Evaluation of the Pharmacokinetics of Glibenclamide in Streptozotocin-Induced Diabetic Rat Models

Objective To explore whether streptozotocin-induced diabetic rat models are suitable to evaluate the pharmacokinetic processes of glibenclamide in the diabetic state.Methods Diabetic rats induced by intraperitoneal injection of 60 mg/kg streptozotocin and normal rats were administered glibenclamide at a dose of 10 mg/kg.The concentration of glibenclamide was determined by high performance liquid chromatography.Pharmacokinetic parameters were calculated using DAS 2.0 software.Results The pharmacokinetic parameters of glibenclamide in normal rats were as following: Tmax was 84.784 min,Cmax was 0.259 mg/L,CL/F was 0.092 L/min/kg and AUC(0-720min) was 509.523 mg/L·min.The same parameters in diabetic rats: Tmax was 255.427 min,Cmax was 0.910 mg/L,CL was 0.092 L/min/kg and AUC(0-720min) 1528.280 was mg/L·min.Conclusions There were significant differences between pharmacokinetic values of normal and diabetic rats.The results were different from that reported in the literature.Therefore,streptozotocin-induced diabetic rat models might not be suitable for pharmacokinetic evaluation of drugs in type Ⅱ diabetic conditions.