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pubmed-article:15744718pubmed:dateCreated2005-4-19lld:pubmed
pubmed-article:15744718pubmed:abstractTextIt was reported that the mean value of the extent of absolute oral bioavailability (F) of oltipraz at a dose of 20 mg/kg was 41.2% and only 2.68% of the oral dose was unabsorbed from the gastrointestinal tract in rats. Hence, the low F in rats could be due to considerable first-pass (gastric, intestinal and hepatic) effects. Hence, the first-pass effects of oltipraz were measured after intravenous, intraportal, intragastric and intraduodenal administration of the drug at a dose of 20 mg/kg to rats. The total area under the plasma concentration-time curve from time zero to time infinity (AUC) values between intragastric and intraduodenal administration (213 and 212 microg min/ml) in rats were almost similar, but the values were significantly smaller than that after intraportal administration (316 microg min/ml) in rats, indicating that gastric first-pass effect was almost negligible (due to negligible absorption of oltipraz from rat stomach), but the intestinal first-pass effect of oltipraz was considerable, approximately 32% of the oral dose. The hepatic first-pass effect of oltipraz was approximately 40% based on AUC values between intravenous and intraportal administration (319 versus 536 microg min/ml). Since approximately 65% of the oral oltipraz was absorbed into the portal vein, the value of 40% was equivalent to 25% of the oral dose. The low F of oltipraz in rats was mainly due to considerable hepatic and intestinal first-pass effects.lld:pubmed
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pubmed-article:15744718pubmed:statusMEDLINElld:pubmed
pubmed-article:15744718pubmed:monthMaylld:pubmed
pubmed-article:15744718pubmed:issn0142-2782lld:pubmed
pubmed-article:15744718pubmed:authorpubmed-author:KimSang GSGlld:pubmed
pubmed-article:15744718pubmed:authorpubmed-author:KimJin WJWlld:pubmed
pubmed-article:15744718pubmed:authorpubmed-author:KimYoon GYGlld:pubmed
pubmed-article:15744718pubmed:authorpubmed-author:LeeMyung GMGlld:pubmed
pubmed-article:15744718pubmed:authorpubmed-author:KimYoung HYHlld:pubmed
pubmed-article:15744718pubmed:authorpubmed-author:BaeSoo KSKlld:pubmed
pubmed-article:15744718pubmed:copyrightInfoCopyright (c) 2005 John Wiley & Sons, Ltd.lld:pubmed
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pubmed-article:15744718pubmed:volume26lld:pubmed
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pubmed-article:15744718pubmed:pagination129-34lld:pubmed
pubmed-article:15744718pubmed:dateRevised2006-11-15lld:pubmed
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pubmed-article:15744718pubmed:year2005lld:pubmed
pubmed-article:15744718pubmed:articleTitleHepatic and intestinal first-pass effects of oltipraz in rats.lld:pubmed
pubmed-article:15744718pubmed:affiliationCollege of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, San 56-1, Shinlim-Dong, Kwanak-Gu, Seoul 151-742, Republic of Korea.lld:pubmed
pubmed-article:15744718pubmed:publicationTypeJournal Articlelld:pubmed
pubmed-article:15744718pubmed:publicationTypeResearch Support, Non-U.S. Gov'tlld:pubmed