替米沙坦片人体相对生物利用度研究

The relative bioavailability of telmisartan tablets

目的:比较国产与进口替米沙坦片药动学及人体生物等效性。方法:20例健康男性志愿者随机交叉口服替米沙坦片受试制剂或参比制剂80mg,采用HPLC-荧光检测法测定血浆中替米沙坦浓度,经3P97软件统计,进行相对生物利用度与生物等效性分析。结果:受试者口服替米沙坦受试制剂和参比制剂后,血浆中替米沙坦T_(max),C_(max),AUC_(0～1),AUC_(0～∞)和t_(1/2)分别为(0.91±0.19)和(0.86±0.21)h;(672.7±275.1)和(710.2±312.9)μg·L^(-1);(4221.4±2909.0)和(4430.2±3487.9)μg·h·L^(-1);(4568.1±3032.5)和(4742.6±3657.3)μg·h·L^(-1);(30.7±7.0)和(28.0±5.9)h。以AUC_(0～1)计算,替米沙坦片相对生物利用度平均为(98.1±12.1)%。结论:经方差分析和双单侧t检验,两种制剂具有生物等效性。

Objective: To evaluate the pharmacokinetics and relative bioavailability of telmisartan tablets imported (test) versus locally manufactured (reference). Methods:20 healthy male volunteers were randomly administered a single crossover dose of 80mg test and reference tablets. Plasma telmisartan concentration was determined by HPLC-Fluorescent analysis, and the relative bioavailability and bioequivalence of the tablets analyzed using the 3p97 program. Results: The pharmacokinetic parameters of test and reference tablets were as follows: T_(max)(0. 91±0.19) vs. (0.86±0.21)h; C_(max) (672.7±275. 1) vs. (710. 2 ± 312. 9) μg?mL^(-1); AUC_(0～t) (4221. 4 ± 2909. 0) vs. (4430. 2±3487.9)μg·h·L^(-1); AUC_(0～∞)(4 568.1±3 032. 5) vs. (4 742. 6 + 3 657. 3)μg·h·L^(-1); t_(1/2)(30.7± 7.0) vs. (28.0 ± 5.9)h.The relative bioavailability of the test formulation was (98.1±12.1) %. Conclusion: The test tablets are bioequivalent to the reference tablets.