【摘要】 目的:评价健康受试者单剂量口服受试替米沙坦胶囊,片剂以及参比替米沙坦片剂的人体药动学与生物等效性。方法:采用3种制剂3周期随机交叉试验设计,LC-MS-MS法测定18例男性健康受试者单剂量口服80 mg国产替米沙坦胶囊、替米沙坦片和进口替米沙坦片后替米沙坦的血药浓度。采用非室模型计算药动学参数。AUC,Cmax对数转换后进行方差分析并计算90％置信区间。结果:国产替米沙坦胶囊、替米沙坦片剂,进口替米沙坦片剂的主要药动学参数分别为:Cmax=(1 016．3±571．7),(869．7±623．8)和(905．7±583．4)ng·mL-1, Tmax=(1．5±1．0),(1．5±0．6)和(1．6±1．1)h,AUC0-t=(7 372±3 955),(7 373±4 347)和(6 774±3 758)ng·h·mL-1,AUC0-∞=(8 432±4 946),(8 623±5 687)和(7 502±4 663)ng·h·mL-1,t1/2=(24．9±9．2),(24．5±11．9)和(23．0±6．5)h。结论:国产替米沙坦胶囊、替米沙坦片与进口替米沙坦片具有生物等效性。更多还原

【Abstract】 Objective: To evaluate the pharmacokinetics and bioequivalence of domestic telmisartan capsules and tablets (test samples) with imported telmisartan tablets ( reference samples) . Method : This was an open randomized, three periods cross over study that recruited eighteen healthy male volunteers. Each volunteer were randomly administered with a single oral dose of telmisartan (test or reference samples) 80 mg. The plasma concentrations of telmisartan were determined by LC-MS-MS. A non-compartmental method was used in analysis of pharmacokinetic parameters. Logarithm-transformed Cmax and AUC were analyzed by the analysis of variance (ANOVA) and 90% confidence intervals. Results; The main pharmacokinetic parameters of domestic telmisartan capsules, tablets and imported telmisartan tablets were as following: Cmax(1016.3±571.7), (869. 7±623. 8) , (905. 7±583. 4) ng·mL-1; Tmax(1.5±1.0), (1.5±0.6), (1.6±1.1)h; AUC0-t(7 372±3 955), (7373±4347), (6774±3 758)ng·h·mL-1; AUC0-∞(8 432±4 946), (8 623±5687), (7 502±4 663 ) ng·h·mL-1; t1/2 (24. 9±9.2), (24. 5±11.9), (23. 0±6. 5) h, respectively. Conclusion: The domestic telmisartan capsules and tablets are bioequivalent with the imported telmisartan tablets.更多还原