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Aim: To evaluate the contribution of the impaired cytochrome P450 and breast cancer resistance protein (BCRP) activity and expression to drug pharmacokinetics under diabetic states.Methods: Diabetic was induced in rats by intraperitoneal administration of streptozocin.Glibenclamide (GLB), a substrate of BCRP, served as a model drug.The pharmacokinetics of orally administered GLB (10 mg/kg) were studied.