奥美拉唑肠溶胶囊人体生物等效性研究

Study on Bioavailability and Pharmacokinetics of Omeprazole Enteric-coated Capsules experiments

目的 进行试验制剂奥美拉唑肠溶胶囊与参比制剂奥美拉唑肠溶胶囊的单剂口服双交叉试验，研究其药代动力学和生物等效性。方法 健康志愿者18名，随机分为2组，随机交叉自身对照，HPE法测定奥美拉唑经时血浓度，数据经DAS程序处理，得奥美拉唑肠溶胶囊药动学参数。结果 试验制剂奥美拉唑肠溶胶囊主要药动学参数T1／2为（1．564±0．30）h；Tmax为（2．254±0．49）h，Cmax为（1．514±0．56）mg·L^-1；AUC0→10为（3．274±1．87）mg·h·L^-1；AUC0→∞为（3．334±1．91）mg·L^-1·h；相对生物利用度17为（100．79．4±14．54）％。参比制剂奥美拉唑肠溶胶囊主要药动学参数T1／2为（1．564±0．23）h，Tmax为（2．084±0．43）h，Cmax为（1．514±0．68）mg·L^-1，AUC0→10为（3．214±1．64）mg·L^-1·h，AUC0→∞为（3．304±1．71）mg·L^-1·h。试验制剂与参比制剂AUC0→∞、AUC0→24、Tmax、T1／2、Cmax方差分析、双向单侧t检验显示，主要药动学参数周期间、剂型间无显著性差异（P〉0．05）。结论 奥美拉唑肠溶胶囊试验制剂与参比制剂具有生物等效性。

Aim To evaluate bioequivalence of Omeprazole enteric-coated capsules and Omeprazole reference entericcoated capsules with crossover design experiments. Methods A single oral dose of Omeprazole test and reference were given to 18 healthy volunteers in a randomized crossover study. The serum concentrations of Omeprazole enteric-coated capsules and reference were determined by HPLC coupled with a UV detector and their pharmacokinetic parameters were obtained after the data were calculated with ＂Drug And Statistics Ver 1＂. Results The pharmacokinetic parameters of Omeprazole capsules and reference were as follows： T 1/2 （1.56 ± 0.30）h and（ 1.56 ± 0.23）h. T max was （2.25 ± 0. 49）h and（2.08 ±0.43h）h. Cmax was（1.51 ±0.56）mg·L^-1 and （1.51 ±0.68）mg·L^-1.AUC0→24 was（3.27± 1.87） mg·L^-1·h and （3.21 ± 1.64）mg·L^-1 ·h. AUC0→∞ was（3.33 ± 1.91）mg·L^-1·h and （3.30 ± 1.71）mg·L^-1·h.Relatire bioavailability F was （ 100.79 ± 14.54） % respectively. Variance analysis and two one-sided test show no significant difference between periods, individuals and preparations. Conclusions Omeprazole enteric-coated capsules tests and reference were bioequivalent.