厄贝沙坦片的人体生物等效性研究

目的：研究厄贝沙坦片在健康人体的药动学和相对生物利用度,并与市售厄贝沙坦片比较,进行生物等效性评价。方法：24例男性健康受试者双周期、随机、交叉、单剂量口服厄贝沙坦受试制剂和参比制剂各0.15g,清洗期为7d,采用LC-MS/MS法测定血浆中厄贝沙坦的浓度。结果：受试制剂与参比制剂主要药动学参数如下：cmax为（1.89±0.54）和（1.99±0.46）μg/ml,tmax为（1.63±0.92）和（1.52±0.83）h,t1/2为（10.9±6.1）和（11.4±7.7）h,AUC0～t为（9.58±2.56）和（8.90±2.87）μg.h.ml-1,AUC0～∞为（10.23±2.98）和（9.56±2.93）μg.h.ml-1。两种制剂主要药动学参数差异无统计学意义（P〉0.05）。受试制剂的相对生物利用度为（110.5±21.6）%。结论：厄贝沙坦片受试制剂和参比制剂具有生物等效性。

Study on bioequivalence of irbesartan tablet in healthy volunteers

Objective： To study the pharmacokinetics and relative bioavailability of irbesartan tablet in healthy volunteers, and evaluate the bioequivalence between two preparations. Methods： Twenty-four healthy male volunteers were enrolled in the study. A single oral dose （0. 15 g） of test and reference tablets were given respectively to the volunteers according to randomized two-way cross-over study design. The washout period was 7 days. The plasma concentration of irbesartan was determined by LC-MS/MS method. Results： The main pharmacokinetic parameters of the test and reference tablets were as follows：cmax（1. 89±0. 54） and （1.99±0.46） μg/ml,tmax （1. 63±0. 92） and （1. 52zk0. 83） h,t1/2 （10. 9± 6. 1） and （11.4± 7.7） h,AUC0-t（9.58±2.56） and （8.90±2.87）μg ± h. ml-1,AUC0-∞（10.23±2. 98） and （9.56±2. 93） μg.h . ml- 1 respectively. There was no significant difference in main pharmacokinetic parameters between the test and reference tablets （P〉0.05）. The relative bioavailability of the test irbesartan was （110. 5 ±21. 6）%. Conclusion： The results of statistical analysis show that the two formulations are bioequivalent.