Transport and metabolism of ampicillin prodrugs and their interactions with P-glycoprotein:in vitro study on successful prodrugs using Caco-2 cell monolayers

摘要

Prodrugs have been developed to overcome the faults of active drugs.One typical example is to improve intestinal absorption by increasing lipophilicity of active drugs.Lenampicillin,bacampicillin,and talampicillin are prodrugs of antibiotics such as ampicillin.Nevertheless,the absorption process of these prodrugs has not been characterized in detail.In addition,it has been reported that a prodrug failed to improve drug absorption [1].These tell us that it is important to verify the absorption process of prodrug.Therefore,we have previously characterized transport and metabolism of lenampicillin using Caco-2 cells [2].In the present paper we report on the transport and metabolism of bacampicillin and talampicillin.