Abstract:
:The biotransformation of netobimin (NTB) pro-drug by ruminal, abomasal and intestinal fluids of sheep and cattle was investigated under anaerobic conditions in vitro. No metabolic conversion of NTB was observed upon incubation with abomasal fluid or boiled samples of different gastrointestinal fluids. NTB pro-drug was reduced and cyclised into albendazole (ABZ) and this further oxidized into ABZ sulphoxide (ABZSO) and ABZ sulphone (ABZSO2) by both sheep and cattle ruminal and ileal fluids. A zwitterion formulation of NTB produced a significantly greater amount of anthelminthically active ABZ metabolites (ABZ and ABZSO) than a trisamine salt formulation of the same compound. Although there was no difference in the total amount of products formed, both cattle ruminal and ileal fluids showed a greater oxidative capacity than sheep derived fluids. This was evidenced by the greater amounts of ABZSO recovered and by the resultant lower ratios of ABZ/ABZSO obtained with cattle fluids.
journal_name
Eur J Drug Metab Pharmacokinetjournal_title
European journal of drug metabolism and pharmacokineticsauthors
Lanusse CE,Nare B,Gascon LH,Prichard RKdoi
10.1007/BF03188780keywords:
subject
Has Abstractpub_date
1992-04-01 00:00:00pages
121-8issue
2eissn
0378-7966issn
2107-0180journal_volume
17pub_type
杂志文章abstract::The main objective of this study was to investigate the release and pharmacokinetic profiles of ketoprofen (KP) from developed thermosensitive and mucoadhesive liquid suppositories. Thermosensitive liquid suppositories were prepared using KP, poloxamer 407 (P 407), poloxamer 188 (P 188) and various amounts of differen...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-013-0157-6
更新日期:2014-12-01 00:00:00
abstract::Because of its special pharmacokinetic properties, plasma levels of theophylline show significant differences between individuals and also its therapeutic index is very low. So, plasma theophylline concentration measurements are essential for an effective and safe treatment. In the present study, age related differenc...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1994-01-01 00:00:00
abstract::Fucithalmic is a newly developed 1% microcrystalline suspension of the antistaphylococcal antibiotic fusidic acid. Penetration into the eye was investigated in twenty patients about to undergo cataract extraction. A single dose produced median antibiotic levels in the aqueous humour of 0.3 mcg/ml, maintained for at le...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
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更新日期:1985-10-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190862
更新日期:2003-01-01 00:00:00
abstract::Fluvastatin (FV), a new cholesterol-lowering agent, has been studied for its effects on hepatic microsomal drug-metabolizing enzymes in male rats. FV was orally administered in dosages of 1, 5, and 30 mg/kg/day for 7 consecutive days. 3-Hydroxy-3-methylglutaryl CoA (HMG-CoA) reductase activities were markedly decrease...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189669
更新日期:1995-07-01 00:00:00
abstract::The purpose of this study was to determine the distribution of cyclosporin A (CsA) in various ocular fluids and tissues in the rabbit by two routes of administration. CsA was administered to two groups of two rabbits either by intramuscular route at a dose of 25 mg/kg/day or by local route using eyedrops, at a dose of...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:
更新日期:1991-01-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
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更新日期:1999-10-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章,评审
doi:10.1007/BF03189473
更新日期:1981-01-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
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更新日期:2019-04-01 00:00:00
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pub_type: 杂志文章
doi:10.1007/BF03190881
更新日期:2008-10-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章,评审
doi:10.1007/s13318-017-0416-z
更新日期:2018-02-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190966
更新日期:1997-10-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 临床试验,杂志文章
doi:10.1007/BF03190358
更新日期:1999-04-01 00:00:00
abstract::It is known that substituted hydrazide hydrazone derivatives have several biological and pharmacological activities; there is limited literature on the metabolism of hydrazide hydrazones in rats. In our previous study, 4-fluorobenzoic acid [(5-nitro-2-furanyl)methylene]hydrazide (S) was found active against Staphyloco...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190075
更新日期:2000-04-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190163
更新日期:1992-10-01 00:00:00
abstract::The disposition kinetics of the N-oxide of picobenzide were studied after administration to rabbits at a bolus dose of 30 mg/kg of picobenzide intravenously. The biotransformation process fits a first-order kinetic process, and the metabolite shows good access capacity to the peripheral compartment. The N-oxide of pic...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190837
更新日期:1989-01-01 00:00:00
abstract::Experimental evidence suggested that H2-receptor antagonists may inhibit not only hepatic but also adrenal cytochrome P-450 dependent monooxygenases. Therefore, the effects of ranitidine (150 mg b.i.d. over 14 days) on cortisol metabolism and antipyrine clearance have been investigated in nine healthy volunteers. Urin...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189981
更新日期:1992-01-01 00:00:00
abstract:BACKGROUND AND OBJECTIVES:Gadobenate dimeglumine (Gd-BOPTA) is a commercialised hepatobiliary contrast agent used during liver magnetic resonance imaging (MRI) to detect liver diseases. It enters into human hepatocytes through organic anion transporting polypeptides (OATP1B1/B3) and crosses the canalicular transporter ...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-016-0382-x
更新日期:2017-08-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190181
更新日期:1993-10-01 00:00:00
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更新日期:2015-06-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 临床试验,杂志文章,随机对照试验
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更新日期:1990-10-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
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更新日期:1999-01-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189442
更新日期:1980-01-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
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更新日期:2005-01-01 00:00:00
abstract::Pharmacokinetics of recombinant human basic fibroblast growth factor (rhbFGF) in mice were studied by using a radioiodination method combined with sodium dodecyl sulfate-polyacrylamide gel electrophoresis (SDS-PAGE) and a sandwich enzyme-Linked immunosorbent assay (ELISA). RhbFGF concentration in serum were dertermine...
journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03190593
更新日期:2004-07-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/s13318-010-0001-1
更新日期:2010-09-01 00:00:00
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更新日期:2016-12-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
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更新日期:2014-12-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03188812
更新日期:1993-07-01 00:00:00
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journal_title:European journal of drug metabolism and pharmacokinetics
pub_type: 杂志文章
doi:10.1007/BF03189910
更新日期:1987-10-01 00:00:00