格列美脲片人体药代动力学及相对生物利用度研究

Pharmacokinetics and Relative Bioavailability of Glimepiride Tablets in Healthy Volunteers

目的:研究国产格列美脲片剂的药代动力学和相对生物利用度。方法:18名健康志愿者随机交叉单剂量口服国产与进口格列美脲4mg,采用柱前衍生化HPLC－紫外法测定其血药浓度。结果:国产片与进口片的主要药代动力学参数tmax分别为3.44±0.92和2.79±0.88h,Cmax分别为2.96.1±108.4和331.8±103.3μ·L-1,t(1/2)ke分别8.03±3.01和 7.73±2.79h,AUCO-t分别为2307.9±800.9和 2302.8±794.8μg·h·L-1,AUC0-∞分别为2672.7±990.5和2589.1±752.5μg·h·L-1。国产片的相对生物利用度为102.4%±19.7%。结论:统计学结果显示,两种片剂具有生物等效性。

OBJETIVE:The aim of this research is to study the pharmacokinetics andrelative bioavailability of domestic glimepiride tablets. METHOD: A single oraldose of 4mg of domestic and imported glimepiride tablets were given to l8 healthyvolunteers in a randomized crossover design. Plasma concentrations weredetermined by pre-column derivatization HPLC method. RESULTS: The mainpharmacokinetic parameters were:tmax3.44±0.92 and 2.97±0.88h, Cmax296.l±l08.4 and 33l.8±l03.3μg.L-1, t(1/2)ke 8.03±0.0l and 7.73±2.79h, AUC0-t,2307.9±800.9 and 2302.8±794.8μg.h.L-1,AUC0-∞2672.7±990.5 and 2589.l±752.5mg.h.L-1 for domestic and imported tablets, respectively. The relative bioavailabilityof domestic tablets was l02.4%±l9.7% .CONCLUSIONS: The results of statisticsanalysis demonstrated that two tablets were bioequivalent.