国产与进口奥美拉唑肠溶胶囊在健康人体内的药代动力学和生物等效性研究

Pharmacokinetics and Bioequivalence of Imported and Domestic Omeprazole Enteric-Coated Capsules in Healthy Human Body

目的探讨奥美拉唑肠溶胶囊在健康人体内的药代动力学。方法20名健康志愿者随机单剂量交叉口服国产或进口奥美拉唑肠溶胶囊60mg,采用高效液相色谱法测定其血浆中药物浓度,3P97软件计算药代动力学参数,t检验比较两种制剂的药代动力学参数。结果国产与进口奥美拉唑肠溶胶囊的药-时曲线符合一室模型,达峰时间分别为(2.30±0.73)h和(2.20±0.89)h,峰浓度分别为(2.19±1.53)μg/mL和(2.13±1.48)μg/mL,0-t药时曲线下面积分别为(7.18±6.86)μg·h/mL和(6.93±6.37)μg·h/mL,国产制剂相对于进口制剂的生物利用度为(95.54±10.99)%,经配对t检验、方差分析、双单侧t检验及(1-2α)置信区间法统计分析,各药代动力学参数两种制剂间无显著差异(P>0.05),具有生物等效性。结论国产与进口奥美拉唑肠溶胶囊具有相同的体内过程。

Objective To observe the pharmacokinetics of omeprazole （OME） enteric-coated capsules. Methods 20 healthy volunteers were given the single dose of 60 mg OME enteric- coated capsules （domestic and imported） according to the randomized cross- over design. The plasma concentrations of OME were determined by HPLC. The pharmacokinetic parameters as well as relative bioavailability were measured by 3P97 software. Results The concentration-time curves of both preparations fitted to a one- compartment model, tmax were （2.30 ± 0.73）h and （2.20±0.89）h, Cmax were （2.19±1.53）μg/mL and （2.13 ± 1. 48） μg/mL, AUC0-t, were （7.18±6.86） μg· h/mL and （6.93 ±6.37）μg·h/mL, respectively. There was no significant difference between the two kinds of enteric-coated capsule in tmax, Cmax, AUC0-t.The relative bioavailability of domestic enteric-coated capsules was （95.54 ± 10. 99）% compared with imported enteric-coated capsules. Conclusion The results of the statistical analysis show that the two kinds of omeprazole enteric- coated capsules are bioequivalent.