European Journal of Drug Metabolism and Pharmacokinetics

article

Pharmacokinetics of a new oral formulation of amoxicillin

M-H. Prevot, F. Jehl, B. Rouveix

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 47-52

Summary The bioavailability of the recently developed 1 g dispersible tablet form of amoxicillin (B) and the 1 g dispersible tablet in suspension form (C) were compared to that of the 1 g standard reference formulation (A). Twelve healthy volunteers were involved in this single-dose, open, randomized, three-way cross-over study. The mean peak serum levels were 14.1±4.1 μg/ml after A, 15.1 ±3.1 μg/ml...

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Practical uses of individual pharmacokinetic parameters in drug development and clinical practice: examples and simulations

T. D. Bjornsson

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 1-14

Summary This article summarizes the practical uses of the six key pharmacokinetic parameters, i.e. elimination half-life, volume of distribution, total clearance, fraction of administered dose eliminated by the kidneys, free fraction in plasma, and bioavailability. Emphasis is on the practical medical uses of these parameters in clinical practice and drug development. Numerous pharmacokinetic simulations...

article

Distribution study of radioactivity in rats after oral administration of the lipido/sterolic extract ofSerenoa repens (Permixon®) supplemented with [1-¹⁴C]-lauric acid, [1-¹⁴C]-oleic acid or [4-¹⁴C]-β-sitosterol

G. Chevalier, P. Benard, H. Cousse, T. Bengone

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 73-83

Summary The study carried out on rats given orally then-hexane lipido/sterolic extract ofSerenoa repens (LSESR), supplemented with [¹⁴C]-labelled oleic or lauric acids or β-sitosterol, demonstrated that radioactivity uptake in prostatic tissues shows the highest level in th case of administration of LSESR supplemented with [¹⁴C]-labelled oleic acid. This was clearly demonstrated on a rat with an induced...

article

Events

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 87-93

article

An approach for determination of chronopharmacokinetic parameters of methotrexate

K. Mansour

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 41-45

Summary In classical pharmacokinetic studies, the organism is represented by one or several compartments described by a system of linear differential equations with constant coefficients. A system of linear differential equations can not describe the compartmental model in the presence of chronobiological variations. The purpose of this study is to calculate the chronopharmacokinetic parameters of...

article

Influence of partial hepatectomy in rats on the activity of hepatic microsomal enzymatic systems

A. M. Maza, A. R. Gascon, M. B. Calvo, R. M. Hernandez, more

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 15-23

Summary The influence of partial hepatectomy on the activity of the hepatic microsomal enzymatic systems was determined in rats. Cytochrome P-450, cytochrome b₅, four mixed functional oxidase (MFO) activities (microsomal aniline hydroxylase,p-nitroanisole O-demethylase, aminopyrine N-demethylase and NADPH cytochrome c reductase) and glutathione levels were measured in unhepatectomized rats (control...

article

Response to letter from Dr Schein

Leonard Williams

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 86-86

article

Disposition of DX-52-1, a novel anticancer agent, after intravenous administration to mice and dogs

E. Fuse, H. Nishiie, H. Kobayashi, S. Ikeda, more

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 53-63

Summary DX-52-1 is a new derivative of a quinocarmycin analogue. The disposition of [³H]-DX-52-1 was investigated in mice and dogs after intravenous administration (4 and 0.15 mg/kg, respectively). The plasma concentration of non-volatile radioactivity was 7.4 μg eq./ml 3 min after administration to mice, the declined biphasically until 2 h. The distribution of non-volatile radioactivity into blood...

article

Ciprofloxacin decreases plasma phenytoin concentrations in the rat

M. S. Al-Humayyd

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 35-39

Summary The pharmacokinetic interaction between phenytoin and ciprofloxacin was studied in rats. One group of animals was given phenytoin (20 mg/kg, p.o.) as a single daily dose for 7 days. In another group of animals, the same protocol was followed except that ciprofloxacin was given in two equal doses (15 mg/kg, i.p., each) on days 5, 6, and 7. On day 8, phenytoin blood sampling was performed at...

article

Metabolism of 4-[1-(2-fluoro-4-biphenylyl)ethyl]-2-methylaminothiazole (SM-8849) in rats

M. Yabuki, J. Shimakura, M. Ito, H. Kanamaru, more

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 25-33

Summary Metabolism of 4-[1-(2-fluoro-4-biphenylyl)ethyl]-2-methylaminothiazole (SM-8849), a novel immunomodulatory agent, in rats was investigated. By co-chromatography with authentic samples, desmethylated (SM-8800)p-hydroxylated (SL-5512) and desmethylated-p-hydroxylated SM-8849 (SL-5515) were detected in the bile. Thermospray mass spectrometry (TSP-MS) analysis of five metabolites isolated from...

article

Cruciferous vegetables and drug metabolism

J. R. Schein

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 85-85

article

Metabolism of mangafodipir trisodium (MnDPDP), a new contrast medium for magnetic resonance imaging, in beagle dogs

K. G. Toft, S. O. Hustvedt, D. Grant, G. A. Friisk, more

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 1 > 65-72

Summary The metabolism of MnDPDP (manganese(II)N,N′-dipyridoxylethylenediamine-N,N′-diacetate-5,5′-bis(phosphate) was studied in dogs after intravenous infusion for 12.5 min with either 10, 30 or 100 μmol MnDPDP/kg b.w. HPLC analyses of plasma samples obtained 1, 5 and 30 min after the end of infusion revealed that MnDPDP was rapidly dephosphorylated to MnDPMP (manganese(II)N,N′-dipyridoxylethylenediamine-...

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In vitro studies on the metabolic fate of mifentidine, a novel histamine H₂-receptor antagonist

K. Pattichis, M. Kajbaf, J. W. Gorrod

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 155-164

Summary The in vitro metabolism of mifentidine and several of its metabolites was studied using hepatic microsomes from seven animal species. The effects of potential enzyme inducers, inhibitors and activators were also studied. Mifentidine metabolites identified and characterised were: 4-imidazolylphenylamine (amine), 4-imidazolylphenyl-formamide (formamide), the urea derivative of mifentidine (urea)...

article

Deuterium isotope effects on caffeine metabolism

Y. Benchekroun, S. Dautraix, M. Desage, J. L. Brazier

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 127-133

Summary The aim of this work was to study the influence of labelling on caffeine metabolism according to the incubation mode. It has been observed that labelling induces an isotopic effect on metabolisation speed: apparent half-lives are systematically increased. Moreover, isotopic effects are in agreement with those previously observed for retention times. Qualitatively, caffeine labelling systematically...

article

Metabolism studies on transdermal prostaglandin E₁ in human foreskin in vitro

M. Foldvari, C. J. N. Oguejiofor

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 111-120

Summary The metabolism of prostaglandin E₁ (PGE₁) in solution and in transdermal liposomal formulations was investigated in vitro by incubation with homogenates from human foreskin (HSH), with rabbit lung (RLH) and human placenta (HPH) and heat denatured homogenates as controls. PGE₁ and its metabolites and degradation products were analyzed by reversed phase HPLC. Metabolism of PGE₁ in HSH was negligible...

article

Involvement of the rat gut epithelial and muscular layer, and microflora in chiral inversion and acyl-glucuronidation of R-fenoprofen

S. Sattari, F. Jamali

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 97-101

Summary In the presence of excised human and rat gut, the pharmacologically inactive R enantiomers of both ibuprofen and fenoprofen (FN) are bioinverted to their anti-inflammatory antipodes. In an attempt to further localize the site of inversion, we incubated R-FN, in oxygenated (O₂:CO₂, 95:5, v/v) Krebs-Henseleit solution (37°C, pH 7.4) for 3 h in the presence of the intestinal contents, epithelium...

article

Maximal biliary transport of sulfobromophthalein in patients with a T-tube placed in the common bile duct

M. A. Serra, A. Caballero, J. A. Olmo, L. Aparisi, more

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 135-139

Summary In 19 adult patients with choledocholithiasis who were operated on, excretion of free and conjugated sulfobromophthalein (BSP) in the bile collected through a T-tube inserted in the common bile duct was determined. The transport maximum (T_m) for BSP was calculated by the constant-infusion technique after an intravenous infusion of the dye at a rate of 0.3 and 0.09 mg/kg/min for the first and...

article

Variability of diphenhydramine N-glucuronidation in healthy subjects

D. Fischer, U. Breyer-Pfaff

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 151-154

Summary The H₁-antagonist diphenhydramine can undergo direct glucuronidation at its tertiary amino group with formation of a quaternary ammonium glucuronide. The intraindividual variability in the amount of N-glucuronide excretion in urine was investigated in two female volunteers who repeatedly took single doses of 25 mg diphenhydramine hydrochloride without and with concomitant administration of...

article

The effect of velnacrine on the mixed function oxidase system

M. J. Eccles, T. C. Danbury, J. M. Ford, C. J. C. Roberts

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 121-125

Summary Velnacrine is a centrally acting anticholinesterase which has been considered for use in the treatment of Alzheimer’s disease. If proven to be of value, it will be used concurrently with other medications. Its potential to cause interaction is, therefore, important to study. The aim of this work was to investigate velnacrine as an inhibitor of hepatic oxidative enzymes. The effects of velnacrine...

article

Interaction of chlormezanone with rat liver microsomes and its degradation

W. Klinger, H. Oelschläger, E. Karge, D. Rothley

European Journal of Drug Metabolism and Pharmacokinetics > 1997 > 22 > 2 > 165-171

Summary Chlormezanone binds to oxidized cytochrome P450 in rat liver microsomes with a binding curve according to type I like hexobarbital but less pronounced and with a general shift to the left. Ethylmorphine N-demethylation, ethoxycoumarin and ethoxyresorufin O-deethylation are inhibited by chlormezanone in mM concentrations only whereas pentoxyreosorufin O-depentylation is inhibited by about 50%...

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European Journal of Drug Metabolism and Pharmacokinetics

Pharmacokinetics of a new oral formulation of amoxicillin

Practical uses of individual pharmacokinetic parameters in drug development and clinical practice: examples and simulations

Distribution study of radioactivity in rats after oral administration of the lipido/sterolic extract ofSerenoa repens (Permixon®) supplemented with [1-¹⁴C]-lauric acid, [1-¹⁴C]-oleic acid or [4-¹⁴C]-β-sitosterol

Events

An approach for determination of chronopharmacokinetic parameters of methotrexate

Influence of partial hepatectomy in rats on the activity of hepatic microsomal enzymatic systems

Response to letter from Dr Schein

Disposition of DX-52-1, a novel anticancer agent, after intravenous administration to mice and dogs

Ciprofloxacin decreases plasma phenytoin concentrations in the rat

Metabolism of 4-[1-(2-fluoro-4-biphenylyl)ethyl]-2-methylaminothiazole (SM-8849) in rats

Cruciferous vegetables and drug metabolism

Metabolism of mangafodipir trisodium (MnDPDP), a new contrast medium for magnetic resonance imaging, in beagle dogs

In vitro studies on the metabolic fate of mifentidine, a novel histamine H₂-receptor antagonist

Deuterium isotope effects on caffeine metabolism

Metabolism studies on transdermal prostaglandin E₁ in human foreskin in vitro

Involvement of the rat gut epithelial and muscular layer, and microflora in chiral inversion and acyl-glucuronidation of R-fenoprofen

Maximal biliary transport of sulfobromophthalein in patients with a T-tube placed in the common bile duct

Variability of diphenhydramine N-glucuronidation in healthy subjects

The effect of velnacrine on the mixed function oxidase system

Interaction of chlormezanone with rat liver microsomes and its degradation

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