Abstract

CASTILLO, Rocío; CHIRIBOGA, Carlos  and  FONTANILLA, Marta R. Standardization of a model based on Caco-2 cell monolayers with application on in vitro drug absorption tests. Rev. colomb. cienc. quim. farm. [online]. 2006, vol.35, n.2, pp.177-191. ISSN 0034-7418.

The bioavailability of orally administered drugs depends mainly on their transport through the intestinal mucosa. Epithelial cell line cultures have been used as models to asses the intestinal absorption of a drug in vitro. The United States Food and Drug Administration (FDA) acknowledges the epithelial Caco-2 system as part of the in vitro tests used to establish a drug’s bioequivalence. Despite the usefulness of this model, in Colombia it has not been applied to predict oral absorption and the biopharmaceutical classification. In the present work the Caco-2 monolayer unidirectional apparent permeability coefficients (Papp) for ranitidine and theophyline were established. Samples from basolateral and apical chambers were analysed by High Performance Liquid Chromatography (HPLC) and Papp values were calculated based on the concentrations found. The accuracy of this system’s measurements was evaluated intra and inter-day experiments. Ranitidine and theophyline Papp values found allowed the correct assignment of these compounds class permeability. Permeability tests of reference compounds are still required to validate this model.

Keywords : Drug absorption; monolayers; permeability; Caco-2 cells.

        · abstract in Spanish     · text in Spanish     · Spanish ( pdf )