Objective:To explore the establishment of Caco-2 cell model and its value.Methods:Established the Caco-2 cell monolayer model and validated its integrality,permeability and the expression of P-glycoprotein(P-gp) using some standard markers.Compared the results with the reported ones.Results:The apparent permeability coefficients(Papp)of Lucifer yellow and propranolol markers of the paracellular and transcellular respectively were all within the range of the reported ones.The efflux of the standard substrate of P-gp verapamil could be effectively inhibited by ketoconazole,the potent inhibitor of P-gp.Conclusion:The Caco-2 cell monolayer model can be used to study major mechanisms of gastro-intestinal(GI)absorption.