Functional characteristics of the intestinal efflux system in in vitro intestinal models

摘要

Oral absorption is in part determined by the ability of a drug to cross the intestinal epithelium. Recent experiments have shown that mucosal(m)-to-serosal(s) transcellular drug transport can be impeded by the p-glycoprotein, located on the apical side of intestinal epithelial cells. This may result in poor oral bioavailability and high variability (1,2) It is therefore important at early stages of drug discovery to screen for compounds which are substrates for P-gp. In this abstract we present data on polarized transport of 3 known P-glycoprotein substrates in rabbit and rat small and large intestinal tissues and Caco-2 cells, to evaluate these systems for apical efflux screening.