奥美拉唑肠溶胶囊的人体药动学及生物等效性

Pharmacokinetics and Bioequivalence of Omeprazole Capsules

目的:建立测定奥美拉唑血药浓度的高效液相色谱法,并考察奥美拉唑肠溶胶囊人体药动学和比较两种制剂的生物等效性。方法:采用两周期两制剂交叉试验设计,24例男性健康志愿者随机分为两组,分别单剂量交叉口服奥美拉唑肠溶胶囊(受试试剂)和洛赛克肠溶胶囊(参比制剂)40 mg,以反相高效液相法测定给药后不同时间点奥美拉唑血药浓度,采用DAS房室模型法和生物等效性计算程序进行统计分析。结果:奥美拉唑肠溶胶囊(受试试剂)和洛赛克肠溶胶囊(参比制剂)血药浓度-时间曲线符合一室开放模型。主要药动学参数:tmax分别为(1．94±0．86)h和(2．11±0．73)h,Cmax分别为(796．57±336．63)ng·ml-1和(776．30±341．55)ng·ml-1,AUC0→∞分别为(1755．86±1169．44)ng·h·ml-1和(1749．90±1241．7)ng·h·ml-1。受试制剂对参比制剂的相对生物利用度为(105．00±30．08)％。结论:两种制剂具有生物等效性。

Objective： To develop a HPLC method for determination the content of omeprazole capsules in human plasma and study on pharmacokinetics and bioavailability in Chinese healthy volunteers. Method： A randomized two-way cross-over study design was adopted. Twenty-four volunteers were randomly divided in to two groups equally. The plasma concentration of omeprazole capsules were determined by HPLC after a single oral dose of 40mg of two omeprazole formulations respectively, the results were analyzed by program DAS. Result： The concentration-time curves of two omeprazole capsules wrere conformed to the one-compartment open model. The main pharmacokinetic parameters were as follows ： tmax were （ 1.94±0.86） h and （2.11 ±0. 73 ） h, Cmax were （796.57 ±336.63 ） ng·ml^ -1 and （776.30±341.55 ）ng·ml^-1, AUC0→∞ were （ 1755.86±169.44 ） ng·h·ml^-1 and （ 1749.90±1241.73 ） ng·h·ml ^-1 respectively, the relative hioavailahility was （105.00±30.08 ）%. Conclusion： Two formulations were hioequivalent.