盐酸二甲双胍片在中国健康人体的生物等效性

目的评价2种国产盐酸二甲双胍片(口服降糖药)在中国健康人体的生物等效性。方法 20名健康男性受试者随机交叉单剂量口服盐酸二甲双胍片试验药物和对照药物,各1.0 g。用高效液相色谱法测定血浆中盐酸二甲双胍的浓度,用DAS 2.0软件计算药代动力学参数,并对2种药物进行生物等效性评价。结果试验药物和对照药物的主要药代动力学参数如下:Cmax为(2.83±0.53),(2.57±0.57)mg.L-1;Tmax为(1.55±0.39),(1.63±0.36)h;t1/2为(3.70±1.76),(3.36±0.72)h;AUC0-24为(10.20±1.95),(9.71±2.56)mg.h.L-1。AUC0-24、AUC0-∞、Cmax的90%可信区间分别为99.1%～114.6%、99.1%～113.8%和100.6%～110.4%。试验药物相对于对照药物的生物利用度F为(108.3±20.5)%。结论试验药物和对照药物生物等效。

Bioequivalence of metformin hydrochloride tablets in Chinese healthy volunteers

Objective To evaluate the bioequivalence of two domestic metformin hydrochloride tablets in healthy volunteers.MethodsA single oral dose(1.0 g of test and reference formulation) was given to 20 healthy volunteers in a randomized crossover study.The concentrations of metformin hydrochloride in plasma were determined by HPLC.The bioavailability and bioequivalence of two formulations were evaluated by DAS 2.0 software,then the bioequivalence was judged.ResultsAfter a single dose,the pharmacokinetic parameters for tested and reference metformin hydrochloride were as follows: Cmax were(2.83±0.53),(2.57±0.57) mg·L-1;Tmax were(1.55±0.39),(1.63±0.36)h;t1/2 were(3.70±1.76),(3.36±0.72)h;AUC0-24 were(10.20±1.95),(9.71± 2.56) mg·h·L-1,respectively.The 90%confidential interval of AUC0-24,AUC0-∞ and Cmax of test formulation were 99.1%-114.6%,99.1%-113.8% and 100.6%-110.4%,respectively.The relative bioavailability of test to reference formulation was(108.3±20.5)%.ConclusionThe test and reference metformin hydrochloride were bioequivalence.