COMPARISON OF THE PERMEABILITY CHARACTERISTICS OF A HUMAN COLONIC EPITHELIAL (CACO-2) CELL-LINE TO COLON OF RABBIT, MONKEY, AND DOG INTESTINE AND HUMAN DRUG ABSORPTION

被引：182

作者：

RUBAS, W ^{[1
]}

JEZYK, N ^{[1
]}

GRASS, GM ^{[1
]}

机构：

[1] SYNTEX INC,INST PHARMACEUT SCI,PALO ALTO,CA 94303

来源：

PHARMACEUTICAL RESEARCH | 1993年 / 10卷 / 01期

关键词：

PERMEABILITY COEFFICIENT; CACO-2; DOG; MONKEY; AND RABBIT INTESTINAL SEGMENTS; HUMAN ABSORPTION;

D O I：

10.1023/A:1018937416447

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

The in vitro permeabilities of Caco-2 monolayers and permeabilities in tissue sections from colon of monkey, rabbit. and dog were compared using a series of compounds. The selected compounds differed in their physicochemical properties, such as octanol/water partition coefficient, water solubility. and molecular Weight. Their structure included steroids, carboxylic acids, xanthins. alcohols, and polyethylene glycols. A linear permeability relationship was established between Caco-2 and colon tissue from both rabbit and monkey. The results suggest that Caco-2 is twice as permeable as rabbit and five times as permeable as monkey colon. However, no clear relationship could be established between Caco-2 monolayers and dog colon permeability. A relationship between permeability in Caco-2 monolayers and human absorption was found. The results suggest that within certain limits, permeability of Caco-2 monolayers may be used as a predictive tool to estimate human drug absorption.

引用

页码：113 / 118

页数：6

共 34 条

[21] LACTULOSE CR-51 LABELED ETHYLENEDIAMINETETRA-ACETATE, L-RHAMNOSE AND POLYETHYLENEGLYCOL-500 AS PROBE MARKERS FOR ASSESSMENT INVIVO OF HUMAN INTESTINAL PERMEABILITY [J].