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标题：Stereoselective Pharmacokinetics of BOF-4272 Racemate after Oral Administration to Rats and Dogs
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作者：Shinsaku Naito ; Masuhiro Nishimura
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2002
卷号：25
期号：5
页码：674-677
DOI：10.1248/bpb.25.674
出版社：The Pharmaceutical Society of Japan
摘要：The stereoselective pharmacokinetics of BOF-4272 enantiomers in rats and dogs was investigated by simultaneously measuring concentrations in arterial, portal, and venous plasma, the liver, and the kidney at 2 h after the oral administration of the racemic drug. The concentrations of BOF-4272 enantiomers were measured using high-performance liquid chromatography. The concentrations of the S (−) enantiomer in arterial, portal, and venous plasma were higher than those of the R (+) enantiomer in rats, but the opposite was found in dogs. In rats, absorption from the intestinal tract into the portal system was almost the same for the two enantiomers, whereas the hepatic uptake of the R (+) enantiomer was greater than that of the S (−) enantiomer. In dogs, absorption from the intestinal tract into the portal system was greater for the R (+) enantiomer than for the S (−) enantiomer, whereas hepatic uptake was comparable for the two enantiomers. The stereoselectivity of the renal uptake of BOF-4272 enantiomers had little effect on the stereoselectivity of enantiomers in the systemic circulation in both rats and dogs. The stereoselectivity in the systemic circulation of BOF-4272 enantiomers is therefore related to hepatic uptake in rats, and to absorption from the intestinal tract into the portal system in dogs.
关键词：stereoselectivity;xanthine oxidase inhibitor;sulphoxide-containing drug;oral administration;hepatic uptake;BOF-4272