Caco2 cell permeability
Numerous in vitro methods have been used in the drug selection process for assessing the intestinal absorption of drug candidates. Among them, Caco-2 cell model and MDCK cell model has been recommended as a reliable in vitro model for the prediction of oral drug absorption.
[ Yamashita,S. et al. Eur. J. Pharm. 2000, 10, 195. ]
Caco-2 cells are derived from human colon adenocarcinoma and possess multiple drug transport pathways through the intestinal epithelium.
For prediction of Caco-2 cell permeability in PreADMET, chemical structures at pH 7.4 are applied, because Caco-2 cell permeability and MDCK cell permeability are measured at about pH 7.4. This is one of options of PreAMDET and user can choose for this option.
Although there are some differences in the experimental values by compounds or their metabolisms, we can put into general categories like below.
[ Yazdanian,M. Pharm. Res. 1998, 15(9), 1490. ]
|Low permeability||less than 4|
|Middle permeability||4 ~ 70|
|High permeability||more than 70|
[ (1) Yamashita,S. et al. Eur. J. Pharm. Sci. 2000, 10, 195., (2) Irvine,J.D. et al. J. Pharm. Sci. 1999, 88, 28. ]