奥美拉唑肠溶胶囊的生物等效性研究

目的:研究奥美拉唑肠溶胶囊在健康人体的药代动力学,并评价其与同剂量制剂间的生物等效性。方法:采用双交叉试验设计,18名健康志愿者口服奥美拉唑肠溶胶囊试验和参比制剂40 mg,服药后0~12 h内间隔取血,用HPLC法测定血药浓度。计算主要药代动力学参数,并以参比制剂计算奥美拉唑肠溶胶囊的相对生物利用度,判断其生物等效性。结果:奥美拉唑肠溶胶囊试验和参比制剂的体内药代动力学参数Cmax(0.632±0.383)mg/L和(0.626±0.415)mg/L、5Tmax(2.39±0.40)h和(2.33±0.42)h、T1/2(1.92±0.64)h和(2.01±0.73)h、Vd/F(81.21±46.68)L和(94.07±89.46)L、CL/F(32.99±20.92)L/h和(31.68±20.41)L/h、AUC0→12(2.03±1.99)mg/(h.L)-1和(1.89±1.62)mg/(h.L)-1;受试奥美拉唑肠溶胶囊的相对生物利用度F=(104.7±17.7)%。结论:2种制剂具有生物等效性。

Bioequivalence of omeprazole enteric capsule

Objective: To evaluate the pharmacokinetics and bioequivalence of omeprazole enteric capsule in heslthy Chinese.Methods: Randomized cross-over design was adopted,18 healthy subjects took omeprazole enteric capsule and reference preparation 40 mg orally in one time.Serial blood samples were collected at scheduled intervals during 12 h.The samples were analyzed for omeprazole and reference preparation concentration in plasma by HPLC.The main pharmacokinetics parameters of the omeprazole and reference preparation were Calculated and analyzed.Results: The main pharmacokinetic parameters in test and reference preparation were following accordingly: Tmax were 2.39±0.40 and 2.33±0.42 h;Cmax were 0.632±0.383 and 0.626±0.415 mg/L;T1/2 were 1.92±0.64 and 2.01±0.73 h;Vd/F were 81.21±46.68 and 94.07±89.46 L;CL/F were 32.99±20.92 and 31.68±20.41 L/h;AUC0→12 were 2.03±1.99 and 1.89±1.62 mg/(h·L)-1.The relative bioavailability of omeprazole was 104.7±17.7%.Conclusion: The two omeprazole preparations are bioequivalent.