Source:http://linkedlifedata.com/resource/pubmed/id/15744718
Switch to
Predicate | Object |
---|---|
rdf:type | |
lifeskim:mentions | |
pubmed:issue |
4
|
pubmed:dateCreated |
2005-4-19
|
pubmed:abstractText |
It 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.
|
pubmed:language |
eng
|
pubmed:journal | |
pubmed:citationSubset |
IM
|
pubmed:chemical | |
pubmed:status |
MEDLINE
|
pubmed:month |
May
|
pubmed:issn |
0142-2782
|
pubmed:author | |
pubmed:copyrightInfo |
Copyright (c) 2005 John Wiley & Sons, Ltd.
|
pubmed:issnType |
Print
|
pubmed:volume |
26
|
pubmed:owner |
NLM
|
pubmed:authorsComplete |
Y
|
pubmed:pagination |
129-34
|
pubmed:dateRevised |
2006-11-15
|
pubmed:meshHeading |
pubmed-meshheading:15744718-Administration, Oral,
pubmed-meshheading:15744718-Animals,
pubmed-meshheading:15744718-Bile,
pubmed-meshheading:15744718-Biological Availability,
pubmed-meshheading:15744718-Duodenum,
pubmed-meshheading:15744718-Injections, Intravenous,
pubmed-meshheading:15744718-Intestines,
pubmed-meshheading:15744718-Liver,
pubmed-meshheading:15744718-Male,
pubmed-meshheading:15744718-Metabolic Clearance Rate,
pubmed-meshheading:15744718-Portal Vein,
pubmed-meshheading:15744718-Pyrazines,
pubmed-meshheading:15744718-Rats,
pubmed-meshheading:15744718-Rats, Sprague-Dawley,
pubmed-meshheading:15744718-Stomach,
pubmed-meshheading:15744718-Tissue Distribution
|
pubmed:year |
2005
|
pubmed:articleTitle |
Hepatic and intestinal first-pass effects of oltipraz in rats.
|
pubmed:affiliation |
College of Pharmacy and Research Institute of Pharmaceutical Sciences, Seoul National University, San 56-1, Shinlim-Dong, Kwanak-Gu, Seoul 151-742, Republic of Korea.
|
pubmed:publicationType |
Journal Article,
Research Support, Non-U.S. Gov't
|