ALBERT

All Library Books, journals and Electronic Records Telegrafenberg

X
feed icon rss

Your email was sent successfully. Check your inbox.

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

Proceed reservation?

Export
Filter
  • pharmacokinetics  (18)
  • NMR  (7)
  • Springer  (25)
  • 2000-2004
  • 1990-1994  (25)
  • 1994  (25)
Collection
Keywords
Publisher
Years
  • 2000-2004
  • 1990-1994  (25)
Year
  • 1
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and Pharmacodynamics of L-703,014, a Potent Fibrinogen Receptor Antagonist, After Intravenous and Oral Administration in the Dog (1994)
    Springer
    Pharmaceutical research 11 (1994), S. 426-431 
    Details
    ISSN: 1573-904X
    Keywords: fibrinogen receptor antagonist ; pharmacokinetics ; pharmacodynamics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The pharmacokinetics and pharmacodynamics of L-703,014, a fibrinogen receptor antagonist, have been examined in the dog. An analytical method which utilizes methanol precipitation of dog plasma proteins followed by HPLC with an automated column switching technique using the chemical analogue L-704,326 as internal standard was developed for the determination of L-703,014 in dog plasma. The compound was not metabolized in the dog and was eliminated in the kidneys and into bile. Of the administered dose, 68.9 ± 1.3% (i.v.) and 80.5 ± 11.9% (p.o.) were recovered in the feces; 20.3 ± 3% (i.v.) and 2.2 ± 0.2% (p.o.) were recovered in the urine by 72 hr. L-703,014 was 23 ± 3.4% bound in dog plasma protein and the mean ratio of plasma/whole blood was 1.22 ± 0.05. The mean terminal half-life was 118 ± 36 min, the mean steady-state volume of distribution was 0.61 ± 0.22 L/kg, and the mean plasma clearance was 8 ± 2 mL/min/kg. Ex vivo platelet aggregation measurements were made by inducing platelet aggregation with 10 µg/ mL collagen in the presence of 1 µM epinephrine as an agonist. The mean C 50 was 44.4 ± 6.0 ng/mL, and the mean Hill coefficient was 1.5 ± 0.3. The mean bioavailability was 4.9 ± 1.4% in dogs administered 2.0 mg/kg (p.o.).
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1023/A:1018973323039
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 2
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and tolerability of ascending intravenous doses of granisetron, a novel 5-HT3 antagonist, in healthy human subjects (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 159-162 
    Details
    ISSN: 1432-1041
    Keywords: Granisetron ; Anti-emetic ; pharmacokinetics ; tolerance ; ascending dose ; healthy subjects
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics and tolerance of granisetron, a novel 5HT3-receptor antagonist which is under development as an anti-emetic agent have been studied after administration of single 30 min intravenous infusions to three groups of 8 healthy male subjects, in a series of placebo-controlled ascending dose studies (50, 80, 100 and 130 μg·kg−1 to group 1; 150, 180, 200 and 230 μg·kg−1 to group 2 and 270 and 300 μg·kg−1 to group 3). Plasma and urine samples were analysed for granisetron by HPLC with fluorimetric detection. Administration of granisetron was well tolerated by the volunteers and there were no serious adverse effects reported. Pharmacokinetic parameters and dose-normalised plasma levels appeared to be independent of dose in the range 50 to 300 μg·kg−1, although there was extensive inter-subject variability. Granisetron was extensively distributed, with mean volumes of distribution ranging from 186–264 l at the various doses. Total plasma clearance was, in general, rapid (mean values of 37.0 to 49.9 l·h−1) and predominantly non-renal, with most subjects excreting less than 20% of the dose unchanged in urine. Mean t1/2 values ranged from 4.1 to 6.3 h and MRT from 5.2 to 8.1 h.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00199881
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 3
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and haemodynamic effects of ISDN following different dosage forms and routes of administration (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 319-324 
    Details
    ISSN: 1432-1041
    Keywords: Isosorbide dinitrate ; route of administration ; isosorbide-5-mononitrate ; finger pulse wave ; pharmacokinetics ; haemodynamic effects ; plasma nitrates
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics and haemodynamic effects of isosorbide dinitrate (ISDN) have been investigated following administration of single doses as a sublingual (SL) spray (2.5 mg), sublingual tablet (5 mg) and peroral tablet (10 mg) in a randomised, placebo-controlled double-blind cross-over trial in 16 healthy volunteers. After the sublingual spray Cmax was higher (39.0 ng·ml-1) and tmax was shorter (3.9 min) than after the sublingual (22.8 ng·ml-1 and 13.8 min) and peroral (16.9 ng·ml-1 and 25.6 min) tablets. The AUC of ISDN did not differ following any of the three formulations (1031; 879; 997 ng·ml-1·min, for the spray, SL tablet and PO-tablet, respectively). Mononitrate metabolites of ISDN (IS-2-MN and IS-5-MN) and total nitrates in plasma increased in proportion to the administered dose. This indicates that the fraction of the dose absorbed was the same for all the formulations but that the extent of first-pass metabolism increased in the order sublingual spray 〈 sublingual tablet 〈 peroral tablet. Thus, compared to the spray, the relative bioavailability of ISDN was 48% and 28% from the sublingual and peroral tablets, respectively. The haemodynamic effects were quantified using the a/b ratio of the finger pulse wave and the systolic blood pressure and heart rate under orthostatic conditions. For the a/b ratio of the finger pulse, the maximal effect was higher (emax=130%) and the time to emax (temax) shorter (16.6 min) after the spray than the sublingual tablet (84.4% and 25.5 min) or peroral tablet (90.2 and 31.3 min). The onset of effect was within 3, 5 and 7.5 min after the spray, sublingual and peroral tablets, respectively. A larger change in the orthostatically-induced decrease in systolic blood pressure and increase in heart rate was obtained following peroral than sublingual administration despite the similar plasma concentrations of ISDN. This probably reflects the larger amount of pharmacodynamically active mononitrate metabolites formed after oral dosing. The integrated effect following administration of 2.5 mg ISDN as spray was similar to that of a sublingual tablet of 5 mg.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00194399
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 4
    Electronic Resource
    Electronic Resource
    A direct carbon-13 and nitrogen-15 NMR study of samarium(III) complexation with nitrate and isothiocyanate in aqueous solvent mixtures (1994)
    Springer
    Journal of solution chemistry 23 (1994), S. 1019-1047 
    Details
    ISSN: 1572-8927
    Keywords: Carbon-13 ; nitrogen-15 ; NMR ; samarium-nitrate complexes ; samarium-isothiocyanate complexes
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Notes: Abstract The extent of inner-shell, contact ion-pairing between samarium(III)-nitrate and in a preliminary manner, samarium(III)-isothiocyanate, has been determined by a direct, low-temperature, multinuclear magnetic resonance technique. In water-acetone mixtures containing Freon-12 or Freon-22, the slow exchange condition is achieved at −110 to −120°C, permitting the observation of15N NMR resonance signals for bulk and coordinated nitrate. In these mixtures, signals are observed for Sm(NO3)2+, Sm(NO3) 2 + , and two higher complexes, possibly the tetranitrato with either the penta-or hexanitrato.1H NMR signals for bound water molecules in these mixtures were observed, but accurate hydration numbers can not yed be determined. In anhydrous or aqueous methanol mixtures,15N NMR signals for only three complexes are observed, with the dinitrato clearly dominating. Using15N and35Cl NMR chemical shift and linewidth measurements, the superior complexing ability of nitrate compared to perchlorate and chloride, was demonstrated. Successful preliminary13C and15N NMR measurements of Sm3+-NCS− interactions in water-acetone-Freon-22 mixtures also have been made. The13C NMR spectra reveal signals for five complexes, presumably Sm(NCS)2+ through Sm(NCS) 5 2− . In the15N NMR spectra, signals for only three complexes are observed (the result of insufficient spectral resolution.) displaced about +240 ppm from bulk anion.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00974101
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 5
    Electronic Resource
    Electronic Resource
    Crystallographic and NMR evidence for the enol tautomer of 3-methoxy-4-hydroxy-5-chloro-phenylpyruvic acid (1994)
    Springer
    Journal of chemical crystallography 24 (1994), S. 665-668 
    Details
    ISSN: 1572-8854
    Keywords: NMR ; enol tautomer ; phenylpyruvic acid
    Source: Springer Online Journal Archives 1860-2000
    Topics: Geosciences , Physics
    Notes: Abstract The structures and conformation of 3-methoxy-4-hydroxy-5-chloro-phenylpyruvic acid3 and its acetate ester4 have been investigated by X-ray crystallography and by spectroscopic methods. Three independent molecules crystallized for the ester4 with the triclinic symmetry and the centrosymmetric space group (Z=6) and with the cell dimensionsa=11.764(6),b=13.549(5),c=13.978(15) Å. α=100.08(7), β=94.62(8), γ=115.06(4)°. The three conformers of4 exist as the enolate tautomers and not the keto form.Trans extended side pyruvic acid side chains were observed for the three conformers. The crystalline cohesion was ensured by a strong network of hydrogen bonds. The NMR spectra of the phenylpyruvic acid3 and the acetate ester4 exhibited each a single proton on the benzylic carbon atom and chemical shift values supporting the existence of the enolate tautomer form for these phenylpyruvic acid compounds in solution.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01668227
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 6
    Electronic Resource
    Electronic Resource
    Syntheses and spectroscopic studies of diphenylphosphinato derivatives of boron (1994)
    Springer
    Monatshefte für Chemie 125 (1994), S. 607-613 
    Details
    ISSN: 1434-4475
    Keywords: Boron ; Diphenylphosphinato ; IR ; NMR ; B-11 ; P-31 ; Sn-119
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology
    Description / Table of Contents: Zusammenfassung 2-Diphenylphosphinato-1,3,2-dioxaborolane und -borinane des Typs (mitG = -CH2CHMe-, -CH2CH2CH2-,-CH2CH2CHMe-, -CMe2CMe2-,-CMe2CH2CHMe-, -CH2CMe2CH2-, -CH2CEt2CH2- und C6H4) erhält man durch Reaktion von Diphenylphosphinsäure mit den entsprechenden 2,2′-Oxo-bis-1,3,2-dioxaborolanen und -borinanen. Die Produkte sind weiße, kristalline, hydrolyseunempfindliche Festkörper. Sie wurden mittels Elementaranalyse, IR-Spektroskopie und multinuklearer NMR-Spektroskopie (11B,31P und119Sn) charakterisiert. Die Resultate legen Strukturen mit monodentaten Phosphinatoeinheiten und dreifach koordinierten Boratomen nahe.
    Notes: Summary 2-Diphenylphosphinato-1,3,2-dioxaborolanes and -borinanes of the type (whereG = -CH2CHMe-, -CH2CH2CH2-, -CH2CH2CHMe-,-CMe2CMe2-, -CMe2CH2CHMe-,-CH2CMe2CH2-, -CH2CEt2CH2-, and -C6H4-) are obtained by the reaction of diphenylphosphinic acid with the corresponding 2,2′-oxo-bis-1,3,2-dioxaborolanes and-borinanes. The products are white crystalline solids, which have sharp melting points and are hydrolytically stable. They have been characterized by elemental analysis, IR and multinuclear NMR (11B,31P, and119Sn) studies. The data suggest structures with monodentate phosphinato moieties and 3-coordinated boron atoms.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF01277620
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 7
    Electronic Resource
    Electronic Resource
    Esmolol, an ultrashort-acting, selective β1-adrenoceptor antagonist: pharmacodynamic and pharmacokinetic properties (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 399-404 
    Details
    ISSN: 1432-1041
    Keywords: Esmolol ; β1-Adrenoceptor antagonist ; tricresylphosphate ; pharmacokinetics ; effect kinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The effects of esmolol at different rates of infusion (100, 250 and 500 μg·kg−1 BW·min−1) were compared with β-adrenoceptor occupancy (β1 and β2, estimated by a subtype selective radioreceptor assay) and plasma concentrations of esmolol and its acid metabolite were measured by HPLC. Up to a rate of infusion of esmolol of 500 μg·kg−1 BW·min−1 there was a maximal β1-receptor occupancy of 84.7% while β2-receptor occupancy was below the detection limit; confirming the β1 selectivity of esmolol. Exercise-induced increases in heart rate and systolic blood pressure were reduced by esmolol in a dose-dependent manner. The estimated EC50 values of rate of infusion for the reduction in heart rate and systolic blood pressure during exercise were 113 and 134 μg·kg−1 BW · min−1, respectively. Additionally, heart rate and systolic blood pressure were reduced moderately at rest. Because of the short elimination half-life of esmolol caused by the rapid hydrolysis to its acid metabolite, 45 min after end of infusion high plasma concentrations of the metabolite (maximally 80 μg·ml−1) but no esmolol were detectable. Since no in vivo effects have been observed, despite the presence of high plasma concentrations of the metabolite, the metabolite did not participate in the observed effects up to an infusion rate of esmolol of 500 μg·kg−1 BW·min−1. The plasma concentrations of antagonist detected by radioreceptor assay and plasma concentrations of esmolol detected by HPLC showed a good correlation (r=0.97). Since the cardiovascular effects, determined before and 45 min after termination of infusion of esmolol were similar, it can be concluded that the observed effects on heart rate and systolic blood pressure are exclusively mediated by esmolol.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00191900
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 8
    Electronic Resource
    Electronic Resource
    Pharmacokinetics and pharmacodynamics of ramipril and piretanide administered alone and in combination (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 545-550 
    Details
    ISSN: 1432-1041
    Keywords: Ramipril ; Piretanide ; pharmacokinetics ; pharmacodynamics ; healthy volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics and pharmacodynamics of single oral doses of 5 mg ramipril and 6 mg piretanide administered separately and in combination were determined in a single blind, randomised, 3-period cross-over study in 24 healthy male volunteers. The peak plasma concentrations of ramipril and ramiprilat increased slightly (from 11.9 to 14.8 ng/ml, and from 6.39 to 8.96 ng/ml, respectively) as did the area under the plasma concentration-time curve of ramipril (0–4 h) and ramiprilat (0–24 h) (from 15.8 to 19.8 ng·ml−1·h, and from 63.4 to 74.6 ng·ml−1·h, respectively). The urinary excretion of ramiprilat also rose (from 6.82 to 7.73 % of dose) following simultaneous treatment with piretanide. These effects were probably due to reduced first-pass metabolism of ramipril/ramiprilat to inactive metabolites. The blood pressure lowering effect, the time course of inhibition of ACE activity in plasma and the concentration-response relationship for the inhibition of plasma ACE activity were not affected by piretanide. The peak plasma concentration of piretanide was somewhat reduced (from 285 to 244 ng/ml) following simultaneous treatment with ramipril. No other pharmacokinetic parameter was affected. Piretanide increased urine flow, and sodium, chloride and potassium excretion, especially during the first 2 hours following administration. These pharmacodynamic parameters were not affected by ramipril. Thus, simultaneous administration of single oral doses of ramipril and piretanide caused modest changes in the peak and average plasma concentrations of both drugs, which did not lead to detectable alterations in the pharmacodynamic parameters measured in healthy volunteers.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00196113
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 9
    Electronic Resource
    Electronic Resource
    The pharmacokinetics and pharmacodynamics of medifoxamine after oral administration in healthy elderly volunteers (1994)
    Springer
    European journal of clinical pharmacology 46 (1994), S. 163-166 
    Details
    ISSN: 1432-1041
    Keywords: Medifoxamine ; pharmacokinetics ; pharmacodynamics ; elderly volunteers
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract The pharmacokinetics and psychomotor effects of medifoxamine, a 5 HT reuptake inhibitory antidepressant, were studied in healthy elderly volunteers after single and multiple dosing. The elimination half life (t1/2z) after single doses of 300 mg was 2.8 h — almost identical to that found in young volunteers. After seven days of dosing at 100 mg three times daily the mean corrected AUC after 300 mg significantly increased from 1.04 to 1.34 mg.h.l−1 and t1/2z increased to 4.0 h (NS). There were no significant changes in critical flicker fusion frequency, symbol digit substitution, continuous attention or choice reaction times.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00199882
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
  • 10
    Electronic Resource
    Electronic Resource
    The effect of renal impairment on the pharmacokinetics of oxcarbazepine and its metabolites (1994)
    Springer
    European journal of clinical pharmacology 47 (1994), S. 161-167 
    Details
    ISSN: 1432-1041
    Keywords: Oxcarbazepine ; 10,11-dihydro-10-hydroxy-carbamazepine ; renal impairment ; pharmacokinetics
    Source: Springer Online Journal Archives 1860-2000
    Topics: Chemistry and Pharmacology , Medicine
    Notes: Abstract We have studied the effect of renal impairment on the pharmacokinetics of oxcarbazepine, its active monohydroxy-metabolite (which predominates in plasma), their glucuronides, and the inactive dihydroxy-metabolite after a single oral dose of oxcarbazepine (300 mg). Six subjects with normal renal function and 20 patients with various degrees of renal impairment participated. The mean areas under the plasma concentration-time curves of oxcarbazepine and its monohydroxy-metabolite were 2–2.5-times higher in patients with severe renal impairment (CLCR〈10 ml·min−1) than in healthy subjects. The apparent elimination half-life of the monohydroxy-metabolite [19 (SD 3) h] in these patients was about twice that in healthy subjects. The effect of renal impairment on the plasma concentrations of glucuronides was more marked. The renal clearances of the unconjugated monohydroxy-metabolite and its glucuronides (the main compounds recovered in urine) correlated well with creatinine clearance. The maximum target dose in patients with slight renal impairment (CLCR〉30 ml·min−1) should not be changed. In patients with moderate renal impairment (CLCR10–30 ml·min−1) it should be reduced by 50%. In patients with severe renal impairment (CLCR〈10 ml·min−1), the glucuronides of oxcarbazepine and its monohydroxy-metabolite are likely to accumulate during repeated administration, and dosage adjustment of oxcarbazepine in these patients could not be proposed from this single administration study.
    Type of Medium: Electronic Resource
    URL: http://dx.doi.org/10.1007/BF00194967
    Location Call Number Expected Availability
    BibTip Others were also interested in ...
    Paper (German National Licenses)
    Fulltext
Close ⊗
This website uses cookies and the analysis tool Matomo. More information can be found here...