BILIARY-SECRETION OF FELODIPINE METABOLITES IN MAN AFTER INTRAVENOUS [C-14] FELODIPINE

被引:14
作者
SUTFIN, TA
LIND, T
GABRIELSSON, M
REGARDH, CG
机构
[1] AB HASSLE,CARDIOVASC RES LABS,DEPT PHARMACOKINET & DRUG METAB,S-43183 MOLNDAL,SWEDEN
[2] SAHLGRENS UNIV HOSP,DEPT SURG 2,GOTHENBURG,SWEDEN
关键词
bile; biliary secretion; dihydropyridines; drug metabolism; felodipine; healthy volunteers; pharmacokinetics;
D O I
10.1007/BF02336677
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The biliary secretion of [ 14 C]felodipine in 4 healthy human subjects was studied by use of the multiple marker dilution principle with double lumen tubes placed in the stomach and intestine. Insignificant amounts of 14 C activity were recovered from gastric aspirates. The individual recovery from intestinal aspirates varied from 2.9 to 8.5% of the dose of radioactivity over the period of 4.5 h after dosing. Less than 0.1% was identified as unchanged felodipine. The results show that biliary secretion is a minor route of elimination of felodipine or its metabolites. Bile collection for 4.5 h had no significant effect on the pharmacokinetics of felodipine, although the 72 h urinary recovery of radioactivity tended to be lower when bile was collected (59%) than in the control experiment (66%). © 1990 Springer-Verlag.
引用
收藏
页码:421 / 424
页数:4
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