摘要
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。
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 concentratlon-time curves of two omeprazole capsules were conformed to the one-compartment open model. The main pharmacokinetlc 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.
出处
《实用药物与临床》
CAS
2007年第6期374-376,共3页
Practical Pharmacy and Clinical Remedies
