人体关键药代动力学参数预测方法

Prediction of key pharmacokinetic parameters in human

分布容积、清除率、半衰期和生物利用度是重要的药物代谢动力学参数,决定着药物在体内的暴露程度与暴露时间,在新药开发过程中尽早预测人体内这些参数对选择与优化潜在新药有重要价值。本文综述了采用临床前药代动力学实验数据、体外吸收与代谢数据、化合物理化性质、计算机模拟等多种方法预测人体内关键药代动力学参数的研究及其进展。

Volume of distribution,clearance,half of life and bioavailability are crucial pharmacokinetic parameters determining the extent and sustained time of drugs exposed in vivo.Thus,in the stage of drug discovery and development,it is of particular interest to estimate the pharmacokinetic parameters of drug candidates in human as early as possible to select the most promising compounds for further development.This paper reviews recent developments in prediction of human key pharmacokinetic parameters based upon preclinical animal pharmacokinetic data,absorption and metabolism data in vitro,physico-chemical property and in silico prediction.