【摘要】 目的研究吲达帕胺片仿制药与原研药在中国健康受试者中单剂量空腹给药的药代动力学和生物等效性,为临床使用和一致性评价提供依据。方法采用开放、随机、单次口服给药、两制剂、两周期交叉设计,共纳入26名健康受试者,随机分为2组,分别单次空腹口服吲达帕胺片受试制剂与参比制剂2.5 mg,给药前和给药后按时采集静脉血,以超高效液相色谱-串联质谱（UPLC-MS/MS）法测定全血中吲达帕胺的浓度,随后用SAS9.4软件计算药代动力学参数,评价生物等效性。结果吲达帕胺片受试制剂和参比制剂后的主要药动学参数如下:C_max分别为（114.28±17.38）μg·L^-1和（96.27±13.36）μg·L^-1;AUC_0-t分别为（1746.80±297.16）μg·L^-1·h和（1717.94±77.49）μg·L^-1·h;AUC_0-∞分别为（1861.97±295.10）μg·L^-1·h和（1835.28±265.85）μg·L^-1·h;T_max（中位数）分别为2.0 h和2.0 h;T_1/2分别为（13.99±1.71） h和（14.21±1.78）h。2种制剂的C_max、AUC_0-t和AUC_0-∞经对数转换后90%的置信区间分别为113.00%¹24.13%,99.49%¹03.67%,99.00%¹03.57%。结论国产吲达帕胺片和进口吲达帕胺片药代动力学生物等效性。更多还原

【Abstract】 Objective To compare the pharmacokinetics and bioequivalence of the domestic and imported tablets of indapamide in Chinese healthy volunteers after single oral administration under fast condition.Methods This was an open,randomized,a single dose,two preparations,two sequences,cross over design.A total of 26 subjects were randomly assigned into two groups and were given a single dose of 2.5 mg indapamide tablets under fasting condition.The blood samples were collected before and after dosing.The concentrations of indapamide in whole blood were determined by an ultra performance liquid chromatographic tandem mass method.The pharmacokinetic parameters were calculated and the bioequivalence was compared by SAS 9.4 software.Results The pharmacokinetic parameters of the domestic and imported tablets were as following:C_max were（114.28±17.38） μg·L^-1 and（96.27±13.36） μg·L^-1;AUC_0-t were（1746.80±297.16）μg·L^-1·h and（1717.94±77.49） μg·L^-1·h;AUC_0-∞ were（1861.97±295.10） μg·L^-1·h and（1835.28±265.85） μg·L^-1·h;T_max（Median） were 2.Oh and 2.0 h;T_1/2 were（13.99±1.71） h and（14.21±1.78） h.The 90% CIs for C_max,AUC_0-t and AUC_0-inf were113.00%-124.13%,99.49%-103.67% and 99.00%-103.57%.Conclusion The results demonstrated that the test products and reference products were bioequivalent.更多还原