Biopartitioning micellar chromatography: an in vitro technique for predicting human drug absorption

The main oral drug absorption barriers are fluid cell membranes and general ly drugs are absorbed by a passive diffusion mechanism. Biopartitioning mic ellar chromatography (BMC) is a mode of micellar liquid chromatography that uses micellar mobile phases of Brij35 under adequate experimental conditio ns and can be useful to mimic the drug partitioning process in biological s ystems. In this paper the usefulness of BMC for predicting oral drug absorp tion in humans is demonstrated. A hyperbolic model has been obtained using the retention data of a heterogeneous set of 74 compounds, which shows pred ictive ability for drugs absorbed by passive diffusion. The model obtained in BMC is compared with those obtained using the well-known systems (Caco-2 and TC-7) that use intestinal epithelium cell lines. The use of BMC is sim ple, reproducible and can provide key information about the transport prope rties of new compounds during the drug discovery process. (C) 2001 Elsevier Science B.V. All rights reserved.