【摘要】 目的 研究阿莫西林颗粒在中国健康人体内的生物等效性。方法 采用单中心、随机、开放、单剂量、两制剂、两周期、双交叉试验设计。空腹试验和餐后试验中分别入组28例受试者，每周期口服阿莫西林颗粒受试制剂或参比制剂0.5 g。用LC-MS/MS法测定人血浆中阿莫西林的血药浓度，并用Phoenix WinNonlin 8.2软件计算主要药代动力学参数，进行生物等效性评价。结果 空腹试验受试制剂和参比制剂阿莫西林的主要药代动力学参数：C_max分别为（11 222.19±2 497.11）和（10 919.47±2 282.44）ng·mL^-1,AUC_0-t分别为（27 238.73±3 324.23）和（26 288.06±2 904.36）h·ng·mL^-1,AUC_0-∞分别为（27 329.87±3 324.57）和（26 373.57±2 902.25）h·ng·mL^-1,T_max均为1.00 h。餐后试验受试制剂和参比制剂阿莫西林的主要药代动力学参数：C_max分别为（7 210.34±1 072.25）和（7 140.64±1 175.17）ng·mL^-1,AUC_0-t分别为（27 840.59±3 112.02）和（27 133.23±2 930.17）h·ng·mL^-1,AUC_0-∞分别为（28 041.75±3 168.89）和（27 330.42±3 025.51）h·ng·mL^-1,T_max均为2.50 h。受试制剂与参比制剂C_max、AUC_0-t、AUC_0-∞几何均值比的90%置信区间均在80.00%～125.00%内。结论 2种阿莫西林颗粒在中国健康受试者体内具有生物等效性。更多还原

【Abstract】 Objective To study the bioequivalence of amoxicillin grains in healthy Chinese subjects.Methods A single-center,randomized,open,single-dose,two-cycle,2*2 cross-over trial design was adopted.Under fasting and fedding conditions,28 healthy subjects were given amoxicillin grains test preparation 0.5 g （0.125 g×4 bags） or reference preparation 0.5 g orally.The plasma concentrations of amoxicillin at different time after treatment were detected by LC-MS/MS,and the main pharmacokinetic parameters were calculated by Phoenix Win Nonlin 8.2 to determine whether the two preparations were equivalent.Results The pharmacokinetic parameters of test preparation and reference preparation in fasting state were as follows:C_maxwere（11 222.19±2 497.11） and （10 919.47±2 282.44） ng·mL^-1;AUC_0-t were （27 238.73±3 324.23） and （26 288.06±2 904.36） h·ng·mL^-1;AUC_0-∞were （27 329.87±3 324.57） and （26 373.57±2 902.25）h·ng·mL^-1.Both of their T_maxwere 1.00 h.The pharmacokinetic parameters of test preparation and reference preparation in postprandial state were as follows:C_maxwere （7 210.34±1 072.25） and （7 140.64±1 175.17） ng·mL^-1;AUC_0-twere（27 840.59±3 112.02） and （27 133.23±2 930.17） h·ng·mL^-1;AUC_0-∞were （28 041.75±3 168.89） and（27 330.42±3 025.51） h·ng·mL^-1.Both of their T_maxwere 2.50 h.The 90%confidence intervals of the geometric mean ratios of C_max,AUC_0-tand AUC_0-∞of the test preparation and the reference preparation were all completely within 80.00%-125.00%.Conclusion The test and reference preparations of amoxicillin were bioequivalent in Chinese healthy subjects.更多还原