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机理性灭活体外细胞色素P450及其对体内药物相互作用定量预测的研究进展
引用本文:曹杉,周宏灏. 机理性灭活体外细胞色素P450及其对体内药物相互作用定量预测的研究进展[J]. 中国临床药理学与治疗学, 2008, 13(3): 241-248
作者姓名:曹杉  周宏灏
作者单位:中南大学临床药理研究所,长沙,410078,湖南
摘    要:近10年来,以体外细胞色素P450抑制数据预测潜在临床药物相互作用的方法得到极大发展。药物相互作用(drug-drug interaction)研究一直是临床实践和新药开发中的重要环节。本文对近年来引起广泛重视的机理性灭活作用(mechanismbased inactivation)进行总结分析,综合传统和经简化的鉴定机理性灭活作用方法,并介绍预测体内由机理性灭活引起药物相互作用的模型和影响参数。

关 键 词:药物相互作用  不可逆性抑制  机理性灭活  细胞色素P450  体外一体外预测
文章编号:1009-2501(2008)03-0241-08
修稿时间:2008-01-22

Advances in predicting of drug-drug interaction in vivo by using cytochrome P450 mechanism-based inhibition data in vitro
CAO Shan,ZHOU Hong-hao. Advances in predicting of drug-drug interaction in vivo by using cytochrome P450 mechanism-based inhibition data in vitro[J]. Chinese Journal of Clinical Pharmacology and Therapeutics, 2008, 13(3): 241-248
Authors:CAO Shan  ZHOU Hong-hao
Affiliation:( Institute of Clinical Pharmacology , Central South University, Changsha 410078, Hunan , China)
Abstract:In the last decade, the approaches for the in vitro inhibition assessment of the potentials of drug-drug interaction in vivo have received process. DDIs remain an important issue in clinical practice and the development of new drugs. Mechanism-based inactivation is gaining more attention among in vitro study. This review would describe methods in identifying mechanism-based inactivation, and introduce predictive models and parameters in the field.
Keywords:drug-drug interaction  irreversible inhibition  mechanism-based inactivation  cytochrome P450  in vitroin vivo extrapolation
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