【作者】 王健；

【导师】 顾景凯；

【作者基本信息】 吉林大学 ， 微生物与生化药学， 2005， 硕士

【摘要】 本试验采用液相色谱-串联质谱（LC-MS-MS）分析方法测定了20 名男性健康受试者随机交叉单剂量口服奥美拉唑肠溶胶囊后不同时刻血浆中奥美拉唑的浓度,绘制血药浓度-时间曲线,并根据血药浓度-时间数据,求算有关药物动力学参数和受试制剂的生物利用度。20 名健康受试者口服受试制剂（相当于奥美拉唑20 mg）和参比制剂（相当于奥美拉唑20 mg）后,血浆中奥美拉唑的T_max分别为2.2±0.6（均值±标准差,下同）和2.4 ±0.8 h;C_max分别为509.6 ±221.4 和524.2 ±195.1 ng/mL;t_1/2 分别为1.7 ±1.2 和1.7 ±1.0 h;采用梯形法计算,AUC_0-t 分别为1414.9 ±1070.3 和1510.5 ±1056.8 ng·h/mL,AUC_0-∞ 分别为1424.8±1082.9 和1529.1 ±1087.4ng·h/mL。以AUC0-t 计算,受试制剂的相对生物利用度为96.7 ±23.5%。主要药动学参数(C_max, AUC_0-t)经对数转换后进行方差分析,并采用双单侧t 检验和（1-2α）置信区间法进行生物等效性评价。结果显示:受试制剂的AUC_0-t的90%置信区间为参比制剂相应参数的85.3～103.5%,Cmax的90%置信区间为参比制剂相应参数的82.1～112.4%。统计分析结果表明:两种制剂具有生物等效性。更多还原

【Abstract】 An analytical method for the determination of pharmacokinetics andbioavailability of omeprazole in human plasma has been developedbased on liquid chromatography with tandem mass spectrometry. Twocapsule formulations of omeprazole have been administered to 20healthy volunteers. Test formulation was provided by Jilin ProvinceNortheast Asia Pharmaceutical Co., Ltd. and standard referenceformulation was Olsten from Shantou Special Economic RegionTuobin Pharmaceutical Factory. The pharmacokinetic parameters andbioavailability were assessed by concentration–time curves.After the administration of test and reference formulation in 20 healthyvolunteers, the T_max of omeprazole was 2.2±0.6 （mean ±sd） and 2.4 ±0.8 h, separately; C_max was 509.6 ±221.4 and 524.2 ±195.1 ng/mL; t1/2was 1.7 ±1.2 and 1.7 ±1.0 h; AUC_0-t was 1414.9 ±1070.3 and 1510.5±1056.8 ng?h/mL; AUC_0-∞ was 1424.8±1082.9 and 1529.1 ±1087.4ng·h/mL. The bioavailability of test formulation calculated by AUC_0-twas 96.7 ±23.5%.The two capsule formulations were found to be equivalent withcalculated 90% confidence intervals for omeprazole/Olsten ratios of更多还原