Objective To explore whether streptozotocin-induced diabetic rat models are suitable to evaluate the pharmacokinetic processes of glibenclamide in the diabetic state. MethodsDiabetic 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. ResultsThe pharmacokinetic parameters of glibenclamide in normal rats were as following:T_max was 84.784 min, C_max 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:T_max was 255.427 min, C_max was 0.910 mg/L, CL was 0.092 L/min/kg and AUC(0-720min) 1528.280 was mg/L·min. ConclusionsThere 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.