Discrimination between drug candidates using models for evaluation of intestinal absorption

被引：52

作者：

Stewart, BH ^{[1
]}

Chan, OH ^{[1
]}

Jezyk, N ^{[1
]}

Fleisher, D ^{[1
]}

机构：

[1] UNIV MICHIGAN, COLL PHARM, ANN ARBOR, MI 48109 USA

来源：

ADVANCED DRUG DELIVERY REVIEWS | 1997年 / 23卷 / 1-3期

关键词：

permeability; stability; intestinal absorption; cell uptake; lipophilicity;

D O I：

10.1016/S0169-409X(96)00424-3

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Methods employing in vitro and in situ means can be used to gain early information regarding the potential for intestinal absorption of new chemical entities (NCEs). Physicochemical and biological approaches for evaluation of the intestinal absorption of NCEs are described in this review. Physicochemical measurements such as aqueous solubility, lipophilicity and membrane partioning form an important base for subsequent biological experiments. Biological techniques that include subcellular membrane fractions, intestinal cells, isolated tissue and organ perfusion are detailed. Several of these preparations can be utilized for transport, as well as stability indicators. While some methods are generally applicable to NCEs, others require selectivity on the parr of the investigator, depending on the information desired.

引用

页码：27 / 45

页数：19

共 145 条

[1] EXTENSION OF THE FRAGMENT METHOD TO CALCULATE AMINO-ACID ZWITTERION AND SIDE-CHAIN PARTITION-COEFFICIENTS [J].