奥美拉唑胶囊的人体药代动力学及生物等效性试验研究

目的建立测定奥美拉唑血药浓度的高效液相色谱法,并考察奥美拉唑胶囊人体药代动力学,比较两种制剂的生物等效性。方法采用双周期随机交叉试验设计,18例男性健康志愿者随机分为2组,分别单剂量交叉口服奥美拉唑胶囊(受试制剂)和奥美拉唑肠溶胶囊(参比制剂)40 mg,以反相高效液相色谱法测定给药后不同时间点的奥美拉唑血药浓度,采用DAS房室模型法和生物等效性计算程序进行统计分析。结果奥美拉唑胶囊(受试制剂)和奥美拉唑胶囊(参比制剂)血药浓度-时间曲线符合一室开放模型。主要药动学参数:t1/2分别为(1.76±0.79)h和(1.66±0.52)h,Tmax分别为(2.73±0.35)h和(2.61±0.4)h。Cmax分别为(1 271.09±351.72)ng/mL和(1 219.02±325.53)ng/mL,AUC0→∞分别为(2 941.85±807.18)ng/(h.mL)和(2 960.57±802.91)ng/(h.mL)。受试制剂对参比制剂的相对生物利用度为(99.63±12.04)%。结论受试制剂与对照制剂比较,其奥美拉唑的t1/2、Tmax、Cmax和AUC0→∞均无显著性差异,两种制剂具有生物等效性。

Pharmacokinetics and bioequivalence of omeprazole capsules

Objective To develop a HPLC method for determinating the content of omeprazole capsules in human plasma and study the pharmacolinetics and bioavailability of them.Methods A randomized two-way cross-over study design was adopted.18 volunteers were randomly divided into two omeprazole formulations respectively,the results were analyzed by program DAS 2.0.Results The concentration-time curves of two omeprazole capsules were conformed to the one-compartment open model.The main pharmacokinetic parameters were as follows:T1/2 were(1.76±0.79) h and(1.66±0.52) h,Tmax were(2.73±0.35) h and(2.61±0.4) h,Cmax were(1 271.09±351.72) ng/mL and(1 219.02±325.53) ng/mL,AUC0→∞ were(2 941.85±807.18) ng/(h·mL) and(2 960.57±802.91)ng/(h·mL) respectively.The relative bioequivalence was(99.63±12.04)%.Conclusion The fomulations were bioequivalent.