SPECIES-DIFFERENCES IN THE GENERATION OF THE CHIRAL SULFOXIDE METABOLITE OF ALBENDAZOLE IN SHEEP AND RATS

被引:59
作者
DELATOUR, P
BENOIT, E
CAUDE, M
TAMBUTE, A
机构
[1] ECOLE SUPER PHYS & CHIM IND,F-75231 PARIS 05,FRANCE
[2] CTR ETUD BOUCHET,F-91710 VERT LE PETIT,FRANCE
关键词
albendazole; enantiomeric separation; metabolism; rat; sheep; sulfoxides;
D O I
10.1002/chir.530020306
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The prochiral anthelmintic drug albendazole was administered orally to sheep and rats. Blood samples were taken at standardized intervals during the time course of the plasma kinetics: 18 h in rats and 48 h in sheep. The enantiomeric ratio of the sulfoxide metabolite was determined by means of HPLC on a chiral stationary phase, the chiral selector of which was a N‐3,5‐dinitrobenzoyl derivative of (S)‐tyrosine. Two enantiomers were detected in both animal species but their ratios were inverted in rat vs. sheep. The evolution of the ratio is turned from a racemate at 15 min to 60(−):40(+) at 12 h in rats, while it moved from 23(−):77(+) at 3 h to 4(−):96(+) at 36 h after administration in sheep. Copyright © 1990 Wiley‐Liss, Inc.
引用
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页码:156 / 160
页数:5
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