COMPARATIVE METABOLISM OF TOSUFLOXACIN AND BMY-43748 IN HEPATOCYTES FROM RAT, DOG, MONKEY AND MAN

被引：3

作者：

DAUPHIN, JF

GRAVIERE, C

BOUZARD, D

ROHOU, S

CHESNE, C

GUILLOUZO, A

机构：

[1] RENNES ATALANTE VILLEJEAN,BIOPRED,F-35000 RENNES,FRANCE

[2] HOP PONTCHAILLOU,INSERM,U49,UNITE RECH HEPATOL,F-35033 RENNEX,FRANCE

来源：

TOXICOLOGY IN VITRO | 1993年 / 7卷 / 04期

关键词：

D O I：

10.1016/0887-2333(93)90054-9

中图分类号：

R99 [毒物学（毒理学）];

学科分类号：

100405 ;

摘要：

Metabolism of two broad spectrum quinolones in advanced preclinical development-tosufloxacin and BMY 43748-was compared in hepatocyte cultures derived from rat, dog, monkey and humans. The drugs were added at the first medium renewal and incubated for 4 or 24 hr in serum-free medium. Metabolites were analysed by HPLC. Marked species differences were found in both the metabolic rates and pathways of the two quinolones. BMY 43748 was found to be more actively metabolized than tosufloxacin in cultured hepatocytes from the three animal species. Human hepatocytes were totally ineffective, thereby indicating that they were metabolically different from monkey cells. Comparison with available in vivo data demonstrated a good but not perfect qualitative in vivo/in vitro

引用

页码：499 / 503

页数：5

共 17 条

[1] CULTURED HUMAN ADULT HEPATOCYTES - A NEW MODEL FOR DRUG-METABOLISM STUDIES [J].