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  • MDPI - Multidisciplinary Digital Publishing Institute  (41)
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  • 1
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    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
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  • 2
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    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
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  • 3
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    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
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  • 4
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    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
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  • 5
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    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
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  • 6
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    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
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  • 7
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    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
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  • 8
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    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
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  • 9
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    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
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  • 10
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    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
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  • 11
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    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
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  • 12
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    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
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  • 13
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    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
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  • 14
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    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
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  • 15
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    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
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  • 16
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    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
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  • 17
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    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
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  • 18
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    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
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  • 19
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    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
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  • 20
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    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
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  • 21
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    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
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  • 22
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    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
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  • 23
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    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
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  • 24
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    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
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  • 25
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    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
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  • 26
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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    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
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  • 40
    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
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  • 41
    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
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  • 42
    Publication Date: 2021-06-14
    Description: Methane plays an important role in the Earth’s atmospheric chemistry and radiative balance being the most important greenhouse gas after carbon dioxide. It has recently been established that geogenic gases contribute significantly to the natural CH4 flux to the atmosphere (Etiope et al., 2008). Volcanic/geothermal areas contribute to this flux, being the site of widespread diffuse degassing of endogenous gases (Chiodini et al., 2005). In such an environment soils are a source rather than a sink for atmospheric CH4 (Cardellini et al., 2003; Castaldi and Tedesco, 2005; D’Alessandro et al., 2009; 2011; 2013). Due to the fact that methane soil flux measurements are laboratory intensive, very few data have been collected until now in these areas. Preliminary studies (Etiope et al., 2007) estimated a total CH4 emission from European geothermal and volcanic systems in the range 4-16 kt a-1. This estimate was obtained indirectly from CO2 or H2O output data and from CO2/CH4 or H2O/CH4 values measured in the main gaseous manifestations. Such methods, although acceptable to obtain order-of-magnitude estimates, completely disregard possible methanotrophic activity within the soil. At the global scale, microbial oxidation in soils contributes for about 3-9% to the total removal of methane from the atmosphere. But the importance of methanotrophic organisms is even larger because they oxidise the greatest part of the methane produced in the soil and in the subsoil before its emission to the atmosphere. Environmental conditions in the soils of volcanic/geothermal areas (i.e. low oxygen content, high temperature and proton activity, etc.) have been considered inadequate for methanotrophic microrganisms. But recently, it has been demonstrated that methanotrophic consumption in soils occurs also under such harsh conditions due to the presence of acidophilic and thermophilic Verrucomicrobia. These organisms were found in Italy at the Solfatara di Pozzuoli (Pol et al., 2007), in New Zealand at Hell’s Gate (Dunfield et al., 2007) and in Kamchatka, Russia (Islam et al., 2008). Both the Italian and the Hellenic territories are geodynamically very active with many active volcanic and geothermal areas. Here we report on methane flux measurements made at Pantelleria (Italy) and at Sousaki and Nisyros (Greece). The total methane output of these three systems is about 10, 19 and 1 t a-1, respectively (D’Alessandro et al., 2009; 2011; 2013). The total emissions obtained from methane flux measurements are up to one order of magnitude lower than those obtained through indirect estimations. Clues of methanotrophic activity within the soils of these areas can be found in the CH4/CO2 ratio of the flux measurements which is always lower than that of the respective fumarolic manifestations, indicating a loss of CH4 during the travel of the gases towards earth’s surface. Furthermore laboratory methane consumption experiments made on soils collected at Pantelleria and Sousaki revealed, for most samples, CH4 consumption rates up to 9.50 µg h-1 and 0.52 µg h-1 respectively for each gram of soil (dry weight). Only few soil samples displayed no methane consumption activity. Finally, microbiological and molecular investigations allowed us to identify the presence of methanotrophic bacteria belonging to the Verrucomicrobia and to the Alpha- and Gamma-Proteobacteria in the soils of the geothermal area of Favara Grande at Pantelleria. While the presence of the former was not unexpected due to the fact that they include acidophilic and thermophilic organisms that were previously found in other geothermal environments, the latter are generally considered not adapted to live in harsh geothermal environments. Their presence in the soils of Pantelleria could be explained by the fact that these soils do not have extremely low pH values (〉5). Indeed thermotollerant methanotrophic Gamma-proteobacteria, have been previously found in the sediments of thermal springs in Kamchatka (Kizilova et al., 2012). Such species could find their niches in the shallowest part of the soils of Favara Grande were the temperatures are not so high and they thrive on the abundant upraising hydrothermal methane.
    Description: Published
    Description: Patras, Greece
    Description: 4.5. Studi sul degassamento naturale e sui gas petroliferi
    Description: open
    Keywords: soil methane fluxes ; methanotrophic activity ; geothermal areas ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
    Type: Oral presentation
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  • 43
    Publication Date: 2017-04-04
    Description: Methane plays an important role in the Earth’s atmospheric chemistry and radiative balance being the second most important greenhouse gas after carbon dioxide. Methane is released to the atmosphere by a wide number of sources, both natural and anthropogenic, with the latter being twice as large as the former (IPCC, 2007). It has recently been established that significant amounts of geological methane, produced within the Earth’s crust, are currently released naturally into the atmosphere (Etiope, 2004). Active or recent volcanic/geothermal areas represent one of these sources of geological methane. But due to the fact that methane flux measurements are laboratory intensive, very few data have been collected until now and the contribution of this source has been generally indirectly estimated (Etiope et al., 2007). The Greek territory is geodynamically very active and has many volcanic and geothermal areas. Here we report on methane flux measurements made at two volcanic/geothermal systems along the South Aegean volcanic arc: Sousaki and Nisyros. The former is an extinct volcanic area of Plio-Pleistocene age hosting nowadays a low enthalpy geothermal field. The latter is a currently quiescent active volcanic system with strong fumarolic activity due to the presence of a high enthalpy geothermal system. Both systems have gas manifestations that emit significant amounts of hydrothermal methane and display important diffuse carbon dioxide emissions from the soils. New data on methane isotopic composition and higher hydrocarbon contents point to an abiogenic origin of the hydrothermal methane in the studied systems. Measured methane flux values range from –48 to 29,000 (38 sites) and from –20 to 1100 mg/mˆ2/d (35 sites) at Sousaki and Nisyros respectively. At Sousaki measurement sites covered almost all the degassing area and the diffuse methane output can be estimated in about 20 t/a from a surface of about 10,000 mˆ2. At Nisyros measurements covered the Stephanos and Kaminakia areas, which represent only a part of the entire degassing area. The two areas show very different methane degassing pattern with latter showing much higher flux values. Methane output can be estimated in about 0.25 t/a from an area of about 30,000 mˆ2 at Stephanos and about 1 t/a from an area of about 20,000 mˆ2 at Kaminakia. The total output from the entire geothermal system of Nisyros probably should not exceed 2 t/a.
    Description: Published
    Description: Vienna, Austria
    Description: 4.5. Studi sul degassamento naturale e sui gas petroliferi
    Description: open
    Keywords: methane output ; diffuse degassing ; volcanic/hydrothermal systems ; Greece ; 01. Atmosphere::01.01. Atmosphere::01.01.03. Pollution ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 05. General::05.02. Data dissemination::05.02.01. Geochemical data ; 05. General::05.08. Risk::05.08.01. Environmental risk
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
    Type: Poster session
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  • 44
    Publication Date: 2017-04-04
    Description: A biomonitoring survey, above tree line level, using two endemic species (Senecio aethnensis and Rumex aethnensis) was performed on Mt. Etna, in order to evaluate the dispersion and the impact of volcanic atmospheric emissions. Samples of leaves were collected in summer 2008 from 30 sites in the upper part of the volcano (1500- 3000 m a.s.l). Acid digestion of samples was carried out with a microwave oven, and 44 elements were analyzed by using plasma spectrometry (ICP-MS and ICP-OES). The highest concentrations of all investigated elements were found in the samples collected closest to the degassing craters, and in the downwind sector, confirming that the eastern flank of Mt. Etna is the most impacted by volcanic emissions. Leaves collected along two radial transects from the active vents on the eastern flank, highlight that the levels of metals decrease one or two orders of magnitude with increasing distance from the source. This variability is higher for volatile elements (As, Bi, Cd, Cs, Pb, Sb, Tl) than for more refractory elements (Al, Ba, Sc, Si, Sr, Th, U). The two different species of plants do not show significant differences in the bioaccumulation of most of the analyzed elements, except for lanthanides, which are systematically enriched in Rumex leaves. The high concentrations of many toxic elements in the leaves allow us to consider these plants as highly tolerant species to the volcanic emissions, and suitable for biomonitoring researches in the Mt. Etna area.
    Description: Published
    Description: Vienna, Austria
    Description: 4.4. Scenari e mitigazione del rischio ambientale
    Description: open
    Keywords: Mt. Etna ; biomonitoring ; Trace elements ; 01. Atmosphere::01.01. Atmosphere::01.01.03. Pollution ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 05. General::05.02. Data dissemination::05.02.01. Geochemical data ; 05. General::05.08. Risk::05.08.01. Environmental risk
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
    Type: Poster session
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  • 45
    Publication Date: 2017-04-04
    Description: This guide reports the description of the experimental apparata in use in the experimental petrology along with an accurate description of some applications of these instrumentations. After a brief introduction concerning what is the experimental petrology and what is used for, we provide a description of the starting materials used in this field of the Earth Sciences. Moreover, particular attention is focused on these apparata used all around the world. We, finally, introduce some examples of different studies conducted with the different experimental equipments. The aim of this guide is, then, to give information concerning the equipments and their potentiality.
    Description: Published
    Description: 1-20
    Description: 2.3. TTC - Laboratori di chimica e fisica delle rocce
    Description: N/A or not JCR
    Description: open
    Keywords: Piston cylinder ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 46
    Publication Date: 2017-04-04
    Description: Volcanoes represent an important natural source of several trace elements to the atmosphere. For some species (e.g., As, Cd, Pb and Se) they may be the main natural source and thereby strongly influencing geochemical cycles from the local to the global scale. Mount Etna is one of the most actively degassing volcanoes in the world, and it is considered to be, on the long-term average, the major atmospheric point source of many environmental harmful compounds. Their emission occurs either through continuous passive degassing from open-conduit activity or through sporadic paroxysmal eruptive activity, in the form of gases, aerosols or particulate. To estimate the environmental impact of magma-derived trace metals and their depositions processes, rainwater and snow samples were collected at Mount Etna area. Five bulk collectors have been deployed at various altitudes on the upper flanks around the summit craters of the volcano; samples were collected every two week for a period of one year and analyzed for the main chemical-physical parameters (electric conductivity and pH) and for major and trace elements concentrations. Chemical analysis of rainwater clearly shows that the volcanic contribution is always prevailing in the sampling site closest to the summit crater (about 1.5 km). In the distal sites (5.5-10 km from the summit) and downwind of the summit craters, the volcanic contribution is also detectable but often overwhelmed by anthropogenic or other natural (seawater spray, geogenic dust) contributions. Volcanic contribution may derive from both dry and wet deposition of gases and aerosols from the volcanic plume, but sometimes also from leaching of freshly emitted volcanic ashes. In fact, in our background site (7.5 km in the upwind direction) volcanic contribution has been detected only following an ash deposition event. About 30 samples of fresh snow were collected in the upper part of the volcano, during the winters 2006 and 2007 to estimate deposition processes at high altitude during cold periods. Some of the samples were collected immediately after a major explosive event from the summit craters to understand the interaction between snow and fresh erupted ash. Sulphur, Chlorine and Fluorine, are the major elements that prevailingly characterize the volcanic contribution in atmospheric precipitation on Mount Etna, but high concentrations of many trace elements are also detected in the studied samples. In particular, bulk deposition samples display high concentration of Al, Fe, Ti, Cu, As, Rb, Pb, Tl, Cd, Cr, U and Ag, in the site most exposed to the volcanic emissions: median concentration values are about two orders of magnitude higher than those measured in our background site. Also in the snow samples the volcanic signature is clearly detectable and decreases with distance from the summit craters. Some of the analysed elements display very high enrichment values with respect to the average crust and, in the closest site to the summit craters, also deposition values higher than those measured in polluted urban or industrial sites.
    Description: Published
    Description: Vienna, Austria
    Description: 4.5. Degassamento naturale
    Description: open
    Keywords: Mt. Etna ; trace elements ; rainwater ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 03. Hydrosphere::03.03. Physical::03.03.01. Air/water/earth interactions ; 03. Hydrosphere::03.04. Chemical and biological::03.04.03. Chemistry of waters
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
    Type: Oral presentation
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  • 47
    Publication Date: 2017-04-04
    Description: Improving the constraints on the atmospheric fate and depletion rates of acidic compounds persistently emitted by non-erupting (quiescent) volcanoes is important for quantitatively predicting the environmental impact of volcanic gas plumes. Here, we present new experimental data coupled with modelling studies to investigate the chemical processing of acidic volcanogenic species during tropospheric dispersion. Diffusive tube samplers were deployed at Mount Etna, a very active open-conduit basaltic volcano in eastern Sicily, and Vulcano Island, a closed-conduit quiescent volcano in the Aeolian Islands (northern Sicily). Sulphur dioxide (SO2), hydrogen sulphide (H2S), hydrogen chloride (HCl) and hydrogen fluoride (HF) concentrations in the volcanic plumes (typically several minutes to a few hours old) were repeatedly determined at distances from the summit vents ranging from 0.1 to ~10 km, and under different environmental conditions. At both volcanoes, acidic gas concentrations were found to decrease exponentially with distance from the summit vents (e.g., SO2 decreases from ~10,000 μg/m3 at 0.1 km from Etna’s vents down to ~7 _μg/m3 at ~10km distance), reflecting the atmospheric dilution of the plume within the acid gas-free background troposphere. Conversely, SO2/HCl, SO2/HF, and SO2/H2S ratios in the plume showed no systematic changes with plume aging, and fit source compositions within analytical error. Assuming that SO2 losses by reaction are small during short-range atmospheric transport within quiescent (ash-free) volcanic plumes, our observations suggest that, for these short transport distances, atmospheric reactions for H2S and halogens are also negligible. The one-dimensional model MISTRA was used to simulate quantitatively the evolution of halogen and sulphur compounds in the plume of Mt. Etna. Model predictions support the hypothesis of minor HCl chemical processing during plume transport, at least in cloud-free conditions. Larger variations in the modelled SO2/HCl ratios were predicted under cloudy conditions, due to heterogeneous chlorine cycling in the aerosol phase. The modelled evolution of the SO2/H2S ratios is found to be substantially dependent on whether or not the interactions of H2S with halogens are included in the model. In the former case, H2S is assumed to be oxidized in the atmosphere mainly by OH, which results in minor chemical loss for H2S during plume aging and produces a fair match between modelled and measured SO2/H2S ratios. In the latter case, fast oxidation of H2S by Cl leads to H2S chemical lifetimes in the early plume of a few seconds, and thus SO2 to H2S ratios that increase sharply during plume transport. This disagreement between modelled and observed plume compositions suggests that more in-detail kinetic investigations are required for a proper evaluation of H2S chemical processing in volcanic plumes.
    Description: Published
    Description: 1441-1450
    Description: 1.2. TTC - Sorveglianza geochimica delle aree vulcaniche attive
    Description: 4.5. Degassamento naturale
    Description: JCR Journal
    Description: open
    Keywords: Mt. Etna ; volcanic gas plumes ; tropospheric processing ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 48
    Publication Date: 2017-04-04
    Description: Volcanic and geothermal areas are one of the major natural sources of H2S to the atmosphere. Its environmental impact is often the main cause of the opposition to the development of geothermal energy exploitation programs. In this paper we analyze the air concentrations and dispersion pattern of naturally emitted H2S at the geothermal area of Sousaki (Corinthia, Greece). Measurements, made with a network of passive samplers, evidence a rapid decrease of concentration values away from the emission points. The fact that the decrease is more pronounced in the summer with respect to the winter indicates that it is not only due to a dilution effect, but also to redox reactions favoured by higher temperatures and intense sunlight typical of the summer period.
    Description: Published
    Description: 1723-1728
    Description: 1.2. TTC - Sorveglianza geochimica delle aree vulcaniche attive
    Description: JCR Journal
    Description: reserved
    Keywords: Hydrogen sulphide ; Environmental impact of volcanic activity ; Gas hazard ; Passive samplers ; 01. Atmosphere::01.01. Atmosphere::01.01.03. Pollution ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.04. Geology::04.04.12. Fluid Geochemistry ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 04. Solid Earth::04.08. Volcanology::04.08.08. Volcanic risk
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 49
    Publication Date: 2017-04-04
    Description: Active volcanoes are thought to be important contributors to the atmospheric mercury (Hg) budget, and this chemical element is one of the most harmful atmospheric pollutants, owing to its high toxicity and long residence time in ecosystems. There is, however, considerable uncertainty over the magnitude of the global volcanic Hg flux, since the existing data on volcanogenic Hg emissions are sparse and often ambiguous. In an attempt to extend the currently limited dataset on volcanogenic Hg emissions, we summarize the results of Hg flux measurements at seven active open-conduit volcanoes; Stromboli, Asama, Miyakejima, Montserrat, Ambrym, Yasur, and Nyiragongo.. Data from the domebuilding Soufriere Hills volcano are also reported. Using our determined mercury to SO2 mass ratios in tandem with the simultaneously-determined SO2 emission rates, we estimate that the 7 volcanoes have Hg emission rates ranging from 0.2 to 18 t yr-1 (corresponding to a total Hg flux of ~41 t·yr-1). Based on our dataset and previous work, we propose that a Hg/SO2 plume ratio ~10-5 is bestrepresentative of gas emissions from quiescent degassing volcanoes. Using this ratio, we infer a global volcanic Hg flux from persistent degassing of ~95 t·yr-1
    Description: Published
    Description: 497-510
    Description: 1.2. TTC - Sorveglianza geochimica delle aree vulcaniche attive
    Description: 2.4. TTC - Laboratori di geochimica dei fluidi
    Description: JCR Journal
    Description: restricted
    Keywords: Volcanogenic mercury ; Mercury ; Volcanic plume ; Mercury flux ; Mercury inventories ; Atmospheric mercury ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.02. Exploration geophysics::04.02.01. Geochemical exploration ; 04. Solid Earth::04.04. Geology::04.04.12. Fluid Geochemistry ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 04. Solid Earth::04.08. Volcanology::04.08.06. Volcano monitoring
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 50
    Publication Date: 2017-04-04
    Description: Emissions of volcanoes and their depositions do have an immediate impact on their surrounding environment. In the present study, emissions and depositions of the active volcanic and geothermal system Vulcano (Italy) were investigated by active moss biomonitoring (Fig. 1) in the spring of 2012. Sphagnum moss bags were exposed for periods of 3 days, 3, 6 and 9 weeks. Soil and rainwater samples as well as meteorological data were also collected. After exposure, mosses were oven-dried, grinded and each sample was extracted either in deionized water or HNO3 (with H2O2). Extraction solutions were analyzed by ICP-MS for total concentrations of Li, Mg, Sr, Ba, Cr, Mn, S, Fe, Co, Cu, Zn, Mo, W, Tl, As, Sb, Bi, I, and Se. Soil and rain water samples were analyzed for the same trace elements. For elements such as As and Tl, deionized water extracts showed comparable concentrations to HNO3 extracts, indicating either the absence of particles or the presence of water-soluble particles. Elements such as Pb, Ba, Se and Sr were only dissolved to about 10 % or less in deionized water, indicating a significant share of water-insoluble particle formation. Distribution patterns of emissions and depositions over the whole island of Vulcano allowed classifying all investigated elements into four groups based on their origin (Fig. 2). Lithium was found ubiquitously on the island thus likely is of either marine or geogenic origin (group a in Fig. 2). The elements Mg, Fe, Sr, Mn, Zn, Co, and W were found predominantly on the crater where bare soil was present, and were grouped as “soilborne elements” (group b). These elements are characterized by deposition close to their source of origin. Elements with higher concentrations at the fumarolic field were grouped according to their transport characteristics. The elements I, Se, Tl, Bi, Sb, As, and S were considered as true volatiles (group c) being found also further away from the fumarolic field than Pb, Cr, Mo, and Ba which were interpreted to be predominantly emitted as particles (group d). Moss-bag biomonitoring proved to be an effective tool for the study of emission and deposition processes in active volcanic areas which also allows a classification of elements accumulated on the moss by their origin and distribution patterns.
    Description: Published
    Description: Patras, Greece
    Description: 4.5. Studi sul degassamento naturale e sui gas petroliferi
    Description: open
    Keywords: Moss-bags ; trace elements ; biomonitoring ; volcanic emissions ; 01. Atmosphere::01.01. Atmosphere::01.01.03. Pollution ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
    Type: Oral presentation
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  • 51
    Publication Date: 2017-04-04
    Description: Here, we report the first continuous data of geochemical parameters acquired directly from the active summit crater of Vulcano. This approach provides a means to better investigate deep geochemical processes associated with the degassing system of Vulcano Island. In particular, we report on soil CO2 fluxes from the upper part of Vulcano, a closed-conduit volcano, from September 2007 to October 2010. Large variations in the soil CO2 and plume SO2 fluxes (order of magnitude), coinciding with other discontinuous geochemical parameters (CO2 concentrations in fumarole gas) and physical parameters (increase of shallow seismic activity and fumarole temperatures) have been recorded. The results from this work suggest new prospects for strengthening geochemical monitoring of volcanic activity and for improving the constraints in the construction of a “geochemical model”, this being a necessary condition to better understand the functioning of volcanic systems.
    Description: Published
    Description: 1859-1863
    Description: 2V. Dinamiche di unrest e scenari pre-eruttivi
    Description: 4V. Vulcani e ambiente
    Description: 5V. Sorveglianza vulcanica ed emergenze
    Description: 1R. Reti di monitoraggio e Osservazioni
    Description: JCR Journal
    Description: restricted
    Keywords: Vulcano Island ; Geochemical monitoring ; CO2 flux ; CO2 fumaroles ; SO2 flux ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 04. Solid Earth::04.08. Volcanology::04.08.06. Volcano monitoring ; 04. Solid Earth::04.08. Volcanology::04.08.08. Volcanic risk ; 05. General::05.02. Data dissemination::05.02.01. Geochemical data
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 52
    Publication Date: 2017-04-04
    Description: Volcanic emissions are considered one of the major natural sources of several trace metals (e.g. As, Cd, Cu, Pb, and Zn) to the atmosphere [Nriagu, 1989], and the geochemical cycles of these elements have to be considered strongly influenced by volcanic input. However, the accurate estimation of the global volcanic emissions of volatile trace metals into the atmosphere is still affected by a high level of uncertainty. The latter depends on the large variability in the emission of the different volcanoes, and on their changing stage of activity. Moreover, only few of the potential sources in the world have been directly measured [Hinkley et al. 1999]. Atmospheric deposition processes (wet and dry) are the pathways through which volcanic emissions return to the ground (soils, plants, aquifers), resulting in both harmful and beneficial effects [Baxter et al. 1982; Aiuppa et al. 2000; Brusca et al. 2001; Delmelle, 2003; Bellomo et al. 2007; Martin et al. 2009; Floor et al. 2011; Calabrese et al. 2011]. In the first part of this study we present the results of a literature review on trace metals emissions from active volcanoes around the world. In the second part, we present new data on the fluxes of the trace metals from Etna (Italy) and four active volcanoes in the world: Turrialba (Costarica), Nyiragongo (DRC), Mutnovsky and Gorely (Kamchatka). We found 27 publications (the first dating back to the 70’s), 13 of which relate to the Etna and the other include some of the world’s most active volcanoes: Mt. St. Helens, Erebus, Merapi, White Island, Kilauea, Popocatepetl, Galeras, Indonesian arc, Satasuma and Masaya. The review shows that currently there are very few data available, and that the most studied volcano is Mt. Etna. Using these data, we defined a range of fluxes for As, Ba, Bi, Cd, Cu, Fe, Mn, Pb, Se, V and Zn (Figure 1). To obtain new data we sampled particulate filters at the five above mentioned volcanoes. Filters were mineralized (acid digestion) and analyzed by ICP-MS. Sulphur to trace element ratios were related to sulphur fluxes to indirectly estimate trace elements fluxes. Etna confirms to be one of the greatest point sources in the world. The Nyiragongo results to be also a significant source of metals to the atmosphere, especially considering its persistent state of degassing from the lava lake. Also Turrialba and Gorely have high emission rates of trace metals considering the global range. Only Mutnovsky Volcano show values which are sometimes lower than the range obtained from the review, consistent with the fact that it is mainly a fumarolic field. This work highlights the need to expand the current dataset including many other active volcanoes for a better constraint of global trace metal fluxes from active volcanoes.
    Description: Published
    Description: Nicolosi (Catania)
    Description: 1.2. TTC - Sorveglianza geochimica delle aree vulcaniche attive
    Description: open
    Keywords: Volcanic degassing ; trace elements ; environmental impact of volcanic activity ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 04. Solid Earth::04.08. Volcanology::04.08.08. Volcanic risk
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
    Type: Oral presentation
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  • 53
    Publication Date: 2017-04-04
    Description: Volcanic emissions represent one of the most relevant natural sources of trace elements to the troposphere, both during and between eruptions. Due to their potential toxicity they may have important environmental impacts from the local to the global scale. Mount Etna, the largest European volcano and one of the most active volcano in the world, covers an area of about 1250 km2 and reaches an altitude of about 3340 m. It has been persistently active during historical time, with frequent paroxysmal episodes separated by passive degassing periods. Atmospheric precipitation was collected approximately every two weeks, from April 2006 to December 2007, using a network of five rain gauges, located at various altitudes on the upper flanks around the summit craters of Etna Volcano. The collected samples were analysed for major (Ca, Mg, K, Na, F, SO4, Cl, NO3) and a large suite of trace elements (Ag, Al, As, Au, B, Ba, Be, Bi, Cd, Co, Cr, Cs, Cu, Fe, Hg, La, Li, Mn, Mo, Ni, Pb, Rb, Si, Sb, Sc, Se, Sr, Th, Ti, Tl, U, V, Zn) by using different techniques (IC, SPEC, ICP-MS and CV-AFS). The monitoring of atmospheric deposition gave the opportunity to occasionally sample volcanic fresh ashes emitted by the volcano during the paroxysmal events. This was possible because the network of five rain gauges were equipped with a filter-system to block the coarse material. In this way, more than twenty events of ashfall were collected. Unfortunately, only half of these samples were suitable for a complete chemical analysis, because of the small amount of sample. In order to obtain elemental chemical composition of ashes, powdered samples were analysed by a combination of methods, including X-ray Fluorescence Spectroscopy (XRF), total digestion followed by Inductively Coupled Plasma Emission Mass Spectrometry (ICP-MS), Instrumental Neutron Activation Analysis (INAA), and infrared detection (IR). The chemistry of rainwater reveals that most of the investigated elements have higher concentrations close to the emission vent of the volcano, confirming the prevailing volcanic contribution. Rainwater composition clearly reflects the volcanic plume input. Ash-normalised rainwater composition indicates a contrasting behaviour between volatile elements, which are highly-enriched in rainwater, and refractory elements, which have low rainwater/ash concentration ratios. The degree of interaction between collected ash and rainwater was variable, depending on several factors: (i) the length of the period in which tephra was present in the sampler (the ash fall may have occurred any day from the first to the last day of the rain collecting period); (ii) the amount of rainwater fallen on the collectors after the ash-fall event, and its acidity; (iii) the granulometry of the ash samples that was widely variable (from few centimetres to micrometric particles) increasing the interaction with decreasing dimensions of the grains; (iv) the distance of collector with respect to the craters. In order to investigate the role of volcanic ash on the evolution of the rainwater chemistry, absolute concentrations of rain and ash were plotted in binary plot diagrams (Figure 1). Each diagram corresponds to a single event, and pH and TDS of the solution collected is reported. The diagonal bars in the diagrams represent the rain/ash ratios (1:1 and 1:10000). The results confirm that sulphate and halide salt aerosols are adsorbed onto ash particles, and their rate of dissolution in rainwater depends on solubility. Moreover, rapid chemical weathering of the silicate glass by volcanic acid (SO2, HCl and HF) can also explain the enrichment of several refractory elements (Na, K, Ca, Mg, Si, Al, Fe, Ti, Sc). Our observations highlight how explosive activity can increase enormously the deposition rate of several chemical elements, up to several km away from the emission vents.
    Description: Published
    Description: Nicolosi (Catania)
    Description: 1.2. TTC - Sorveglianza geochimica delle aree vulcaniche attive
    Description: open
    Keywords: volcanic ash ; trace elements ; environmental impact of volcanic activity ; rainwater chemistry ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases ; 04. Solid Earth::04.08. Volcanology::04.08.08. Volcanic risk
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 54
    Publication Date: 2019-11-04
    Description: Volcanic eruptions are unsteady multiphase phenomena, which encompass many inter-related processes across the whole range of scales from molecular and microscopic to macroscopic, synoptic and global. We provide an overview of recent advances in numerical modelling of volcanic effects, from conduit and eruption column processes to those on the Earth s climate. Conduit flow models examine ascent dynamics and multiphase processes like fragmentation, chemical reactions and mass transfer below the Earth surface. Other models simulate atmospheric dispersal of the erupted gas-particle mixture, focusing on rapid processes occurring in the jet, the lower convective regions, and pyroclastic density currents. The ascending eruption column and intrusive gravity current generated by it, as well as sedimentation and ash dispersal from those flows in the immediate environment of the volcano are examined with modular and generic models. These apply simplifications to the equations describing the system depending on the specific focus of scrutiny. The atmospheric dispersion of volcanic clouds is simulated by ash tracking models. These are inadequate for the first hours of spreading in many cases but focus on long-range prediction of ash location to prevent hazardous aircraft - ash encounters. The climate impact is investigated with global models. All processes and effects of explosive eruptions cannot be simulated by a single model, due to the complexity and hugely contrasting spatial and temporal scales involved. There is now the opportunity to establish a closer integration between different models and to develop the first comprehensive description of explosive eruptions and of their effects on the ground, in the atmosphere, and on the global climate.
    Description: Published
    Description: JCR Journal
    Description: open
    Keywords: numerical modeling ; explosive volcanic eruptions ; conduit flow ; multiphase flow simulation ; stratospheric sulfate aerosol ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects ; 04. Solid Earth::04.08. Volcanology::04.08.99. General or miscellaneous ; 04. Solid Earth::04.08. Volcanology::04.08.01. Gases
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  • 55
    Publication Date: 2017-04-04
    Description: Natural precipitation and water samples from passive devices were collected at Mt. Vesuvius and Vulcano Island, Italy, during the period 2004–2006, in order to investigate its possible interactions with fumarolic gases. Evidence of chemical reactions between fumarolic fluids and rain samples before and after its deposition into the sampling devices was found at Vulcano Island. Very low pH values (down to 2.5) and significant amounts of chlorine and sulfate (up to 22 mEq/l) were measured at sampling points located close to the fumarolic field. In contrast, anthropogenic contributions and/or dissolution of aerosols (both maritime and continental) influence the chemistry of rainwaters at Mt. Vesuvius, which show inter-annual variations that are highly consistent with those recorded at the coastal site at Vulcano Island. Chemistry of waters directly exposed to fumarolic fluids may then give useful information about its temporal evolution, holding the signal of the ‘‘maximum’’ chemical event occurred in the meanwhile. In addition, the observation of the health status of vegetation colonizing the immediate surroundings of the fumarolic fields, due to its strong dependence on the interactions with these fluids, may work as a possible biomarker of volcanic activity.
    Description: Published
    Description: 159-171
    Description: 1.2. TTC - Sorveglianza geochimica delle aree vulcaniche attive
    Description: JCR Journal
    Description: restricted
    Keywords: Precipitation ; Fumarole ; Vesuvius ; Vulcano ; 01. Atmosphere::01.01. Atmosphere::01.01.07. Volcanic effects
    Repository Name: Istituto Nazionale di Geofisica e Vulcanologia (INGV)
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  • 56
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    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.
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  • 57
    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.
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  • 58
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    European journal of nutrition 24 (1985), S. 113-119 
    ISSN: 1436-6215
    Keywords: Chloramphenicol ; pharmacokinetics ; residue ; pig
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition , Medicine
    Description / Table of Contents: Summary Residues of Chloramphenicol (CAP) were examined in 24 pigs after intramuscular injection of 30 mg CAP/kg body weight. Two pigs were slaughtered after 3, 6, 12,18, 24, 36 hours, 2, 3, 6, 10, 21 and 30 days, respectively. CAP-concentrations were determined in muscle, blood, urine, liver, kidney, bile, and fat. Methods used were gas-liquid chromatography and radioimmunoassay. Detection limits reached were 1−5 ppb. The concentration-time curves obtained reflected a long elimination phase and allowed only calculation of this half-life. Elimination half-life was estimated to be for muscle, blood and urine 160–170 hours, for kidney 310 and for bile 250 hours. Significant correlations were found to exist between CAP-concentrations in plasma and muscle. It appears that blood would be a good body fluid for monitoring CAP-residues in tissue.
    Notes: Zusammenfassung Zur Untersuchung des Rückstandsverhaltens von Chloramphenicol (CAP) wurden 24 Mastschweine, 24–28 Wochen alt, intramuskulär mit 30 mg CAP/kg Körpergewicht behandelt und je 2 Tiere nach 3, 6, 12, 18, 24, 36 Stunden, 2, 3, 6, 10, 21 und 30 Tagen geschlachtet. Die CAP-Gehalte in Muskulatur, Blut, Urin, Leber, Niere, Galle und Fett wurden gaschromatographisch und radioimmunologisch bestimmt. Die Nachweisgrenze beider Methoden liegt in Abhängigkeit von der Matrix zwischen 1 und 5 ppb. Die erhaltenen Kinetiken weisen eine terminale Elimination auf, deren Halbwertszeiten für Muskulatur, Blut und Urin ca. 160–170 Stunden, für Niere 310 Stunden und für Galle 250 Stunden betragen. Die CAP-Konzentration in Muskulatur und Blut weisen eine signifikante, lineare Korrelation auf. Blutuntersuchungen könnten deshalb als Screening-Methode bei umfangreichen Rückstandskontrollen eingesetzt werden.
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  • 59
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    European journal of nutrition 22 (1983), S. 14-26 
    ISSN: 1436-6215
    Keywords: branched chain α-keto acids ; 4-methyl-2-oxopentanoate, 3-methyl-2-oxopentanoate ; 3-methyl-2-oxobutyrate ; dehydrogenation ; transamination ; pharmacokinetics ; absorption
    Source: Springer Online Journal Archives 1860-2000
    Topics: Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition , Medicine
    Description / Table of Contents: Zusammenfassung Michaelis-Konstanten und Aktivitäten von Dehydrogenasen und Transaminasen der drei verzweigten α-Ketosäuren Keto-Valin, Keto-Leucin und Keto-Isoleucin in Leber, Niere, Skeletmuskel und Gehirn von Ratten werden mitgeteilt. Nach oraler Zufuhr passieren nur 11–22% der Ketosäuren unverändert die Leber. Aus pharmakokinetischen und Resorptions-Untersuchungen erhaltene Blutspiegel an Ketosäuren werden zu den Michaelis-Konstanten in Beziehung gesetzt. Bei den geringen Konzentrationen an Ketosäuren nach oraler Zufuhr kann angenommen werden, daß die oxidativen Prozesse in den nichthepatischen Geweben über die Transaminierung überwiegen. Daten über die Wachstumseffizienz von verzweigtkettigen α-Ketosäuren im Vergleich zu den entsprechenden Aminosäuren stimmen mit dieser Vorstellung überein. Bei intravenöser Verabreichung müßten die Voraussetzungen für Transaminierung besser sein als nach oraler Zufuhr. Auf der Basis von Daten aus der Literatur werden die Übertragbarkeit unserer Befunde auf den Menschen und die verschiedenen Faktoren, welche die Effizienz der verzweigten α-Ketosäuren durch Einwirkung auf ihren Stoffwechsel beeinflussen können, diskutiert.
    Notes: Summary Miehaelis-constants and enzyme activities for dehydrogenation and transamination of the three branched chainα-keto acids in liver, kidney, skeletal muscle, and brain of rats are reported. After oral load only 11–22 % of the keto acids pass the liver unchanged. Blood levels in pharmacokinetic and absorption studies are related to the Michaelis-constants. At the low keto-acid concentrations after oral application, dehydrogenation in the non-hepatic tissues is supposed to prevail over transamination. Data on feed efficiency of branched chain α-keto acids reported in the literature support this view. The chance for transamination is better after intravenous administration. The transferability of our data to humans, and various factors influencing the efficiency of branched chain α-keto acids are discussed in connection with data reported in the literature.
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  • 60
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    Cellular and molecular life sciences 41 (1985), S. 1554-1557 
    ISSN: 1420-9071
    Keywords: Immunocytochemistry ; neuropeptide Y ; radioimmunoassay ; rat pancreas
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Significant quantities of a newly discovered peptide, neuropeptide Y, were found in the rat pancreas, where they were localized to nerves in the exocrine parenchyma and around arterial and ductal structures. Although unaffected by surgical parasympathectomy, the periarterial and periductal nerves were abolished by chemical sympathectomy, suggesting that NPY is partially costored with sympathetic transmitters in nerve fibers.
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  • 61
    ISSN: 1420-9071
    Keywords: Interferon ; immunomodulator ; catabolism ; pharmacokinetics ; administration routes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary When human recombinant interferon-α2 diluted in saline was injected s.c. into rabbits, the total amount recovered in thoracic lymph was less than 0.4%. Recoveries increased from 2- to 8-fold if interferon was injected in 4% albumin or with hyaluronidase, respectively. Albumin added to interferon acts as an interstitial fluid expander, thus favoring interferon absorption through lymphatics rather than blood capillaries. This strategy may increase the therapeutic index of interferon.
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  • 62
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    Calcified tissue international 12 (1973), S. 313-321 
    ISSN: 1432-0827
    Keywords: Cathepsin D ; Extracellular ; Ossification ; Immunocytochemistry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine , Physics
    Description / Table of Contents: Résumé De la cathepsine D extracellulaire d'origine principalement ostéoblastique a été démontrée par immunohistochimie dans le cartilage en voide de calcification de cultures d'os des membres d'embryons de poulet. L'intérêt de ce fait pour l'ossification est discuté.
    Abstract: Zusammenfassung Es wurde mit einer immunohistochemischen Methode gezeigt, daß extrazelluläres Kathepsin D, welches hauptsächlich aus Osteoblasten gewonnen wurde, Knorpel von kultivierten Knochen von Kükenembryonen mineralisiert. Die Bedeutung dieser Feststellung für den Mechanismus der Knochenbildung wird diskutiert.
    Notes: Abstract Extracellular cathepsin D derived mainly from osteoblasts has been demonstrated immunohistochemically in ossifying cartilage of cultured embryonic chick limb bones. The relevance of this observation to the mechanism of ossification is discussed.
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  • 63
    ISSN: 1432-1351
    Keywords: Photoreception ; Extraretinal Photoreceptor ; Chromophore ; Opsin ; Reptile ; Immunocytochemistry ; HPLC
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Since the beginning of this century evidence has accumulated which demonstrates that non-mammalian vertebrates possess photoreceptors situated deep within the brain. While many attempts have been made to localize these sensory cells, studies have either failed or been inconclusive. In this report we have used several experimental approaches to localize the deep brain photoreceptors of the lizard Anolis carolinensis. Using 3 antibodies that bind vertebrate cone opsins, we have immunolabelled cerebrospinal fluid (CSF)-contacting neurons located at the ventricular border within the nucleus ventromedialis of the septum. Western blot analysis indicates that these antibodies recognized a single 40 kD protein in ocular, anterior brain, and pineal extracts. Immunoblots of rodent brain did not show a similar protein band. We have also identified specific retinoids associated with phototransduction (11-cis and all-trans-3,4-didehydroretinaldehyde) within anterior brain extracts. This combined data provides the most detailed analysis of deep brain photoreceptors in any vertebrate. Consequently, we feel Anolis provides an excellent model to study this unexplored sensory system of the vertebrates.
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  • 64
    ISSN: 1432-1351
    Keywords: Egg laying hormone ; Aplysia ; Binding protein ; Immunocytochemistry ; Reproductive system
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract A protein solubilized from a membrane preparation of the gonad of Aplysia californica has been isolated by affinity chromatography, using bag cell egg-laying hormone (ELH) as the bound ligand, and partially purified and characterized by gel electrophoresis. The protein has an apparent molecular weight of 52 kDa and consists of two disulfide-linked subunits of about 30 kDa each. The protein is glycosylated and has an acidic pI. Approximately 10–15 μg of this protein can be isolated from a single ovotestis, representing less than 1% of the total protein in the gonad; but the protein could not be detected in buccal mass or body wall, tissues which do not have apparent response to ELH. Antibodies generated against this ELH-binding protein (ELHBP) were used to localize sites in the ovotestis which might contain this molecule and thus represent targets for egg-laying hormone. Immunocytochemical results indicate that the oocytes are a rich source of this protein, since their cytoplasm was the only detectable site of immunoreactivity. Whether this binding protein represents an egg-laying hormone receptor is uncertain, but its prevalence in oocytes suggests that ELH plays a signaling role on these gametes.
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  • 65
    ISSN: 1573-0832
    Keywords: ELISA ; Endodermis ; H. annosum ; Immunocytochemistry ; Root rot ; Vascular tissues
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract Vascular disintegration mainly of medulla rays of spruce roots is of major significance in root rot disease of spruce caused byH. annosum. Using seedling roots as an experimental model, the possible routes and initial host reactions preceding invasion of vascular tissues was investigated. Transmission electron microscopy showed that penetration through the endodermis was an obvious route but not without host resistance. Using antibodies againstH. annosum hyphal materials, some labelling of vascular tissues remote from sites of fungal colonization suggest the release of fungal secretory products partly active in tissue disintegration. Similarly, intense labelling was also observed in severely colonized host tissues at late stages of infection. Strong labelling recorded at 3 d p.i. mainly on fungal hyphae and scant gold particles on invaded host tissues could imply that induction of host antifungal metabolites may have been a late event. A correlation was found between total antigenic material in root homogenates measured by ELISA, density of tissue labelling by immunocytochemistry and severity of disease symptoms. The importance of this in relation to diagnosis of biotic root rot diseases in the field is discussed.
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  • 66
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    Mycopathologia 125 (1994), S. 107-117 
    ISSN: 1573-0832
    Keywords: Aflatoxin B1 ; Immunocytochemistry ; Regeneration ; Tissue culture ; Tobacco plantlets
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Abstract The effects of aflatoxin B1, (0.5–25 µg ml−1) on in vitro root and shoot development in young tobacco explants were investigated. Despite an initial apparent stimulatory effect on most measured parameters at 0.5 µg ml−1 AFB1, the number of leaves, root and leaf mass per plantlet were progressively inhibited with increasing AFB1 concentration. The number of explants developing roots was reduced to 34% at the highest (25 µg ml−1) AFB1 concentration, following 3 weeks exposure to the toxin. Leaf chlorophyll content at this toxin concentration was significantly lower than that measured for control plantlets. Thin layer chromatography confirmed the absorption of AFB1 by the plantlets. Using immunocytochemical techniques, AFB1 was immunolocated predominantly in the vacuoles, the nucleus and the cytoplasm (possibly intravesicularly). The results are discussed in terms of this immunolocation within the cell.
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  • 67
    ISSN: 1432-041X
    Keywords: Vitellin ; Yolk granule ; Yolk protein ; Silkworm ; Embryogenesis ; Immunocytochemistry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary Vitellin was purified from eggs of the silkworm,Bombyx mori, by a new method in which vitellin was extracted from isolated yolk granules. The purified vitellin had a molecular weight of 540,000. An antibody against purified vitellin was prepared in rabbits. It reacted with the hemolymph vitellogenin as well as with purified vitellin, but not with other proteins in the hemolymph or in the extract from yolk granules. The anti-vitellin IgG was used to immunocytochemically locate vitellin in theBombyx non-diapause egg during early developmental stages. In the egg, just after oviposition, vitellin was located in internal yolk granules and in small yolk granules of the periplasm. During the early developmental stages studied, vitellin was not metabolized uniformly throughout the egg. The vitellin of the internal yolk granules located at the posterior-dorsal part and of the small peripheral yolk granules was utilized in 16 h and 2 days, respectively, after oviposition. A thin, very vitellin-poor layer was located between the periplasm and the vitellin-rich interior in the newly laid egg. it was always in close contact with the periphery where blastoderm and germ-band cells developed.
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  • 68
    ISSN: 1432-041X
    Keywords: Major haemolymph proteins ; Development ; Cuticle ; Immunocytochemistry ; Ceratitis capitata
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary The developmental profile of the major haemolymph proteins (ceratitins) inCeratitis capitata was studied. Ceratitin concentration in the haemolymph decreases dramatically during the last days of pupal life, while the amounts of ceratitins in whole organism extracts remain unchanged. By electrophoretic, immunological and immunofluorescence techniques it was revealed that ceratitins are reabsorbed by the fat body and a fraction of them is deposited in the cuticle. The possible role of ceratitins is discussed.
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  • 69
    ISSN: 1432-041X
    Keywords: Sea urchin ; Jelly coat ; Accessory cell ; Oogenesis ; Immunocytochemistry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary The immunocytochemical localization of the egg-jelly macromolecule, a fucose sulphate glycoconjugate (FSG) that induces the acrosome reaction in spermatozoa, was investigated in ovaries of the sea urchin Hemicentrotus pulcherrimus by use of a polyclonal antibody. The polyclonal antibody reacted with the accessory cells and oocytes in the ovarian lumen. In the accessory cells, evidence of an intense immunohistochemical reaction was observed in many globules of variable density. Products of the specific immunohistochemical reaction were frequently observed in the surface region of oocytes, at a distance from the ovarian wall. At the ultrastructural level, the polyclonal antibody was found to react with the material present in the vacuole-like structures of the globules in the accessory cells. Many gold particles, demonstrating specific immunolabelling, were associated with well-developed microvilli on the vitellogenic oocytes. In the mature oocytes, intense labelling was observed in the jelly coat but not in the vitelline coat. By contrast, oogonia and early oocytes were barely labelled. Quantitative data indicated that the extent of immunolabellings in the surface region of oocytes was very high in the vitellogenic and mature oocytes. In all cases, neither the oocyte cytoplasm nor the subcellular organelles were labelled. These results suggest that FSG is produced by the accessory cells and is deposited initially on the surface of vitellogenic oocytes for the formation of jelly. These findings may provide a new insight into the role of the accessory cells in the reproductive process of the sea urchin.
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  • 70
    ISSN: 1432-041X
    Keywords: Sea urchin ; Egg jelly ; Ovary ; Development ; Immunocytochemistry
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract In the sea urchin Hemicentrotus pulcherrimus, the egg-jelly macromolecule, a fucose sulphate glycoconjugate (FSG) that induces the acrosome reaction in spermatozoa, originates from the accessory cells in the ovary. In the present study we examined the seasonal variations in the distribution of FSG in the ovary by immunocytochemistry with a polyclonal antibody. An enzyme-linked immunosorbent assay indicated that FSG was present in supernatants of extracts of ovaries throughout the development of the ovary. However, the immunohistochemical study showed that there are marked seasonal changes in the distribution of FSG in ovaries. The polyclonal antibody reacted strongly with globules of accessory cells before the beginning of the breeding season (August to December). During the breeding season (February to April), the immunohistochemical reaction was found on the surface of oocytes but was weak in the accessory cells. At the ultrastructural level, the antibody reacted with globules of variable density in accessory cells. Intense immunolabelling was observed in the vacuole-like structures of the globules. Sometimes, products of the specific immunocytochemical reaction were found in the Golgi apparatus in these globules. Quantitative examination indicated that FSG was actively produced by the accessory cells from the late non-breeding season to the pre-breeding season. These results suggest that there are marked seasonal variations in the production of FSG by the accessory cells in the sea urchin ovary. These findings also provide new evidence that accessory cells exhibit dynamic changes during the reproductive process in the sea urchin.
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  • 71
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    Cellular and molecular life sciences 41 (1985), S. 1340-1342 
    ISSN: 1420-9071
    Keywords: Immunocytochemistry ; calmodulin ; secretory granules
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Medicine
    Notes: Summary Calmodulin is a regulator of several calcium-dependent cellular processes. It has been suggested that it plays a role in the mechanism of secretion. Employing an indirect immunoperoxidase technique at the light microscope level, this study demonstrates the presence of calmodulin in several exocytotic cells (mast cells, thyroid follicular cells, neurohypophyseal neurosecretory terminals, pancreaticβ-cells and pancreatic acinus cells) in rat and man. The positive staining reaction for calmodulin was granular and at least in the case of rat mast cells it appeared to be associated with the granule membrane.
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  • 72
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    Trees 13 (1999), S. 138-151 
    ISSN: 0931-1890
    Keywords: Key words Cytoskeleton ; Immunocytochemistry ; Model systems ; Populus ; Secondary vascular system
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology , Agriculture, Forestry, Horticulture, Fishery, Domestic Science, Nutrition
    Notes: Abstract  Trees represent a, probably the, major component of the biosphere and have a unique place in the history of Mankind. One of their most fascinating features is the process of secondary growth which is effected principally by the secondary vascular system, the developmental continuum of secondary phloem, vascular cambium, and secondary xylem. However, for too long assumptions about the developmental biology of trees have had to be based upon studies of primary growth systems within annual, herbaceous species because study of the secondary vascular system had been largely ignored. Even when attempts are made to understand some of the most fundamental features of the secondary vascular system, such as xylogenesis, the current model system, isolated Zinnia mesophyll cells, is not entirely appropriate to the situation in the intact tree. Some deficiencies of the Zinnia system are discussed, and the advantages of the genus Populus as a model for study of the hardwood secondary vascular system are considered. Some of the new approaches which are poised to lead to significant advances in our knowledge of the cell bio-logy of the secondary vascular system of trees – spe-cifically of the cell wall, the plasmalemma, and the cytoskeleton – are discussed. The value of one of these new techniques – immunocytochemistry – is demonstrated by a consideration of recent work on the role of the cytoskeleton in the hardwood secondary vascular system.
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  • 73
    ISSN: 1432-0827
    Keywords: Androgen Receptor ; Osteoclast ; Mouse ; Immunocytochemistry
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    Topics: Biology , Medicine , Physics
    Notes: Summary Expression of androgen receptor (AR) in mouse osteoclast-like multi-nucleated cells (OCs) was examined with immunocytochemical techniques. Murine OCs were obtained by co-culturing mouse osteoblastic cells and bone marrow cells. Three preparations of polyclonal anti-AR antibody which were raised in rabbit against different parts of the human AR were employed for the experiments. Specific staining for AR was demonstrated in the nuclei and the perinuclear area of mouse OCs. This is the first report demonstrating the presence of AR in osteoclast-like cells.
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  • 74
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    Calcified tissue international 24 (1977), S. 223-229 
    ISSN: 1432-0827
    Keywords: Enamel-cementum-morphology ; Immunocytochemistry ; Biochemistry
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    Topics: Biology , Medicine , Physics
    Notes: Summary The continuously erupting rabbit incisor tooth is normally thought of as having an enamel covered “crown” on its labial surface and a cementum covered “root” on its lingual surface. We have examined both surfaces of continuously erupting rabbit incisor teeth taken from near term embryos by a variety of means, including transmission and scanning electron microscopy, biochemical fractionation, and immunohistochemistry. In all cases, we could detect no qualitative difference in the early extracellular matrices taken from the labial and lingual surfaces of the teeth. Both matrices were shown to be composed of dentin and enamel, although the thickness and geometry of the enamel matrix on the lingual surface was somewhat different from that on the labial surface.
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  • 75
    ISSN: 1432-0827
    Keywords: Growth hormone ; Growth hormone receptor ; Odontogenesis ; Bone remodeling ; Immunocytochemistry
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    Topics: Biology , Medicine , Physics
    Notes: Summary Growth hormone (GH) may regulate tooth formation and bone remodeling associated with tooth eruption. This study reports the distribution of growth hormone receptor/binding protein in developing rat molars and adjacent alveolar bone by immunocytochemistry using well-characterized anti-growth hormone receptor monoclonal antibodies. These tissues represent an excellent model for studying the ontogenic changes that occur in odontogenic and osteogenic cells, as these cells are found in linear arrays displaying the various stages of morphological and functional differention, and differentiated function. Immunoreactivity was first seen in precementoblasts in contact with the epithelial root sheath, and preodontoblasts. However, growth hormone receptor immunoreactivity was associated primarily with the cytoplasm of odontogenic and osteogenic cells forming their respective matrices. Thus, cementoblasts and odontoblasts at sites of new matrix formation showed intense immunoreactivity whereas cementocytes and mature odontoblasts at later stages of tooth development were nonreactive. Osteoblasts engaged in intramembranous ossification in the alveolar bone were positive, although osteocytes and endosteal cells were immunonegative. Osteoclasts at sites of alveolar bone remodeling resorption were also immunopositive. These patterns of receptor expression parallel the ontogenic sequences of odontogenic and osteogenic cells and suggest that GH promotes the functional state of these cells. Our results also imply that GH may influence differentiation or differentiated functions associated with odontogenesis, osteogenesis, and bone remodeling independent of systemic insulin-like GF-I.
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  • 76
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    Histochemistry and cell biology 106 (1996), S. 9-17 
    ISSN: 1432-119X
    Keywords: Silver enhancement ; Immunogold-silver staining ; Immunocytochemistry
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    Topics: Biology , Medicine
    Notes: Abstract The immunogold silver staining method (IGSS) is widely used as a sensitive and specific immunohistochemical visualisation technique. IGSS involves the specific deposition of metallic silver at the site of immunogold labelling and provides a means of visualisation at low magnification by light or electron microscopy. Silver developers for IGSS rapidly deposit metallic silver only at the site of heavy metals, including gold and silver, because of their catalytic activity. The developing solution contains the silver ions and reducing agent necessary for this reaction. Using different silver salts as ion donors and by selecting an appropriate temperature and pH, visible amounts of silver can be deposited in a few minutes at the site of colloidal gold labelling while little non-specific background deposition occurs. Inclusion of protective colloids in the solution can also be used to control the reaction. Although studies of the chemical basis of silver deposition around unlabelled colloidal gold date back to 1939, immunogold enhancement by silver was established in 1983. The IGSS method evolved from the combination of disparate photographic, histochemical and immunogold techniques which have been effectively combined and optimised over the last 10 years to provide a visualisation system which is well suited to many immunohistochemical studies.
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    Histochemistry and cell biology 106 (1996), S. 9-17 
    ISSN: 1432-119X
    Keywords: Key words Silver enhancement ; Immunogold-silver staining ; Immunocytochemistry
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    Topics: Biology , Medicine
    Notes: Abstract  The immunogold silver staining method (IGSS) is widely used as a sensitive and specific immunohistochemical visualisation technique. IGSS involves the specific deposition of metallic silver at the site of immunogold labelling and provides a means of visualisation at low magnification by light or electron microscopy. Silver developers for IGSS rapidly deposit metallic silver only at the site of heavy metals, including gold and silver, because of their catalytic activity. The developing solution contains the silver ions and reducing agent necessary for this reaction. Using different silver salts as ion donors and by selecting an appropriate temperature and pH, visible amounts of silver can be deposited in a few minutes at the site of colloidal gold labelling while little non-specific background deposition occurs. Inclusion of protective colloids in the solution can also be used to control the reaction. Although studies of the chemical basis of silver deposition around unlabelled colloidal gold date back to 1939, immunogold enhancement by silver was established in 1983. The IGSS method evolved from the combination of disparate photographic, histochemical and immunogold techniques which have been effectively combined and optimised over the last 10 years to provide a visualisation system which is well suited to many immunohistochemical studies.
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  • 78
    ISSN: 1432-2048
    Keywords: Immunocytochemistry ; Lectin (localization) ; Phaseolus (lectin) ; Phytohemagglutinin ; Seed (lectin)
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    Topics: Biology
    Notes: Abstract We have examined the properties and subcellular localization of phytohemagglutinin (PHA), the major lectin of the common bean (Phaseolus vulgaris.), in the axis cells of nearly mature and imbibed mature seeds. On a protein basis the axis contained about 15% as much PHA as the cotyledons. Localization of PHA was done with an indirect immunolabeling method (rabbit antibodies against PHA, followed by colloidal gold particles coated with goat antibodies against rabbit immunoglobulins) on ultra-thin cryosections which were embedded in plastic on the grids after the immunolabeling procedure. The embedding greatly improved the visualization of the subcellular structures. The small (4 nm) collodial gold particles, localized with the electron microscope, were found exclusively over small vacuoles or protein bodies in all the cell types examined (cortical parenchyma cells, vascular-bundle cells, epidermal cells). The matrix of these vacuoles-protein bodies appears considerably less dense than that of the protein bodies in the cotyledons, but the results confirm that in all parts of the embryo PHA is localized in similar structures.
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  • 79
    ISSN: 1432-2048
    Keywords: Glycine (xanthine dehydrogenase) ; Immunocytochemistry ; Polyclonal antibody ; Root nodule ; Xanthine dehydrogenase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract Xanthine dehydrogenase (XDH, EC 1.2.1.37) was purified from root nodules of soybean (Glycine max) and used to prepare a polyclonal rabbit antiserum. Monospecificity of this antiserum was ascertained by sodium dodecyl sulfate-polyacrylamide gel electrophoresis of the immunoprecipate. During root nodule development of soybean, only one form of XDH was detected on an immunological basis. Titration of XDH by immunoelectrophoresis showed that a remarkable increase in the amount of XDH occurred between two and four weeks after inoculation, in parallel with the increase in enzyme activity. Localization of XDH by immunofluorescence indicated that the enzyme was present exclusively in uninfected cells where it appeared to be associated with discrete organellels
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  • 80
    ISSN: 1432-2048
    Keywords: Avena ; Immunocytochemistry ; Phytochrome
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    Topics: Biology
    Notes: Abstract Phytochrome of oat (Avena sativa L., cv. Garry) coleoptile cells in the red-light-absorbing form, Pr, is diffusely distributed while after conversion to the far-red-light-absorbing form, Pfr, it is observed only in very small areas within the cell. Comparison of phytochrome photoversibility measurements to the distribution of the pigment within the cell indicates that the spectral assay is not influenced by the observed compartmentalization of the chromoprotein. However, the observed compartmentalization of phytochrome is correlated with a loss in spectrophotometrically detectable Pr.
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  • 81
    ISSN: 1432-2048
    Keywords: Cotyledons ; Endoplasmic reticulum ; Ferritin labeling ; Immunocytochemistry ; Phaseolus ; Protein (reserve) ; Reserve protein
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Abstract The ultrastructure of the storage parenchyma cells of the cotyledons of developing bean (Phaseolus vulgaris L.) seeds was examined in ultrathin frozen sections of specimens fixed in a mixture of glutaraldehyde, formaldehyde and acrolein, infused with 1 M sucrose, and sectioned at-80° C. Ultrastructural preservation was excellent and the various subcellular organelles could readily be identified in sections which had been stained with uranyl acetate and embedded in Carbowax and methylcellulose. The cells contained large protein bodies, numerous long endoplasmic reticulum cisternae, mitochondria, dictyosomes, and electron-dense vesicles ranging in size from 0.2 to 1.0 μm. Indirect immunolabelling using rabbit immunoglobulin G against purified phaseolin (7S reserve protein), and ferritin-conjugated goat immunoglobulin G against rabbit immunoglobulin G was used to localize phaseolin. With a concentration of 0.1 mg/ml of anti-phaseolin immunoglobin G, heavy labeling with ferritin particles was observed ober the protein bodies, the cisternae of the endoplasmic reticulum, and the vesicles. The same structures were lightly labeled when the concentration of the primary antigen was 0.02 mg/ml. Ferritin particles were also found over the Golgi bodies. The absence of ferritin particles from other organelles such as mitochondria and from areas of cytoplasm devoid of organelles indicated the specificity of the staining, especially at the lower concentration of anti-phaseolin immunoglobulin G.
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  • 82
    ISSN: 1432-2048
    Keywords: Immunocytochemistry ; (PEP carboxylase) ; PEP carboxylase ; Sorghum
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    Topics: Biology
    Notes: Abstract The localization of phosphoenol pyruvate carboxylase (EC 4.1.1.3.1.) in the leaf cells of Sorghum vulgare was investigated by using three techniques: the conventional aqueous and non aqueous methods gave conflicting results; the immunocytochemical techniques clearly showed that the enzyme is predominantly located in the cytoplasm of mesophyll cells.
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  • 83
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    Sexual plant reproduction 5 (1992), S. 89-100 
    ISSN: 1432-2145
    Keywords: Actin ; Cytoskeleton ; Generative cell ; Immunocytochemistry ; Microtubule ; Mitosis ; Phragmoplast ; Pollen ; Rhodamine phalloidin ; Sperm
    Source: Springer Online Journal Archives 1860-2000
    Topics: Biology
    Notes: Summary Disagreement has arisen over the presence of actin-containing microfilaments (Mfs) in angiosperm generative cells and sperm (GSP). In order to address this issue, we subjected GSP of Tradescantia virginiana, Nicotiana tabacum and Rhododendron laetum to a series of localizations using different antiactins, rhodamine phalloidin and antimyosin. Coordinate staining with antitubulin and Hoechst 33258 defined the status of the microtubule (Mt) cytoskeleton and stages of generative cell division. Additional experiments utilized cytochalasin D (CD). In no instance could Mfs be detected in GSP of the three species. Instead, Mfs seen at the periphery of GSP appear to be continuous with vegetative Mfs and thus are in the vegetative cytoplasm. Mfs are not seen in the constriction zone of dividing T. virginiana generative cells, nor are they indicated in the phragmoplast of N. tabacum and R. laetum. Myosin localizations reveal punctate staining in the vegetative cytoplasm and a thin line of fluorescence around the the outside of the generative cell. While CD seems to delay generative cell division, cytokinesis still takes place. CD-induced Mf fragments are evident in the vegetative cytoplasm but not in GSP. The weight of evidence therefore indicates that GSP do not contain Mfs. The implications of this conclusion for the behavior of GSP and the mechanism of cytokinesis in dividing generative cells are considerable.
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  • 84
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    European journal of clinical pharmacology 32 (1987), S. 631-634 
    ISSN: 1432-1041
    Keywords: salbutamol ; albuterol ; pharmacokinetics ; bioavailability ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Salbutamol was administered to sixteen healthy male volunteers intravenously and by mouth in liquid, tablet, and capsule form using a Latin-Squares design. Pharmacokinetic parameters from intravenous data were similar to previously reported values obtained with oral administration, with a mean terminal half-life of 3.8 h and a mean clearance of 439 ml·min−1·1.73 m−2. Peak plasma concentrations of 10–20 ng·ml−1 were obtained 1–3 h following oral administration. The absolute bioavailability of each of the oral preparations was 44%. While statistically significant differences in lag time and time to peak concentration were noted among the various oral preparations, the drug is rapidly absorbed in all three dosage forms and the observed differences are unlikely to be of clinical significance.
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    European journal of clinical pharmacology 42 (1992), S. 101-105 
    ISSN: 1432-1041
    Keywords: Rufloxacin ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The plasma and urine kinetics of rufloxacin were assessed in healthy volunteers after single (100, 200, 400 and 800 mg) and multiple (300 mg followed by 150 mg daily, Group 1, and 400 mg followed by 200 mg daily, Group 2) oral doses. The kinetics of a single oral dose of 800 mg was assessed in fasting and non-fasting subjects to assess the influence of food intake on drug absorption. The AUCs were 134, 266 and 375 μg · h · ml−1 after 100, 200 and 400 mg, respectively. The AUC after 800 mg p. o. was 715 μg · h · ml −1 in fasting subjects and 614 μg · h · ml−1 in non-fasting subjects. The parameters of the model and the mean renal clearance values indicated some departure from linearity in rufloxacin kinetics. After multiple doses the plasma drug levels during the 6th treatment day were similar to those after the first dose in Group 1 and were about 30–40% higher after the first dose in Group 2. The half-lives after the last dose were much shorter than those estimated in the single dose studies (33–36 h and 50–80 h, respectively).
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    European journal of clinical pharmacology 42 (1992), S. 535-538 
    ISSN: 1432-1041
    Keywords: Meropenem ; Carbapenem ; pharmacokinetics ; uraemia ; haemodialysis
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of IV meropenem (500 mg over 30 min) has been studied in 6 healthy volunteers and 26 patients with various degrees of renal impairment. Blood samples were taken at different times over 24 h in healthy subjects and 36 to 48 h in uraemic patients, and four or five urine samples were collected over 24 or 48 h. Meropenem concentrations in plasma and urine were measured by a microbiological assay. The mean peak plasma concentration of meropenem ranged from 28 to 40 μg·ml−1 and was not affected by the degree of renal impairment. The terminal half-life of meropenem was approximately 1 h in subjects with normal kidney function and it was proportionately increased as renal function decreased. A significant linear relationship between total body clearance and creatinine clearance as well as between renal clearance and creatinine clearance was observed. The mean apparent volume of distribution at steady state was not significantly altered in uraemic patients. The mean cumulative urinary recovery of meropenem in healthy volunteers was 77% of the administered dose and it was significantly decreased in patients with renal impairment. Haemodialysis shortened the elimination half-life, from 9.7 h during the predialysis period to 1.4 h during the dialysis period. The dose of meropenem should be reduced in relation to the decrease in creatinine clearance.
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  • 87
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    European journal of clinical pharmacology 34 (1988), S. 179-186 
    ISSN: 1432-1041
    Keywords: ceftazidime ; pharmacokinetics ; elderly patients ; young volunteers ; acute infection
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of ceftazidime have been investigated after single and multiple i.v. doses in 9 young healthy male volunteers and 15 elderly male patients with acute bacterial infections. All subjects had normal, age-correlated glomerular function. Distribution and elimination in young volunteers were unaffected by posture and were similar to what has been reported earlier. In contrast, elderly patients had longer t1/2β (3.1 vs 1.9 h), larger AUC (414.0 vs 276.6 h·mg/l), lower total and renal clearances, reduced urinary recovery over 12 h and enlarged Vss. Total serum clearance of ceftazidime was closely correlated with the51Cr-EDTA clearance. There was no significant change in51Cr-EDTA clearance after seven days of treatment. A reduction in the dose of betalactam antibiotics eliminated by the kidney is advisable in elderly patients with an acute bacterial infection.
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    European journal of clinical pharmacology 42 (1992), S. 559-560 
    ISSN: 1432-1041
    Keywords: Mefloquine ; Thai subjects ; pharmacokinetics ; Primaquine ; drug interaction ; adverse effects
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    Topics: Chemistry and Pharmacology , Medicine
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  • 89
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    European journal of clinical pharmacology 39 (1990), S. 395-397 
    ISSN: 1432-1041
    Keywords: atropine ; exercise ; pharmacokinetics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Seven healthy males (19–32 y) underwent each of four separate conditions in a repeated measures design. Five of these subjects underwent an additional trial. In four of five trials subjects received 2.0 mg atropine sulfate intramuscularly in the anterolateral portion of the left thigh: at rest (T1); following completion of a single exercise (Ex) bout (T2), (Each bout consisted of 25 min of stationary cycling at 40% VO2 max with 5 min of seated rest), prior to three Ex bouts (T3) and following one and prior to three Ex bouts (T5). Trial 4 (T4) was the same as T3 with the substitution of a saline placebo. Serum samples were collected over a 12 h period and atropine concentration was determined by RIA. Ex trials were compared to T1. Ex prior to atropine (T2) significantly decreased the mean volume of distribution (Vz, 278 vs 2321). Ex in T3 significantly decreased the serum half life (t1/2, 4.2 vs 3.5 h), Vz (278 vs 1981), and clearance (CL, 763 vs 638 ml·min−1) and significantly increased the peak concentration (Cp, 6.7 vs 12.3 ng·ml−1) and area under the curve (AUC, 44.1 vs 53.1 ng·ml−1). In T5, Ex significantly decreased the t1/2 (3.4 h), Vz (182 l) and CL (575 ml·min−1) and significantly increased the absorption rate constant (ka, 0.482 vs 1.1 min−1), elimination rate constant (ke, 0.0012 vs 0.0015 min−1), Cp (14 ng·ml−1) and AUC (53.3 ng·h·ml−1). These results demonstrate that moderate Ex either prior to and/or immediately following drug administration has the capacity to significantly modify atropine pharmacokinetics.
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  • 90
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    European journal of clinical pharmacology 42 (1992), S. 689-691 
    ISSN: 1432-1041
    Keywords: Diphemanil methylsulphate ; pharmacokinetics ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetic parameters of oral diphemanil methylsulphate have been evaluated in six healthy male volunteers. Absorption of the drug was slow (tmax=2 to 4 h), the mean half-life was 8.35 h, and the amount of the drug recovered in urine within 48 h ranged from 0.6 to 7.4% of the administered dose. The results suggest low bioavailability, assuming that the drug is poorly metabolized.
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  • 91
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    European journal of clinical pharmacology 42 (1992), S. 693-694 
    ISSN: 1432-1041
    Keywords: Loperamide ; loperamide oxide ; diarrhoea ; pharmacokinetics ; dose-proportionality
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of loperamide, after oral administration of increasing doses (1 to 16 mg) of loperamide oxide, has been investigated in 10 healthy male volunteers, using a randomised cross-over design. Comparison of the maximum plasma loperamide concentration and AUC demonstrated that the bioavailability of loperamide was proportional to the dose of loperamide oxide administered.
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  • 92
    ISSN: 1432-1041
    Keywords: Alpidem ; Anxiolytics ; pharmacokinetics ; tolerance ; metabolites ; sedation ; adverse events
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary In a double-blind, placebo-controlled, crossover experiment in 21 healthy male volunteers, aged 19 to 27 y, the pharmacokinetics and tolerance of the new anxiolytic drug alpidem (SL80.0342) and its three major metabolites were studied after single doses of 25, 50, 100 and 200 mg. Plasma concentrations of alpidem (in 20 subjects) and metabolites (in 6 subjects) were measured by HPLC over a period of 54 h after dosing. Cmax, tmax and AUC(0–54) and, when possible, t1/2 were determined for alpidem and metabolites and the dose linearity of the parameters was investigated. The time to peak of alpidem was dose independent in most subjects and was short (1–4 h); the mean values at the four dosing levels were 1.9, 1.7, 1.6 and 1.8 h. The peak concentration increased with the dose, the mean values being 17, 34, 88 and 115 ng · ml−1, respectively. In 50% of the subjects cmax tended to stabilize between the 100 and 200 mg dose. Dose linearity was also present for the AUC, which plateaued between the 100 and 200 mg dose in only 3 out of 20 subjects; the mean AUC was 119, 281, 669 and 1117 ng · ml−1 · h, respectively. The apparent half-life of elimination appeared to be dose independent, mean values at the increasing dosing levels being 18.7, 19.9, 18,1 and 17.9 h. A similar relationship between the kinetics parameters and dose of the alpidem was observed for the metabolites SL83.0912, SL80.0522 and SL83.0725. The formation of metabolites was not saturated as their AUCs relative to corresponding alpidem AUCs were not dose related. Thus the kinetics of alpidem and its three major metabolites were linear after doses of 25 to 200 mg. The drug was well tolerated by most of the subjects. Sedation and dizziness occurred mainly after the 100 and 200 mg doses.
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  • 93
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    European journal of clinical pharmacology 43 (1992), S. 67-75 
    ISSN: 1432-1041
    Keywords: Morphine ; Patient-controlled analgesia ; opioids ; pharmacokinetics ; bolus-elimination-transfer ; computer-assisted continuous infusion
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Bone marrow transplant patients having severe, prolonged oral mucositis pain (expected to last for one to three weeks) used a computer-controlled infusion system to self-administer morphine for pain control. Individual patient pharmacokinetic information, derived from a pretreatment bolus morphine dose, was used in a new bolus-elimination transfer algorithm to produce rapid adjustments of steady plasma morphine concentrations when the patient requested more or less drug. We evaluated the performance characteristics (bias and precision) of this pharmacokinetically based patient-controlled analgesic infusion system (PKPCA) in a group of 15 cancer patients over six to 14 days. Although we found a three- to fivefold pharmaco-kinetic variability in the tailoring morphine dose data, the PKPCA system was free of systematic bias (insignificant overall prediction error) during the patient-controlled infusions in this study population. The absolute prediction error was 19.9% for the group on the first study day and 25.6% over the entire study period (aggregate results; 6–14 days of continuous use). Two-thirds of the patients exhibited no bias throughout the study period, and individual bias in the others was symmetrically distributed (three patients with underpredictions and two overpredicted). Magnitude of prediction error during the patient-controlled morphine infusions was not related to the magnitude of pharmacokinetic deviation of individual subjects from group parameters. Our results indicate that this PKPCA system provides accurate control of plasma morphine concentration when used by patients to self-administer opioid for prolonged pain relief continuously over 1 to 2 weeks. Use of individual pharmacokinetic information, instead of population parameters, may account for superior performance characteristic of this computer-assisted continuous drug infusion system.
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  • 94
    ISSN: 1432-1041
    Keywords: Indomethacin ; steady-state ; pharmacokinetics ; elderly
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The steady-state pharmacokinetic profile of indomethacin was examined in twelve healthy volunteers (4 m, 8 f; 20–34 y) and in 12 elderly subjects (7 m, 5 f; 70–88 y). Two formulations of indomethacin were examined, providing duplicate data for each subject group. The subjects received each formulation of indomethacin (25 mg tid) for 6 days in a single blind crossover fashion. On day 7, after an overnight fast, a final 25 mg dose of indomethacin was given and plasma concentrations measured over the following 12 h. Kinetic parameters Cpmin, tmx and AUC (0–12 h) were determined. There were no differences in the pharmacokinetic parameters between young and elderly subjects or between data for the two formulations of indomethacin. AUC values (μg · ml−1 · h), for example, for the two formulations in the young subjects were 5.85 and 6.85 while the values for the elderly subjects were 6.55 and 6.50 respectively. When each treatment period was considered independently there was a significant difference between young and elderly subjects with regard to compliance. The rates of non compliance (over and under compliance) using a capsule count technique were, however, low with a mean maximum value of 5.8% being recorded for the elderly subjects.
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    European journal of clinical pharmacology 41 (1991), S. 449-452 
    ISSN: 1432-1041
    Keywords: Diabetes mellitus ; Caffeine ; pharmacokinetics ; P-450 mono-oxygenase
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Diabetes may alter the pharmacokinetics of aminopyrine and antipyrine, which are used to assess liver function. Caffeine has recently been used to test liver function, but the effect of diabetes on caffeine kinetics is not known. The kinetics of caffeine has been examined in patients with decompensated Type I and Type II diabetes and in two age- and sex-matched control groups. In both types of diabetes the apparent caffeine clearance, half-life, and apparent volume of distribution were similar to controls. It is concluded that decompensated diabetes does not influence the cytochrome P-448 mono-oxygenase system responsible for caffeine metabolism.
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  • 96
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    European journal of clinical pharmacology 42 (1992), S. 231-233 
    ISSN: 1432-1041
    Keywords: Isradipine ; Haemodialysis ; pharmacokinetics ; dialysability
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics of isradipine, a calcium-channel blocker, have been studied in eight patients on chronic haemodialysis. A single oral dose of 5 mg was administered on both a non-haemodialysis and a haemodialysis day and the plasma concentrations of isradipine were analyzed. The mean cmax, tmax, AUC, and t1/2 in plasma on the non-haemodialysis day were 5.2 ng·ml−1, 1.4 h, 23.8 ng·h·ml−1, and 3.1 h, respectively. The dialysis clearance of isradipine was negligible (5.0 ml·min−1). The t1/2 values during haemodialysis were not significantly different from those observed during the same period post dose on the non-haemodialysis day. The study demonstrates that supplemental doses of isradipine are not necessary in these patients since isradipine is not significantly removed by haemodialysis.
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  • 97
    ISSN: 1432-1041
    Keywords: Liver cirrhosis ; Spirapril ; ACE inhibitor ; pharmacokinetics ; haemodynamic effects ; liver function tests
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The pharmacokinetics and haemodynamic effects of orally administered spirapril, a novel angiotensinconverting enzyme (ACE) inhibitor, have been investigated in patients with liver cirrhosis (n=10), in patients with chronic, non-cirrhotic liver disease (n=8) and in a control group of healthy subjects (n=16). The absorption and elimination of spirapril did not differ between patients with liver disease and control subjects. In contrast, the bioavailability of spiraprilat, the metabolite responsible for the pharmacological action of spirapril, was significantly reduced in patients (AUC 820 μg·h·l−1, 923 μg·h·l−1 and 1300 μg·h·l−1 in patients with cirrhosis, patients with non-cirrhotic liver disease and in healthy subjects, respectively. Compared to healthy subjects, cirrhotic patients had a reduced rate constant of spiraprilat formation (1.10 h−1 in patients vs. 2.00 h−1 in control subjects) while the elimination half-life of spiraprilat was not different. The effect of spirapril on diastolic blood pressure was decreased in patients with chronic liver disease as compared to the controls. Thus, the pharmacokinetics of spirapril was unchanged in patients with different types of liver disease, including cirrhosis. However, the bioavailability of spiraprilat and hypotensive effect of spirapril were reduced in patients.
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  • 98
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    Springer
    European journal of clinical pharmacology 40 (1991), S. 593-597 
    ISSN: 1432-1041
    Keywords: Dopamine ; Newborns ; critically ill patients ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary Dopamine is frequently used in critically ill newborn infants for treatment of shock and cardiac failure, but its pharmacokinetics has not been evaluated using a specific analytical method. Steady-state arterial plasma concentrations of dopamine were measured in 11 seriously ill infants receiving dopamine infusion, 5–20 μg · kg−1 · min−1, for presumed or proven sepsis and hypotensive shock. Steady-state concentrations of dopamine ranged from 0.013–0.3 μg/ml. Total body clearance averaged 115 ml · kg−1 · min−1. The apparent volume of distribution and elimination half life averaged 1.8 1 · kg−1 and 6.9 min, respectively. No relationship was observed between dopamine pharmacokinetics and gestational age, postnatal age or birthweight. Substantial interindividual variation was seen in dopamine pharmacokinetics in seriously ill infants, and plasma concentrations could not be predicted accurately from its infusion rate. Marked variation in clearance explains in part, the wide dose requirements of dopamine needed to elicit clinical response in critically ill newborn infants.
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  • 99
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    Electronic Resource
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    European journal of clinical pharmacology 40 (1991), S. 619-624 
    ISSN: 1432-1041
    Keywords: Inulin ; pharmacokinetics ; half life ; distribution ; concentration-dependent clearance ; healthy subjects ; chronic renal failure
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The disposition of inulin was studied in 30 healthy male and 10 healthy female volunteers, and 10 patients with stable chronic renal failure (mean creatinine clearance 45 ml·min−1) following intravenous infusion of 70 mg·kg−1 over 5 min. Plasma concentrations fell rapidly initially but the rate of decline decreased continuously over 8 h and a linear terminal elimination phase could not be identified. Inulin was excreted rapidly by the subjects with normal renal function and 97.3% of the dose was recovered in the urine in 8 h. There was a progressive highly significant fall in the renal clearance of inulin after 2 h as plasma concentrations fell below about 150 mg·l−1. Six to 8 h after administration the clearance was less than 50% of the initial value in the healthy volunteers and the corresponding fall in the renal patients was 33%. The concentration-dependent renal clearance of inulin was confirmed in “step-up” and “step-down” constant infusion studies in which clearances were measured at mean plasma concentrations ranging from 35.2 to 186.7 mg·l−1. These studies virtually excluded time, changes in posture and urine flow rate as important factors. There was no statistically significant fall in clearance during the first 2 h and kinetic analysis was based on data obtained over this time. Under these conditions the mean plasma half life, volume of distribution (Vss) and total body clearance of inulin in the healthy males, healthy females and patients with chronic renal failure were 73.2, 65.5 and 172.4 min, 10.5, 9.6 and 8.81·70 kg−1 and 113.3, 111.5 and 43.3 ml·min−1·70 kg−1 respectively. There were no sex differences in any of the kinetic variables. The mechanism of the concentration-dependent clearance of inulin is unknown but the findings are consistent with saturable renal tubular reabsorption. Care is required with the use of inulin for measurement of the glomerular filtration rate by the single injection technique.
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  • 100
    Electronic Resource
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    Springer
    European journal of clinical pharmacology 40 (1991), S. 631-633 
    ISSN: 1432-1041
    Keywords: Mefloquine ; ampicillin ; Thai subjects ; pharmacokinetics ; enterohepatic recycling ; drug interaction ; adverse effects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Summary The kinetics of a single oral dose of mefloquine given either alone or with ampicillin has been studied in 8 healthy Thai male volunteers. There was a significantly higher maximum whole blood mefloquine concentration after coadministration with ampicillin (1648 vs 1228 ng·ml−1), as well as a significantly reduced terminal half life (15.3 vs 17.7 days), mean residence time (20.1 vs 23.4 days) and volume of distribution at steady state (14.1 vs 19.4 l·kg−1). Although there was no significant change in the AUC from zero time to infinity, the AUC from zero time to 5 days was significantly increased by ampicillin (4.86 vs 3.27 μg·ml−1 day). These changes in mefloquine disposition after antibiotic treatment may be due both to an increase in fractional bioavailability and a reduction in the enterohepatic recycling of mefloquine.
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