埃索美拉唑肠溶胶囊人体生物等效性试验

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。

Pharmacokinetic and Bioavailability of Esomeprazole Enteric Capsule In Healthy Volunteers

Objective To study the pharmacokinetic and bioavailability of esomeprazole enteric capsule and esomeprazole enteric tablet in healthy volunteers with high performance liquid chromatography.Methods Thirty-six healthy male volunteers were enrolled in the study during September to October in 2009.The subjects were orally administered a single dose of 40 mg esomeprazole test preparation(capsule) or reference preparation(tablet).The concentrations of plasma esomeprazole were assessed and data were analyzed automatically with DAS 2.0 Pharmacokinetic program.The relative bioavailability of esomeprazole test or reference preparation was calculated.Results The parameters of esomeprazole test or reference preparation were as following: the time to peak plasma concentration was(2.19 ± 0.96) and(2.43 ± 0.92) hours;the peak plasma concentration were(1 748.86 ± 615.81) μg/L and(1 442.92 ± 476.41) μg/L;the area under the plasma concentration-time curve(AUC)0-t were(3 927.14 ± 1 839.10) μg/L.h and(3 878.79 ± 1 734.84) μg/L.h,AUC0-∞ were(3 998.36 ± 1 866.22) μg/L.h and(3 918.31 ± 1 773.44) μg/L.h,respectively.The relative bioavailability of esomeprazole enteric capsule was 94.0% and 90% CI was(82.3%,107.2%).Conclusion Esomeprazole enteric capsule shows a bioequivalence compared with reference preparation.