Absorption prediction from physicochemical parameters

被引:80
作者
Krämer, SD [1 ]
机构
[1] Univ London Kings Coll, GKT Sch Biomed Sci, Div Physiol, London WC2R 2LS, England
来源
PHARMACEUTICAL SCIENCE & TECHNOLOGY TODAY | 1999年 / 2卷 / 09期
关键词
D O I
10.1016/S1461-5347(99)00188-1
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Modern drug design not only focuses on the pharmacological activity of a compound but also considers its ability to be absorbed and to reach its site of action. The prediction of in vivo barrier permeabilities, particularly intestinal absorption and blood-brain barrier passage, are substantial concerns in the development of new drug compounds. For several decades, n-octanol-water partition coefficients dominated absorption prediction, In recent years, the basic physicochemical parameters describing both membrane permeability and lipophilicity have been established. This review provides an outline of some selected absorption-prediction models with emphasis on intestinal absorption.
引用
收藏
页码:373 / 380
页数:8
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