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目的采用高效液相色谱法测定受试者口服埃索美拉唑肠溶胶囊与埃索美拉唑镁肠溶片后血药浓度,评价埃索美拉唑肠溶胶囊的生物等效性。方法 2009年9月-10月,36例健康男性受试者单次交叉口服埃索美拉唑肠溶胶囊(试验制剂)和埃索美拉唑镁肠溶片(参比制剂),测定给药后不同时间点血浆中埃索美拉唑经时血药浓度,采用DAS 2.0软件进行药物代谢动力学参数计算和生物等效性评价。结果受试者单次口服试验制剂与参比制剂后,达峰时间分别为(2.19±0.96)、(2.43±0.92)h,峰浓度分别为(1 748.86±615.81)、(1 442.92±476.41)μg/L,药时曲线下面积(AUC)0-t分别为(3 927.14±1 839.10)、(3 878.79±1 734.84)μg/L.h,AUC0-∞分别为(3 998.36±1 866.22)、(3 918.31±1 773.44)μg/L.h。试验制剂与参比制剂的生物等效性为94.0%,其90%CI为(82.3%,107.2%)。结论埃索美拉唑肠溶胶囊与埃索美拉唑镁肠溶片生物等效。
Objective To determine the bioequivalence of esomeprazole enteric-coated capsules by HPLC after oral administration of esomeprazole enteric-coated capsules and esomeprazole magnesium enteric-coated tablets. Methods From September to October 2009, 36 healthy male subjects received oral administration of esomeprazole enteric-coated capsules (test preparations) and esomeprazole magnesium enteric-coated tablets (reference preparations) in a single crossover test The plasma concentration of esomeprazole in plasma at different time points after drug administration was used to calculate the pharmacokinetic parameters and evaluate the bioequivalence using DAS 2.0 software. Results The peak time of single oral test formulation and reference formulation was (2.19 ± 0.96) and (2.43 ± 0.92) h, respectively. The peak concentrations were (1 748.86 ± 615.81) and (1442.92 ± 476.41) (AUC) 0-t were (3 927.14 ± 1 839.10), (3 878.79 ± 1 734.84) μg / Lh, AUC0-∞ were (3 998.36 ± 1 866.22) and 3 918.31 ± 1 773.44) μg / Lh. The bioequivalence of the test and reference formulations was 94.0% with a 90% CI of (82.3%, 107.2%). Conclusion Esomeprazole enteric-coated capsules are bioequivalent to esomeprazole magnesium enteric-coated tablets.