奥美沙坦酯片人体生物等效性研究

Bioequivalence of olmesartan medoxomil tablet in healthy volunteers

目的:评价奥美沙坦酯片与奥美沙坦酯胶囊的人体生物等效性。方法:采用双周期交叉设计,28例健康志愿者随机交叉口服单剂量奥美沙坦酯片(受试制剂)或奥美沙坦酯胶囊(参比制剂)20 mg,采用高效液相色谱法测定血浆中奥美沙坦的血药浓度。结果:受试制剂与参比制剂的t_(1/2)分别为(6．72±1．80)和(6．49±1．52)h, C_(max)分别为(495．0±255．3)和(396．0±147．5)μg·L^(-1),T_(max)分别为(2．4±0．7)和(2．9±1．0)h,AUC_(0-t)分别为(2 899±877)和(2 658±840)μg·h·L^(-1),AUC_(0-∞)分别为(3 091±925)和(2 847±932)μg·h·L^(-1),以AUC_(0-∞)计算,奥美沙坦酯胶囊的相对生物利用度平均为(114．0±34．5)％。结论:奥美沙坦酯片与奥美沙坦酯胶囊生物等效。

Objective：To evaluate the relative bioavailability of olmesartan medoxomil tablet （test） versus capsule（reference）. Methods ：Twenty-eight healthy male volunteers received a single crossover dose of test and reference olmesartan medoxomil 20 mg. The plasma concentrations of olmesartan were determined by HPLC. Results ：The pharmacokinetic profiles of test and reference olmesartan were as following： t1/2 （6.72 ± 1.80）vs（6.49 ± 1.52） h, Cmax （495.0 ±255.3 ）vs（396.0 ± 147.5 ） μg· L^-1, Tmax （2. 4 ± 0.7）vs（2. 9 ± 1.0） h, AUC0-t（2 899 ±877）vs（2 658 ±840） μg·h· L^-1, AUC0-∞ （3 091 ±925）vs（2 847 ± 932） μg·h· L^-1, respectively. The relative bioavailability of the test olmesartan was （ 114.0 ± 34.5 ） %. Conclusion：The test olmesartan medoxomil was bioequivalent to the reference olmesartan medoxomil.