替米沙坦片人体生物等效性

Bioequivalence study of telmisartan tablets in healthy volunteers

目的 研究国产替米沙坦片与进口替米沙坦片的人体生物等效性。方法 用LC-MS法,测定20名健康男性单次交叉口服参比制剂及试验制剂80mg后血浆中不同时间点的药物浓度,经SPSS软件统计拟合,计算其药物动力学参数和相对生物利用度,评价两制剂的生物等效性。结果参比制剂及试验制剂的主要药代动力学参数C_(max)、t_(max)、AUC_(0→96)和AUC_(0→∞)分别为:347.2±41.1和352.4±42.9 μg·L^(-1);1.1±0.25和1.1±0.21h;2910.5±289.6和2866.8±235.5 μg·h·L^(-1);3044.8±307.2和3006.4±251.3 μg·h·L^(-1)。试验制剂对参比制剂的相对生物利用度F为(98.9±7.0)％。AUC_(0→96),C_(max)对数转换后,经双单侧t检验并计算AUC(0→96),C_(max)的90％可信区间。结论 两制剂具有生物等效性。

Objective To study the bioequivalence of telmisartan tablets in healthy volunteers.Methods Telmisartan concentrations in serum were determined by LC-MS after a single oral dose of 80mg of telmisartan tablet or reference telmisartan tablet was given to 20 healthy male volunteers in an randomized cross-over design.The pharmacokinetic parameters and relative bioavailability were calculated by SPSS program to evaluate the bioequivalence of two preparations. Results AUC_(0→96) of reference and test drug were 2910.5± 289.6 and 2866.8± 235.5 μ g·h·L^(-1), C_(max) were 347.2± 41.1 and 352.4± 42.9 μ g·L^(-1), t_(max) were 1.1± 0.25 and 1.1± 0.21 h, respectively. Conclusion The 2 preparations are bioequivalent.The relative bioavailability of the test drug was (98.9± 7.0)%. The two preparations are bioequivallent.