国产与进口奥美沙坦酯片在健康人体中的生物等效性分析

Bioequivalence analysis of domestic and imported olmesartan medoxomil tablets in healthy volunteers

目的研究南京正大天晴制药有限公司研制的奥美沙坦酯片在人体中的生物利用度,并与进口奥美沙坦酯片比较,评价两者生物等效性。方法选取2015年1-6月健康自愿受试者20名,采用标准两阶段自身对照试验设计,口服国产药物(受试制剂)或进口药物(参比制剂)20 mg后,采用LC-MS/MS法测定受试者血浆中奥美沙坦的血药浓度,计算主要药动学参数和相对生物利用度,进行生物等效性检验。结果单次口服20 mg奥美沙坦酯片受试制剂和参比制剂后,药动学参数分别为:Cmax为(613.3±127.7)ng/ml和(541.0±86.0)ng/ml;Tmax为(1.9±0.6)和(2.2±0.8)h;t1/2为(7.1±1.5)和(7.0±0.8)h;AUC0~48为(3811±674)h·ng^(-1)·ml^(-1)和(3484±643)h·ng^(-1)·ml^(-1),AUC0~∞为(3895 677)h·ng^(-1)·ml^(-1)和(3472 670)h·ng^(-1)·ml^(-1)。各药动学参数间比较,差异无统计学意义(P>0.05)。结论南京正大天晴制药有限公司研制的奥美沙坦酯片和日本第一三共生产的奥美沙坦酯片生物等效。

Objective To study the bioequivalence of olmesartan medoxomil tablets manufactured in Nanjing Chia Tai Tianqing Pharmaceutical Co.,Ltd,and compared with imported olmesartan medoxomil tablets to evaluate the bioequivalence.Methods A total of healthy male volunteers were selected from January to June 2015,designed of a standard two-stage their own test,after oral dose of 20 mg of domestic tablets（ test formulation） or imported tablets（ reference formulation）,olmesartan medoxomil plasma concentration was measured by LC-MS/MS method,and calculated the main pharmacokinetic parameters and relative bioavailability to evaluate the bioequivalence. Results After a single oral dose of 20 mg olmesartan medoxomil and reference formulation,the main pharmacokinetic parameters were listed as follows： Cmaxwas（ 613. 3 ± 127. 7） ng/ml and（ 541. 0 ± 86. 0） ng/ml; Tmaxwas（ 1. 9 ± 0. 6） h and（ 2. 2 ± 0. 8） h; t1/2was（ 7. 1 ± 1. 5） h and（ 7. 0 ± 0. 8） h; AUC0-48was（ 3811 ± 674） h·ng^-1·ml^-1and（ 3484 ± 643） h · ng^-1·ml^-1,AUC0-∞was（ 3895 677） h · ng^-1·ml^-1and（ 3472 670） h·ng^-1·ml^-1. There is no significant different between the formulations in the pharmacokinetic parameters（ P〉 0. 05）. Conclusion The olmesartan medoxomil tablets manufactured by Nanjing Chia Tai Tianqing Pharmaceutical Co.,Ltd and Daiichi sankyo are bioequivalent.