【摘要】 目的 评价2种恩替卡韦片在中国健康受试者空腹条件下的药代动力学和生物等效性。方法 采用单中心、随机、开放、双周期交叉试验设计。30例健康中国受试者空腹口服恩替卡韦受试制剂或参比制剂0.50 mg后，血浆样品中加入乙腈直接沉淀蛋白后，按照质谱和色谱条件进行HPLC-MS/MS分析，利用WinNonlin软件（版本6.4）计算药代动力学参数，并对2种制剂的空腹给药进行生物等效性评价。结果 空腹给药受试和参比制剂血浆中恩替卡韦的C_max分别为（4 390.00±1 257.56）和（4 421.00±1 239.55） pg·mL^-1,t_max为0.67（0.33,2.00）和0.75（0.50,2.00） h,t_1/2为（29.71±14.50）和（35.43±16.58） h, AUC_{0-72 h}为（12 252.43±2 671.28）和（12 063.43±2 151.50） pg·mL^-1·h。受试制剂和参比制剂C_max、AUC_{0-72 h}和AUC_0-∞的均值比的90%置信区间均落在80.00%～125.00%。结论 受试制剂和参比制剂在空腹状态下具有生物等效性。更多还原

【Abstract】 Objective To evaluate the pharmacokinetics and bioequivalence of two entecavir tablets under fasting condition in Chinese healthy volunteers. Methods A single oral dose of 0.50 mg entecavir test and reference formulations was given to 30 healthy volunteers in the fasting state according to two randomized open-label crossover clinical studies. Plasma concentrations were determined by HPLC-MS/MS after deproteinized with acetonitrile. The pharmacokinetic parameters were calculated by WinNonlin 6.4. The bioequivalence of entecavir tablets test and its reference in the fasting state were evaluated respectively. Results In the fasting state, the main pharmacokinetic parameters of entecavir were as follows: C_max were（4 390.00±1 257.56） and（4 421.00±1 239.55） pg·mL^-1; t_max were 0.67（0.33, 2.00） and 0.75（0.50, 2.00） h; t_1/2 were（29.71±14.50） and（35.43±16.58） h, AUC_{0-72 h} were（12 252.43±2 671.28） and（12 063.43±2 151.50） pg·mL^-1·h. The 90% confidence intervals of the mean ratio of C_max,AUC_{0-72 h} and AUC_0-∞ of the text and reference formulations were all within the equivalent interval of 80.00%-125.00%. Conclusion The entecavir tablets test and its reference were bioequivalent in the fasting state.更多还原