guidelines of 1.5 for pharmacokinetic variability in the DCF, and keeping all other aspects of the derivations unchanged, would result in an RfD of 0.2 μg/kg/day and an MRL of 0.3 μg/kg/day.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 69
    ISSN: 1573-0646
    Keywords: pharmacokinetics ; capecitabine ; 5-fluorouracil ; phase I trials
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract An excretion balance and pharmacokinetic study was conducted in cancer patients with solid tumors who received a single oral dose of capecitabine of 2000 mg including 50 μ Ci of 14C-radiolabelled capecitabine. Blood, urine and fecal samples were collected until radioactive counts had fallen to below 50 dpm/mL in urine, and levels of intact drug and its metabolites were measured in plasma and urine by LC/MS-MS (mass spectrometry) and 19F-NMR (nuclear magnetic resonance) respectively. Based on the results of the 6 eligible patients enrolled, the dose was almost completely recovered in the urine (mean 95.5%, range 86–104% based on radioactivity measurements) over a period of 7 days after drug administration. Of this, 84% (range 71–95) was recovered in the first 12 hours. Over this time period, 2.64% (0.69–7.0) was collected in the feces. Over a collection period of 24–48h, a total of 84.2% (range 80–95) was recovered in the urine as the sum of the parent drug and measured metabolites (5′-DFCR, 5′-DFUR, 5-FU, FUH2, FUPA, FBAL). Based on the radioactivity measurements of drug-related material, absorption is rapid (tmax 0.25–1.5 hours) followed by a rapid biphasic decline. The parent drug is rapidly converted to 5-FU, which is present in low levels due to the rapid metabolism to FBAL, which has the longest half-life. There is a good correlation between the levels of radioactivity in the plasma and the levels of intact drug and the metabolites, suggesting that these represent the most abundant metabolites of capecitabine. The absorption of capecitabine is rapid and almost complete. The excretion of the intact drug and its metabolites is rapid and almost exclusively in the urine.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 70
    ISSN: 1573-0646
    Keywords: docetaxel ; plasma assay ; clinical trials ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract We have developed a specific and sensitive method aiming atdocetaxel (Taxotere®) determination in plasma of treatedpatients. This involved solid-phase extraction of 1 ml of plasmaonto carboxylic acid (CBA) grafted silica cartridges followed byreversed-phase liquid chromatography with UV detection. The bestselectivity was obtained through the use of C18 Uptisphere® asstationary phase. The low limit of quantitation obtained (LOQ:5 ng/ml) allowed measurements of docetaxel up to 24 hours afterone-hour infusions with low dosages of drug (60 mg/m2). Themethod was applied successfully to monitor docetaxel plasma levelswithin two protocols associating fixed dosages of either methotrexate or gemcitabine with escalating doses of Taxotere®.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 71
    ISSN: 1573-8744
    Keywords: pharmacokinetics ; pharmacodynamics ; effect compartment model ; indirect response ; sigmoid E max ; tiagabine ; GABA uptake inhibitor
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Pharmacological inhibition of GABA uptake transporters provides a mechanism for increasing GABAergic transmission, which may be useful in the treatment of various neurological disorders. The purpose of our investigations was to develop an integrated pharmacokinetic–pharmacodynamic (PK/PD) model for the characterization of the pharmacological effect of tiagabine, R-N-(4,4-di-(3-methylthien-2-yl)but-3-enyl)nipecotic acid, in individual rats in vivo. The tiagabine-induced increase in the amplitude of the EEG 11.5–30 Hz frequency band (β), was used as pharmacodynamic endpoint. Chronically instrumented male Wistar rats were randomly allocated to four groups which received an infusion of 3, 10, or 30 mg kg −1 $$(\bar x \pm SE,{\text{ }}n = 23)$$ $$96 \pm 9$$ ml min -1 kg−1, 1.5ŷ0.1 L kg−1 and 20ŷ0.2 min.A time delay was observed between the occurrence of maximum plasma drug concentrations and maximal response. A physiological PK/PD model has been used to account for this time delay, in which a biophase was postulated to account for tiagabine available to the GABA uptake carriers in the synaptic cleft and the increase in EEG effect was considered an indirect response due to inhibition of GABA uptake carriers. The population values for the pharmacodynamic parameters characterizing the delay in pharmacological response relative to plasma concentrations were keo=0.030 min −1 and kout=81 min−1, respectively. Because of the large difference in these values the PK/PD model was simplified to the effect compartment model. Population estimates $$(\bar x \pm SE)$$ were E0=155 ŷ 6 μV, Emax=100 ŷ 5 μV, EC50=287 ŷ 7 ng ml−1, Hill factor=1.8 ŷ 0.2 and keo=0.030 ŷ 0.002 min −1. The results of this analysis show that for tiagabine the combined “effect compartment-indirect response” model can be simplified to the classical “effect compartment” model.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 72
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 27 (1999), S. 491-512 
    ISSN: 1573-8744
    Keywords: muscle relaxants ; peripheral elimination ; pharmacokinetics ; peripheral concentrations ; volume of distribution ; pharmacokinetic model
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract For anesthetic drugs undergoing nonorgan-based elimination, there is a definite trend towards using pharmacokinetic (PK) models in which elimination can occur from both central (k10 ) and peripheral compartments(k20 ). As the latter cannot be assessed directly, assumptions have to be made regarding its value. The primary purpose of this paper is to evaluate the impact of assuming various degrees of peripheral elimination on the estimation of PK parameters. For doing so, an explanatory model is presented where previously published data from our laboratory on three muscle relaxants, i.e., atracurium, doxacurium, and mivacurium, are used for simulations. The mathematical aspects for this explanatory model as well as for two specific applications are detailed. Our simulations show that muscle relaxants having a short elimination half-life are more affected by the presence of peripheral elimination as their distribution phase occupies the major proportion of their total area under the curve. Changes in the exit site dependent PK parameters (Vdss ) are also mostly significant when k20 is smaller than k10 . Although the physiological processes that determine drug distribution and those affecting peripheral elimination are independent, the two are mathematically tied together in the two-compartment model with both central and peripheral elimination. It follows that, as greater importance is given to k20 , the rate of transfer from the central compartment (k12 ) increases. However, as a result of a proportional increase in the volume of the peripheral compartment, peripheral concentrations remain unchanged whether or not peripheral elimination is assumed. These findings point out the limitations of compartmental analysis when peripheral elimination cannot be measured directly.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 73
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 27 (1999), S. 325-328 
    ISSN: 1573-8744
    Keywords: anesthetic techniques ; continuous infusion ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract We have previously described a method of rapidly obtaining a specified steady-state plasma concentration of an intravenous drug within precise limits. However the method is limited to drugs whose disposition may be characterized by an open two-compartment system. In this paper, we illustrate how the method can be extended to drugs whose disposition may be characterized by a mammillary model with any number of compartments. Refinements of our previous technique are also described.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 74
    ISSN: 1573-8744
    Keywords: psoriasis ; hu1124 ; CD11a ; CD3-positive lymphocytes ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics of hu1124, a human anti-CD11a antibody, were investigated in human subjects with psoriasis. CD11a is a subunit of LFA-1, a cell surface molecule involved in T cell mediated immune responses. Subjects received a single dose of 0.03, 0.1, 0.3, 0.6, 1, 2, 3, or 10 mg/kg of hu1124 intravenously over 1–3 hr. Blood samples were collected at selected times from 60 min to 72 days after administration. Plasma samples were assayed for hu1124 by ELISA, and pharmacokinetic analyses were performed on the drug plasma concentrations. As the dose of hu1124 was increased, the clearance decreased from 322 ml/day per kg at 0.1 mg/kg to 6.6 ml/day per kg at 10 mg/kg of hu1124. The plasma hu1124 concentration–time profile suggested that the clearance of hu1124 was saturable above 10 μg/ml. In addition, treatment with hu1124 caused a rapid reduction in the level of CD11a expression on CD3-positive lymphocytes (T cells) to about 25% of pretreatment levels. Regardless of the hu1124 dose administered, cell surface CD11a remained at this reduced level as long as hu1124 was detectable (〉0.025 μg/ml) in the plasma. When hu1124 levels fell below 3 μg/ml, the drug was rapidly cleared from the circulation and expression of CD11a returned to normal within 7–10 days thereafter. In vitro, half-maximal binding of hu1124 to lymphocytes was achieved at about 0.1 μg/ml and saturation required more than 10 μg/ml. One of the receptor-mediated pharmacokinetic/pharmacodynamic models which was developed describes the dynamic interaction of hu1124 binding to CD11a, resulting in the removal of hu1124 from the circulation and reduction of cell surface CD11a. The model accounts for the continually changing number of CD11a molecules available for removing hu1124 from the circulation based on prior exposure of cells expressing CD11a to hu1124. In addition, the model also accounts for saturation of CD11a molecules by hu1124 at drug concentrations of approximately 10 μg/ml, thereby reducing the clearance rate of hu1124 with increasing dose.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 75
    ISSN: 1573-8744
    Keywords: drug–drug interactions ; NPML ; experimental design ; pharmacodynamic variability ; pharmacokinetics ; entropy ; covariate ; second stage model ; controlled trial
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Population approaches are appealing methods for detecting then assessing drug–drug interactions mainly because they can cope with sparse data and quantify the interindividual pharmacokinetic (PK) and pharmacodynamic (PD) variability. Unfortunately these methods sometime fail to detect interactions expected on biochemical and/or pharmacological basis and the reasons of these false negatives are somewhat unclear. The aim of this paper is firstly to propose a strategy to detect and assess PD drug–drug interactions when performing the analysis with a nonparametric population approach, then to evaluate the influence of some design variates (i.e., number of subjects, individual measurements) and of the PD interindividual variability level on the performances of the suggested strategy. Two interacting drugs A and B are considered, the drug B being supposed to exhibit by itself a pharmacological action of no interest in this work but increasing the A effect. Concentrations of A and B after concomitant administration are simulated as well as the effect under various combinations of design variates and PD variability levels in the context of a controlled trial. Replications of simulated data are then analyzed by the NPML method, the concentration of the drug B being included as a covariate. In a first step, no model relating the latter to each PD parameter is specified and the NPML results are then proceeded graphically, and also by examining the expected reductions of variance and entropy of the estimated PD parameter distribution provided by the covariate. In a further step, a simple second stage model suggested by the graphic approach is introduced, the fixed effect and its associated variance are estimated and a statistical test is then performed to compare this fixed effect to a given value. The performances of our strategy are also compared to those of a non-population-based approach method commonly used for detecting interactions. Our results illustrate the relevance of our strategy in a case where the concentration of one of the two drugs can be included as a covariate and show that an existing interaction can be detected more often than with a usual approach. The prominent role of the interindividual PD variability level and of the two controlled factors is also shown.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 76
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 27 (1999), S. 329-338 
    ISSN: 1573-8744
    Keywords: propofol ; anaesthesia ; pharmacokinetics ; compartment models ; effect compartment models
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Conventional compartmental pharmacokinetic analysis may provide inaccurate prediction of drug concentrations after rapid iv administration. To examine this, compartment and effect compartment analysis was applied to measured arterial and brain concentrations of propofol in sheep after iv administration at a range of doses and dose rates. Although arterial and brain concentrations were reasonably well fitted to compartmental and effect compartment models for individual doses and dose rates, the structure and parameters of all models differed with changes in both dose and rate of administration. There were large discrepancies between predicted and measured arterial and brain concentrations when these models were used to predict drug concentrations across doses and dose rates. These data support the limitations of this type of modeling in the setting of rapid propofol administration.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 77
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 27 (1999), S. 513-529 
    ISSN: 1573-8744
    Keywords: desmopressin ; indirect-response modeling ; overhydration ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The objective of the present study was to investigate the pharmacokinetics (PK) and pharmacodynamics (PD) of desmopressin in healthy male subjects at different levels of overhydration. Also, we examined if an indirect-response model could be related to renal physiology and the pharmacological action of desmopressin. Eight healthy male subjects participated in this open, randomized crossover study with three periods. Each subject was orally water loaded (0 to 20ml·kg −1 body weight) on 3 study days in order to achieve three different levels of hydration. After the initial water load, urine was voided every 15 min and the volumes were measured. To ensure continuous overhydration the subjects replaced their fluid loss with drinking-water. When a steady-state diuresis was achieved after approximately 2 hr, 0.396 μg of desmopressin was administered intravenously as a bolus injection. Blood was sampled and urine was collected at intervals throughout the study day (10 hr). An indirect-response model, where desmopressin was assumed to inhibit the elimination of response, was fit to the urine osmolarity data. There were no statistically significant effects of different levels of hydration, as expressed by urine flow rate at baseline, on the estimates of the PK and PD model parameters. The calculated terminal half-lives of elimination (t1/2 β) ranged between 2.76 and 8.37 hr with an overall mean of 4.36 hr. The overall means of plasma clearance and the volumes of distribution of the central compartment (Vc ) and at steady state (Vss ) were estimated to be 1.34 (SD 0.35) ml·min −1 ·kg −1 , 151 (SD28) ml·kg −1 , and 386 (SD 63) ml·kg −1 , respectively. High urine flow rate, indicating overhydration, produced a diluted urine and thus a low osmolarity at baseline (R0 ). The effect of the urine flow rate on the urine osmolarity at baseline was highly significant (p〈0.0001). The mean values for IC50 and the sigmoidicity factor (γ) were 3.7 (SD 1.2) pg·ml −1 and 13.0 (SD 3.5), respectively. In most cases when there was a high urine flow rate at baseline, the model and the estimated PD parameters could be related to the pharmacological action of desmopressin and renal physiology. Thus, the indirect-response model used in this study offers a mechanistic approach of modeling the effect of desmopressin in overhydrated subjects.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 78
    ISSN: 1573-8744
    Keywords: prediction interval ; pharmacokinetics ; population analysis ; NONMEM ; inverse regression ; immunosuppressives
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Basiliximab is an immunosuppressant chimeric monoclonal antibody directed to the human interleukin-2 receptor α-chain used for prevention of acute rejection episodes in organ transplantation. The minimally effective serum concentration necessary to saturate receptor epitopes in kidney transplant patients is 0.2 μg/ml. To guide dose selection for Phase 3 efficacy trials, a population pharmacostatistical model was fitted to intensively sampled Phase 2 pharmacokinetic data. This served as a basis from which to examine candidate dose regimens with respect to the duration over which receptor-saturating concentrations would be achieved posttransplant. Three prediction methods were assessed: one based on simulations, and two others based on first-order approximation using either inverse regression or inversion of confidence intervals. An 80% prediction interval was generated by each method to evaluate its predictive performance against prospectively collected Phase 3 data in 39 renal transplant patients who received two injections of 20mg basiliximab, one prior to surgery and one on Day 4 posttransplant. All methods provided correct prediction of the duration of receptor-saturating concentration. As anticipated, the best performance was obtained from the simulation method which predicted 30 values in the 80% prediction interval, 19.7–52.7 days. The actually observed 80% interval from the Phase 3 data was 23.7–58.3 days.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 79
    Electronic Resource
    Electronic Resource
    Springer
    Journal of pharmacokinetics and pharmacodynamics 27 (1999), S. 559-575 
    ISSN: 1573-8744
    Keywords: T-helper cells ; trafficking ; rebound ; corticosteroids ; circadian rhythm ; methylprednisolone ; drug interactions ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract A physiologic pharmacodynamic model was developed to jointly characterize the effects of corticosteroid treatment on adrenal suppression and T-helper cell trafficking during single and multiple dosing in asthmatic patients. Methylprednisolone (MP), cortisol, and T-helper cell concentrations obtained from a previously published study during single day and 6 days of multiple dosing MP treatment were examined. The formation and disposition kinetics of MP were described with a compartmental model. The biorhythmic profile of basal cortisol secretion rate was analyzed using a recent Fourier approach based on circadian harmonics. A three-compartment loop model was proposed to represent three major T-helper cell pools: blood, extravascular site, and lymph nodes. T-helper cell synthesis and degradation rate constants were obtained from the literature. The suppressive effects of cortisol and MP on T-helper cell concentrations were described with a joint additive inhibition function altering the cell migration rate from lymph nodes to blood. The model adequately described both plasma cortisol profiles and T-helper cells in blood after single and multiple doses of MP. The potency of MP for suppression of cortisol secretion was estimated as IC50 = 0.8 ng/ml. The biorhythmic nature of the basal T-helper cells in blood was well described as under the influence of basal circadian cortisol concentrations with IC50 = 79 ng/ml. The model fitted potency of MP for suppression of T-helper cells was IC50 = 4.6 ng/ml. The observed rebound of T-helper cells in blood can also be described by the proposed model. The rhythm and suppression of plasma cortisol and T-helper cells before and during single and multiple dose MP treatment were adequately described by these extended indirect response models.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 80
    ISSN: 1573-904X
    Keywords: etomidate ; pharmacokinetics ; pharmacodynamics ; rat ; electroencephalogram
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The effect-plasma concentration relationship of etomidate was studied in the rat using electroencephalographic changes as a pharmacodynamic parameter. Methods. Etomidate was infused (50 mg/kg/h) in chronically instrumented rats (n = 6) until isoelectric periods of 5 s or longer were observed in the electroencephalogram (EEG). The EEG was continuously recorded during the experiment and frequent arterial blood samples were taken for determination of etomidate plasma concentrations. The changes observed in the raw EEG signal were quantified using aperiodic analysis in the 2.5−7.5 Hz frequency band. The return of the righting reflex was used as another parameter of anesthesia. Results. A mean dose of 8.58 ± 0.41 mg/kg needed to be infused to reach the end point of 5 s isoelectric EEG. The plasma concentration time profiles were most adequately fitted using a three-exponential model. Systemic clearance, volume of distribution at steady-state and elimination half-life averaged 93 ± 6 ml/min/kg, 4.03 ± 0.24 l/kg and 59.4 ± 10.7 min respectively. The EEG effect-plasma concentration relationship was biphasic exhibiting profound hysteresis. Semi-parametric minimization of this hysteresis revealed an equilibration half-life of 2.65 ± 0.15 min, and the biphasic effect-concentration relationship was characterized nonparametrically by descriptors. The effect-site concentration at the return of the righting reflex was 0.44 ± 0.03 μg/ml. Conclusions. The results of the present study show that the concentration-effect relationship of etomidate can be characterized in individual rats using aperiodic analysis in the 2.5−7.5 Hz frequency band of the EEG. This characterization can be very useful for studying the influence of diseases on the pharmacodynamics of etomidate in vivo.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 81
    ISSN: 1573-904X
    Keywords: bioequivalence ; neural networks ; prediction ; pharmacokinetics ; verapamil
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The methodology of predicting the pharmacokinetic parameters (AUC, cmax, tmax) and the assessment of their variability in bioequivalence studies has been developed with the use of artificial neural networks. Methods. The data sets included results of 3 distinct bioequivalence studies of oral verapamil products, involving a total of 98 subjects and 312 drug applications. The modeling process involved building feedforward/backpropagation neural networks. Models for pharmacokinetic parameter prediction were also used for the assessment of their variability and for detecting the most influential variables for selected pharmacokinetic parameters. Variables of input neurons based on logistic parameters of the bioequivalence study, clinical-biochemical parameters, and the physical examination of individuals. Results. The average absolute prediction errors of the neural networks for AUC, cmax, and tmax prediction were: 30.54%, 39.56% and 30.74%, respectively. A sensitivity analysis demonstrated that for verapamil the three most influential variables assigned to input neurons were: total protein concentration, aspartate aminotransferase (AST) levels, and heart-rate for AUC, AST levels, total proteins and alanine aminotransferase (ALT) levels, for cmax, and the presence of food, blood pressure, and body-frame for tmax. Conclusions. The developed methodology could supply inclusion or exclusion criteria for subjects to be included in bioequivalence studies.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 82
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 1392-1398 
    ISSN: 1573-904X
    Keywords: topical application ; dermal absorption ; cutaneous perfusion ; pharmacokinetics ; binding ; half life
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Many compounds are applied to the skin with the aim of targeting deeper underlying tissues. This work sought to define the pharmacokinetics of solutes in tissues below a topical application site in terms of perfusate binding, tissue binding and perfusate flow rate. Methods. The disposition kinetics of diclofenac in a single pass perfused limb preparation after dermal application disposition was studied using dextran and bovine serum albumin (BSA) containing perfusates. A pharmacokinetic model was then developed to relate the tissue retention half lives for diclofenac, diazepam, water, lignocaine and salicylate to their fraction unbound in the tissues, their fraction unbound in the perfusate and the perfusate flow rate. Results. Diclofenac had estimated tissue retention half lives of 18.1 hr and 3.5 hr for the dextran and BSA containing perfusates, respectively. The fraction of diclofenac and other solutes unbound in the tissues correlated with their corresponding fraction unbound in the perfusate. The tissue retention half lives for diclofenac and other solutes could be described in terms of the fraction of solute unbound in the tissues and perfusate, together with the flow rate. Conclusions. The tissue pharmacokinetics of solutes below a topical application are a function of their binding in the tissues, binding in perfusate and local blood flow.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 83
    ISSN: 1573-904X
    Keywords: submicron lipid emulsion ; supersaturation ; tirilazad ; venous irritation ; pharmacokinetics ; tissue distribution
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To compare the venous irritation, pharmacokinetics, and tissue distribution of tirilazad in rats after intravenous administration of a submicron lipid emulsion with that of an aqueous solution. Methods. Venous irritation was determined by microscopic evaluation of injury to the lateral tail veins of rats. Pharmacokinetic parameters were determined by following plasma concentrations of drug. Tissue distribution of [14C]-tirilazad was determined by quantitative whole body autoradiography. Results. Single dose injections of tirilazad as an emulsion at doses ranging from 1.52 mg to 13.5 mg were non-irritating whereas the solution was irritating at a dose of 1.3 mg. The pharmacokinetic parameters were not statistically different between the emulsion and the solution (p 〉 0.2) at doses of 6 mg/kg/day and 20 mg/kg/day. However, at 65 mg/kg/day dose, a higher AUC(0,6) (4-fold) and lower Vss (18-fold) and CL(5-fold) were observed for the lipid emulsion as compared to the solution (p 〈 0.05). Tissue distribution showed higher initial concentrations (two fold or more) in most tissues for the solution. These values, however, equilibrated by 4 h and AUC(0,4) differences were less than two fold in most tissues. Conclusions. Formulating tirilazad in the lipid emulsion significantly reduces the venous irritation without changing the pharmacokinetics and tissue distribution at low doses.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 84
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 587-591 
    ISSN: 1573-904X
    Keywords: quinolones ; pharmacokinetics ; permeability ; tissue binding ; hindlimb
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 85
    ISSN: 1573-904X
    Keywords: C6-glioma ; methotrexate ; microdialysis ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Establishment of the pharmacokinetic profile of methotrexate (MTX) in the extracellular fluid (ECF) of a brain C6-glioma in rats. Methods. Serial collection of plasma samples and ECF dialysates after i.v. infusion of MTX (50 or 100 mg/kg) for 4 h. HPLC assay. Results. Histological studies revealed the presence of inflammation, edema, necrosis, and hemorrhage in most animals. In vivo recovery (reverse dialysis) was 10.8 ± 5.3%. MTX concentrations in tumor ECF represented about 1−2% of the plasma concentrations. Rapid equilibration between MTX levels in brain tumor ECF and plasma. ECF concentrations almost reached steady-state by the end of the infusion (4 h), then decayed in parallel with those in plasma. Doubling of the dose did not modify MTX pharmacokinetic parameters (t1/2α, t1/2β, MRT, fb, Vd, and CLT), except for a 1.7-fold increase of AUCPlasma and a 3.8-fold increase in AUCECF which resulted in a 2.3-fold increase in penetration (AUCECF/AUCPlasma). In spite of an important interindividual variability, a relationship between MTX concentrations in plasma and tumor ECF could be established from mean pharmacokinetic parameters. Conclusions. High plasma concentrations promote the penetration of MTX into brain tissue. However, free MTX concentrations in tumor ECF remain difficult to predict consistently.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 86
    ISSN: 1573-904X
    Keywords: HI-240 ; nonnucleoside inhibitor ; pharmacokinetics ; HPLC
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. The purpose of the present study was to examine the pharmacokinetic features and tissue distribution of N-[2-(2-fluorophenethyl)]-N′-[2-(5-bromopyridyl)]-thiourea (HI-240), a novel non-nucleoside inhibitor of HIV reverse transcriptase with potent anti-viral activity against AZT-sensitive as well as multidrug-resistant HIV-1 strains. Methods. A sensitive and accurate high performance liquid chromatography (HPLC)-based quantitative detection method was established to measure concentrations of HI-240 in pharmacokinetic studies. The plasma concentration-time data were modeled by using the WinNonlin program to estimate the pharmacokinetic parameter values. Results. HI-240 had an elimination half-life of 78.3 ± 2.0 min after i.v. administration and 196.8 ± 3.1 min after i.p. administration. The systemic clearance of HI-240 was 2194 ± 61 ml/h/kg after i.v. administration and 9339 ± 1160 ml/h/kg after i.p. administration. Following i.v. injection, HI-240 rapidly distributed to and accumulated in multiple tissues with particularly high accumulation in adipose tissue, adrenal gland, and uterus+ovary. The concentration of HI-240 in brain tissue was comparable to that in the plasma, indicating that HI-240 easily crosses the blood-brain-barrier. Following i.p. injection, HI-240 was rapidly absorbed with a t1/2ka and a tmax values of less than 10 min. Following oral administration, HI-240 was absorbed with a t1/2ka of 4.2 ±1.1 min and a tmax of 95.1 ± 25.1 min. The intraperitoneal bioavailability was estimated at 23.5%, while the oral bioavailability was only 1%. Conclusions. The HPLC-based accurate and precise analytical detection method and pilot pharmacokinetic studies described herein provide the basis for advanced preclinical pharmacodynamic studies of HI-240. The ability of HI-240 to distribute rapidly and extensively into extravascular compartments and easily cross the blood-brain barrier represent significant pharmacokinetic advantages over AZT.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 87
    ISSN: 1573-904X
    Keywords: pharmacokinetics ; Calphostin C ; HPLC ; perylenequinone
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To examine the pharmacokinetic features and metabolism of calphostin C, a naturally occurring perylenequinone with potent antileukemic activity. Methods. HPLC-based quantitative detection methods were used to measure calphostin C levels in lysates of leukemic cells and in plasma of mice treated with calphostin C. The plasma concentration-time data were analyzed using the WinNonlin program. In vitro esterases and a microsome P450 preparation in conjunction with a LC-MS(API-EI) system were used to study the metabolism of calphostin C. Results. An intracellular exposure level (AUC0−6h) of 257 μM·h was achieved after in vitro treatment of NALM-6 cells with calphostin C at a 5 μM final concentration in culture medium. After intraperitoneal (i.p.) injection of a 40 mg/kg nontoxic bolus dose of calphostin C, the estimated Cmax was 2.9 μM, which is higher than the effective in vitro concentration of calphostin C against leukemic cells. Drug absorption after i.p. administration was rapid with an absorption half-life of 24.2 min and the estimated tmax was 63.0 min. Calphostin C was cleared with an elimination half-life of 91.3 min. An inactive and smaller metabolite (calphostin B) was detected in plasma of calphostin C-treated mice with a tmax of 41.3 min. Esterase (but not P450) treatment of calphostin C in vitro yielded an inactive metabolite (calphostin B) of the same size and elution profile. Conclusions. Target plasma calphostin C concentrations of potent antileukemic activity can be reached in mice at nontoxic dose levels. This pilot pharmacokinetic study of calphostin C combined with the availability of the described quantitative HPLC method for its detection in cells and plasma provide the basis for future preclinical evaluation of calphostin C and its potential as an anti-leukemic drug.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 88
    ISSN: 1573-904X
    Keywords: bezafibrate ; hyperlipidemia ; pharmacodynamics ; pharmacokinetics ; sustained release
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To evaluate the role of different routes and modes of administration of bezafibrate (BZF) on its hypolipidemic activity. We hypothesize that the major sites of BZF action are located presystemically as in other 'gastrointestinal (GI) drugs.' Thus, continuous administration of the drug to the GI tract is expected to augment its efficacy and provides a rationale for an oral sustained release preparation of the drug. Methods. The hypothesis was investigated in three experimentally induced-hyperlipidemia rat models. Models A and B were based on cholesterol-enriched diets and Model C on induced acute hyperlipidemia by triton 225 mg/kg. The pharmacokinetics and the pharmacodynamics of the drug following various modes of administration were examined. Results. In all cases, continuous administration of the drug into the duodenum (IGI) at a dose of 30 mg/kg/day for 3 days (Models A and B) or over 18 hr (Model C) reduced significantly both total cholesterol and triglycerides levels and elevated HDL cholesterol levels in comparison to bolus oral administration of the same dose, as well as in comparison to equivalent intravenous infusion (Model C). Infusion of the drug directly into the portal vein produced an equivalent activity to IGI administration. The pharmacokinetic study showed 100% oral bioavailability, good colonic absorption properties and an indication for an enterohepatic cycle. Conclusions. The results confirm that BZF has a first pass hepatic pharmacodynamic effect. Administration of BZF in a slow release matrix tablet to the rats produced the same magnitude of effect as IGI administration, thus proving the pharmacodynamic rationale for this mode of administration for GI drugs.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 89
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular neurobiology 19 (1999), S. 309-323 
    ISSN: 1573-6830
    Keywords: cytochrome P450 ; enzyme inhibition ; enzyme induction ; pharmacokinetics ; drug interaction ; in vitro assessment ; clinical assessment
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract 1. The cytochrome P450 enzyme family is one of the major drug metabolizing systems in man. 2. Factors such as age, gender, race, environment, and drug treatment may have considerable influence on the activity of these enzymes. 3. There are now well-established in vitro techniques for assessing the role of specific cytochrome P450 enzymes in the metabolism of drugs, as well as the inhibitory or inducing effects of drugs on enzyme activity. In vitro data have been utilized to predict clinical outcomes (i.e., pharmacokinetic interactions), with close correlations between in vitro and in vivo data. 4. This information can be of considerable practical assistance to clinicians, to help with rational prescribing or to prevent or minimize the potential for drug interactions.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 90
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular neurobiology 19 (1999), S. 355-372 
    ISSN: 1573-6830
    Keywords: enantiomers ; racemic ; chiral ; stereoselective ; pharmacokinetics ; cytochrome P450 ; geometric isomers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract 1. Many drugs used to treat psychiatric disorders contain a chiral center or a center of unsaturation and are marketed as a mixture of the resultant enantiomers or geometric isomers, respectively. These enantiomers or geometric isomers may differ markedly with regard to their pharmacodynamic and/or pharmacokinetic properties. 2. Examples of the effects of chiral centers or geometric centers on such properties are given for drugs from the following classes: antidepressants (tricyclics, selective serotonin reuptake inhibitors, monoamine oxidase inhibitors, viloxazine, bupropion, trazodone, mianserin, venlaflaxine); benzodiazepines, zoplicone, and antipsychotics. 3. As described in this review, there are several notable examples of psychiatric drugs currently available where the individual enantiomers or geometric isomers differ considerably with regard to factors such as effects on amine transport systems, interactions with receptors and metabolizing enzymes, and clearance rates from the body. Indeed, relatively recent developments in analytical and preparative resolution of racemic and geometric drug mixtures and increased interest in developing new drugs which interact with specific targets, which have been described in detail at the molecular level, have resulted in increased emphasis on stereochemistry in drug development.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 91
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular neurobiology 19 (1999), S. 443-466 
    ISSN: 1573-6830
    Keywords: selective serotonin reuptake inhibitors ; metabolism ; pharmacokinetics ; fluoxetine ; fluvoxamine ; paroxetine ; sertraline ; citalopram ; cytochrome P450
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract 1. Five drugs with the predominant pharmacologic effect of inhibiting the neuronal reuptake of serotonin are available worldwide for clinical use. This class of psychoactive drugs, known as selective serotonin reuptake inhibitors (SSRIs), is comprised of fluoxetine, sertraline, paroxetine, fluvoxamine, and citalopram. 2. The SSRIs appear to share similar pharmacodynamic properties which translate to efficacy in the treatment of depression and anxiety syndromes. The drugs are differentiated by their pharmacokinetic properties with regard to stereochemistry, metabolism, inhibition of cytochrome enzymes, and participation in drug–drug interactions. Studies focusing on the relationship of plasma drug concentration to therapeutic and adverse effects have not confirmed the value of plasma concentration monitoring. 3. This review summarizes the metabolism and relevant pharmacokinetic properties of the SSRIs.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 92
    Electronic Resource
    Electronic Resource
    Springer
    Cellular and molecular neurobiology 19 (1999), S. 373-409 
    ISSN: 1573-6830
    Keywords: antidepressants ; tricyclic ; metabolism ; hydroxy metabolites ; pharmacokinetics ; pharmacogenetics ; drug–drug interactions ; toxicity ; plasma concentrations
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract 1. Despite the considerable advances in the treatments available for mood disorders over the past generation, tricyclic antidepressants (TCAs) remain an important option for the pharmacotherapy of depression. 2. The pharmacokinetics of TCAs are characterized by substantial presystemic first-pass metabolism, a large volume of distribution, extensive protein binding, and an elimination half-life averaging about 1 day (up to 3 days for protriptyline). 3. Clearance of tricyclics is dependent primarily on hepatic cytochrome P450 (CYP) oxidative enzymes. Although the activities of some P450 isoenzymes are largely under genetic control, they may be influenced by external factors, such as the concomitant use of other medications or substances. Patient variables, such as ethnicity and age, also affect TCA metabolism. The impact of gender and related reproductive issues is coming under increased scrutiny. 4. Metabolism of TCAs, especially their hydroxylation, results in the formation of active metabolites, which contribute to both the therapeutic and the adverse effects of these compounds. 5. Renal clearance of the polar metabolites of TCAs is reduced by normal aging, accounting for much of the increased risk of toxicity in older patients. 6. Knowledge of factors affecting the metabolism of TCAs can further the development and understanding of newer antidepressant medications.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 93
    ISSN: 1573-904X
    Keywords: antisense ; Brown-Norway rat ; oligodeoxynucleotide ; pulmonary delivery ; ISIS 2105 ; pharmacokinetics ; airway inflammation
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To evaluate the pulmonary distribution of CGP69846A (ISIS 5132), a phosphorothioate oligonucleotide, following intra-tracheal (i.t.) instillation into Brown-Norway rats. Methods. The pharmacokinetic profile of [3H]-CGP69846A was investigated following i.t. instillation into both naïve and inflamed airways of Brown-Norway rats. The cellular distribution was determined using autoradiography, immunohistochemistry and flow cytometry/fluorescence microscopy, in inflamed airways. Results. CGP69846A displayed a dose-dependent lung retention following i.t. administration which was unaffected by local inflammation. Autoradiography and immunohistochemistry showed distribution to alveolar macrophages, eosinophils, bronchial and tracheal epithelium and alveolar cells. Studies with [FITCJ-CGP69846A demonstrated a preferential association of oligonucleotide with leukocytes in bronchial lavage fluid of: macrophages 〉 eosinophils = neutrophils 〉 〉 lymphocytes. Conclusions. The dose-dependency of lung retention together with cell-specific uptake suggests that the lung can be used as a local target for antisense molecules with potentially minimal systemic effects. Furthermore, the preferential targeting of macrophages and the airway epithelium by oligonucleotides may represent rational cellular targets for antisense therapeutics.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 94
    ISSN: 1573-904X
    Keywords: nonlinear mixed effects modeling (NONMEM) ; pharmacokinetics ; telmisartan ; bioavailability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 95
    ISSN: 1573-904X
    Keywords: antisense phosphorothioate oligonucleotide ; stealth liposome ; pharmacokinetics ; monkey ; capillary gel electrophoresis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. This study examined the pharmacokinetics and tissue distribution of an antisense oligonucleotide ISIS 2503, formulated in stealth (pegylated) liposomes (encapsulated) or in phosphate-buffered saline (unencapsulated). Methods. Encapsulated or unencapsulated ISIS 2503 was administered to rhesus monkeys by intravenous infusion. The concentrations of ISIS 2503 and metabolites in blood, plasma, and tissue samples were determined by capillary gel electrophoresis. Results. Plasma concentrations of encapsulated ISIS 2503 decreased mono-exponentially after infusion with a mean half-life of 57.8 hours. In contrast, the concentration of unencapsulated ISIS 2503 in plasma decreased rapidly with a mean half-life of 1.07 hours. Both encapsulated and unencapsulated ISIS 2503 distributed widely into tissues. Encapsulated ISIS 2503 distributed primarily to the reticulo-endothelial system and there were few metabolites observed. In contrast, unencapsulated ISIS 2503 distributed rapidly to tissue with highest concentration seen in kidney and liver. Nuclease-mediated metabolism was extensive for unencapsulated oligonucleotide in plasma and tissues. Conclusions. The data suggest that stealth liposomes protect ISIS 2503 from nucleases in blood and tissues, slow tissue uptake, and slow the rate of clearance from the systemic circulation. These attributes may make these formulations attractive for delivering oligonucleotides to sites with increased vasculature permeability such as tumors or sites of inflammation.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 96
    ISSN: 1573-904X
    Keywords: aminolevulinic acid ; intravesical ; pharmacokinetics ; photodiagnosis ; bladder ; cancer
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To examine the stability and systemic absorption of aminolevulinic acid (ALA) in dogs during intravesical administration. Methods. Nine dogs received an intravesical dose of ALA either with no prior treatment, after receiving ammonium chloride for urinary acidification, or after receiving sodium bicarbonate for urinary alkalinization. Urine and blood samples collected during and after administration were monitored for ALA using an HPLC assay developed in our laboratories. Concentrations of pyrazine 2,5-dipropionic acid, the major ALA degradation product, and radiolabeled inulin, a nonabsorbable marker for urine volume, were also determined. Results. Less than 0.6% of intravesical ALA doses was absorbed into plasma. Urine concentrations decreased to 37% of the initial concentration during the 2 hour instillation. Decreases in urinary ALA and radiolabeled inulin concentrations were significantly correlated, indicating that urine dilution accounted for over 80% of observed decreases in urinary ALA. ALA conversion to pyrazine 2,5-dipropionic acid was negligible. Conclusions. These studies demonstrate that ALA is stable and poorly absorbed into the systemic circulation during intravesical instillation. Future studies utilizing intravesical ALA for photodiagnosis of bladder cancer should include measures to restrict fluid intake as a means to limit dilution and maximize ALA concentrations during instillation.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 97
    ISSN: 1573-904X
    Keywords: diffusion model ; drug delivery system ; ocular penetration ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To characterize the ocular pharmacokinetics of beta-blockers (timolol and tilisolol) after instillation in the albino rabbit using a mathematical model that includes a diffusion process. Methods. The disposition of fluorescein isothiocyanate-dextran (FITC-dextran, molecular weight 4400), timolol, and tilisolol was determined in tear fluid and aqueous humor after instillation or ocular injection in rabbits. The in vivo penetration parameters were estimated by fitting the concentration-time profiles to the Laplace equations based on a diffusion model using MULTI(FILT) program. Thein vivo permeability of drugs was measured across cornea using a two-chamber diffusion cell. Results. Concentration-time profiles of drugs in the tear fluid after instillation showed a monoexponential curve. Although a monoexponential curve was observed in the aqueous humor concentration of FITC-dextran after injection into the aqueous chamber, timolol and tilisolol showed a biexponential curve. On the basis of these results, anin vivo pharmacokinetic model was developed for estimation of penetration parameters. The in vitro partition parameters were higher than those of the in vivo parameters. Conclusions. The ocular absorption of timolol and tilisolol was characterized using an in vivo pharmacokinetic model and in vivo penetration parameters.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 98
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 1608-1615 
    ISSN: 1573-904X
    Keywords: tenidap ; pharmacokinetics ; EM algorithm ; nonlinear mixed-effects modelling ; covariates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. To develop a pharmacokinetic model for tenidap and to identify important relationships between the pharmacokinetic parameters and available covariates. Methods. Plasma concentration data from several phase I and phase II studies were used to develop a pharmacokinetic model for tenidap, a novel anti-rheumatic drug. An appropriate pharmacokinetic model was selected on the basis of individual nonlinear regression analyses and an EM algorithm was used to perform a nonlinear mixed-effects analysis. Scatter plots of posterior individual pharmacokinetic parameters were used to identify possible covariate effects. Results. Predicted responses were in good agreement with the observed data. A bi-exponential model with zero order absorption was subsequently used to develop the mixed-effects model. Covariate relationships selected on the basis of differences in the objective function, although statistically significant, were not particularly strong. Conclusions. The pharmacokinetics of tenidap can be described by a bi-exponential model with zero order absorption. Based on differences in the log-likelihood, significant covariate-parameter relationships were identified between smoking and CL, and between gender and Vss and CLd. Simulated sparse data analyses indicated that the model would be robust for the analysis of sparse data generated in observational studies.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 99
    ISSN: 1573-904X
    Keywords: amphotericin B ; liposomes ; pharmacokinetics ; tissue distribution ; toxicity ; toxicokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Purpose. Amphotericin B (AmB) in small, unilamellar liposomes (AmBisome ®) has an improved therapeutic index, and altered pharmacokinetics. The repeat-dose safety and toxicokinetic profiles of AmBisome were studied at clinically relevant doses. Methods. Beagle dogs (5/sex/group) received intravenous AmBisome (0.25, 1,4, 8, and 16 mg/kg/day), empty liposomes or vehicle for 30 days. AmB was determined in plasma on days 1, 14, and 30, and in tissues on day 31. Safety parameters included body weight, clinical chemistry, hematology and microscopic pathology. Results. Seventeen of twenty animals receiving 8 and 16 mg/kg were sacrificed early due to weight loss caused by reduced food intake. Dose-dependent renal tubular nephrosis, and other effects characteristic of conventional AmB occurred at 1 mg/kg/day or higher. Although empty liposomes and AmBisome increased plasma cholesterol, no toxicities unique to AmBisome were revealed. Plasma ultrafiltrates contained no AmB. AmBisome achieved plasma levels 100-fold higher than other AmB formulations. AmBisome kinetics were non-linear, with clearance and distribution volumes decreasing with increasing dose. This, and nonlinear tissue uptake, suggest AmBisome disposition was saturable. Conclusions. AmBisome has the same toxic effects as conventional AmB, but they appear at much higher plasma exposures. AmBisome's non-linear pharmacokinetics are not associated with increased risk, as toxicity increases linearly with dosage. Dogs tolerated AmBisome with minimal to moderate changes in renal function at doses (4 mg/kg/day) producing peak plasma concentrations of 18−94 µg/mL.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
  • 100
    Electronic Resource
    Electronic Resource
    Springer
    Pharmaceutical research 16 (1999), S. 176-185 
    ISSN: 1573-904X
    Keywords: pharmacokinetics ; pharmacodynamics ; pharmacology ; modeling
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract Pharmacokinetic/pharmacodynamic (PK/PD)-modeling links dose-concentration relationships (PK) and concentration-effect relationships (PD), thereby facilitating the description and prediction of the time course of drug effects resulting from a certain dosing regimen. PK/PD-modeling approaches can basically be distinguished by four major attributes. The first characterizes the link between measured drug concentration and the response system, direct link versus indirect link. The second considers how the response system relates effect site concentration to the observed outcome, direct versus indirect response. The third regards what clinically or experimentally assessed information is used to establish the link between concentration and effect, hard link versus soft link. And the fourth considers the time dependency of pharmacodynamic model parameters, distinguishing between time-variant versus time-invariant. Application of PK/PD-modeling concepts has been identified as potentially beneficial in all phases of preclinical and clinical drug development. Although today predominantly limited to research, broader application of PK/PD-concepts in clinical therapy will provide a more rational basis for patient-specific dosage individualization and may thus guide applied pharmacotherapy to a higher level of performance.
    Type of Medium: Electronic Resource
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...