2种替米沙坦制剂的人体生物等效性研究

目的:研究替米沙坦胶囊与替米沙坦片在人体内的生物等效性。方法:20名志愿者随机交叉单剂量口服国产替米沙坦胶囊(受试制剂)或进口替米沙坦片(参比制剂)80mg后,采用高效液相色谱法测定血药浓度,用3p97软件计算二者的药动学参数,并评价其生物等效性。结果:受试制剂与参比制剂的药-时曲线均符合口服吸收一室模型,药动学参数分别为:t1/2K(e74.23±25.11)、(79.18±23.27)h,tma(x2.08±1.64)、(2.02±0.86)h,cma(x2.10±1.36)、(1.95±1.08)μg·mL-1,AUC0～144(h116.25±55.97)、(123.94±65.66)μg·h·mL-1。国产替米沙坦胶囊的相对生物利用度为(93.80±12.24)%。经方差分析、双单侧t检验及1-2α置信区间法统计分析,各药动学参数无显著性差异(P>0.05)。结论:国产替米沙坦胶囊与进口替米沙坦片具有生物等效性。

Study on the Bioequivalence of 2 Kinds of Domestic Telmisartan Preparations in Human

OBJECTIVE ： To study the bioequivalence of Telmisartan capsule and Telmisartan tablet. METHODS： A randomized crossover design was performed in 20 healthy volunteers. A single oral dose of either domestic Telmisartan capsules （test preparation） or imported Telmisartan tablets （reference preparation） 80 mg were administered. Plasma concentration of telmisartan was measured by HPLC. The pharmacokinetic parameters were measured by 3p97 software. RESULTS： Blood concentration-time curves of test preparation or reference preparation fitted to one-compartment open model. Pharmacokinetic parameters were as follows： t1/2Ke were（74.23± 25.11）h and （79.18±23.27）h, tmax（2.08± 1.64） h and （2.02± 0.86） h,Cmax（2.10 ± 1.36）μg·mL^-1 and （ 1.95 ±1.08） μg·mL^-1, AUC0-144 h （ 116.25± 55.97） μg·mL^-1 and （123.94 ± 65.66）μg·mL^-1, respectively. The relative bioavailability of domestic capsules was （93.80 ± 12.24）%, compared with imported tablet. There was no significant difference in pharmaceutical parameters through variance analysis, t-test and 1- 2a confidence interval method. CONCLUSION： Domestic Telmisartan capsule and imported Telmisartan tablet are bioequivalent.