Abstract: AIM: To establish an HPLC-MS MS method for the simultaneous determination of glimepiride and its hydroxy-metabolite M1 in human plasma, and to study their pharmacokinetic profiles in healthy Chinese volunteers.METHODS: A single oral dose of 2 mg glimepiride tablet was given to 22 healthy male volunteers individually.The concentrations of glimepiride and M1 in plasma were determined and their pharmacokinetic parameters were simulated by WinNonlin software.RESULTS: The main pharmacokinetic parameters of glimepiride and M1 were as follows:T_max 2.7 ±0.6 and 4.2 ±1.6 h,C_max 188 ±52 and 34 ±11 μg·L^-1 , AUC_{0 -24} 813 ±277and 258 ±66 μg·h·L^-1 , t_1/2 6.6 ±2.1 and 6.3 ±2.5h.CONCLUSION: The HPLC-MS/MS method developed in our lab was sensitive and precise.Glimepiride was well tolerated and exhibited ethnic difference between Chinese and Caucasian.

Key words: glimepiride, metabolite, HPLC-MS/MS, pharmacokinetics