奥美拉唑的药代动力学及人体生物利用度的研究

Study on the pharmacokinetics and human bioavailability of omeprazole

目的研究奥美拉唑的药代动力学和人体生物利用度。方法１０例男性健康志愿者分别空腹口服国产奥美拉唑肠溶胶囊和洛赛克肠溶胶囊（对照品）２０ｍｇ。以高效液相法测定两药血药浓度。结果经３Ｐ８７软件处理后表明该药的血药浓度－时间曲线符合一级吸收－房室开放模型。主要药代参数如下：Ｔ１２＝（１．６８±１．０５）ｈ，Ｔｍａｘ＝（１．９４±０．２３）ｈ，Ｃｍａｘ＝（１１５７±５９２）ｎｍｏｌ·Ｌ－１，ＡＵＣ＝（３９９８．９５±２２０７．２７）ｎｍｏｌ·Ｌ－１·ｈ－１，ＣＬ／Ｆ（Ｓ）＝（１８．５５±８．２６）Ｌ·ｈ－１，Ｖ／Ｆ（Ｃ）＝（３８．４０±１９．２７）Ｌ。奥美拉唑胶囊相对生物利用度为９２．０９％±１２．００％。结论生物等效性分析证明两药具生物等效性。

AIM To study the pharmacokinetics and human bioavailability of omeprazole. METHOD Ten male healthy volunteers orally took domestic omeprazole entero dissolving capsules and Losec entero dissolving capsules(used as reference ) 20 mg respectively. Blood concentrations of two drugs were tested with HPLC. RESULTS Data were processed by using 3P87 program. The plasma concentration time curves of these two drugs appeared to fit oral first order absorption and one compartment open model. The pharmacokinetic parameters of omeprazole are as follows: T 12 is (1 68±1 05) h, T max is (1 94±0 23) h, C max is ( 1 157 ±592) nmol·L -1 ,AUC is (3 998 95±2 207 27) nmol·L -1 ·h -1 ,CL/ F is (18 54±8 26)L, V/F is (38 40±19 27)L. The relative bioavailability of omeprazole entero dissolving capsule is 92 09%±12 00%. CONCLUSION After analysis, these two drugs have the same bioequivalence.