国产与进口阿那曲唑片在健康人体生物等效性研究  

Study on Bioequivalence of Domestic and Imported Anastrozole Tablets in Healthy Volunteers

作　　者：赵春艳[1] 姜春梅[1] 

机构地区：[1]辽宁中医药大学附属第二医院I期临床试验病房,辽宁沈阳110034

出　　处：《肿瘤药学》2014年第2期144-152,共9页Anti-Tumor Pharmacy

摘　　要：目的研究国产阿那曲唑片在人体内的生物利用度,并与参比制剂比较,评价两者生物等效性。方法 20名健康男性志愿者随机口服国产阿那曲唑片(受试制剂)或进口阿那曲唑片(参比制剂)1 mg后,采用高效液相色谱串联质谱法测定不同时刻血浆中阿那曲唑的浓度,用WinNonlin 5.2.1数据统计软件计算药代动力学参数,并评价其生物等效性。结果单次口服国产阿那曲唑片1 mg或参比制剂1 mg后,受试制剂和参比制剂的Tmax分别为(1.45±0.5)h和(1.50±0.63)h,Cmax分别为(16.962±4.291)ng·mL-1和(15.928±3.799)ng·mL-1,T1/2分别为(40.00±7.27)h和(42.50±10.81)h,用梯形法计算,AUC0-t分别为(722.7±139.6)ng·h·mL-1和(730.3±138.6)ng·h·mL-1,AUC0-∞分别为(791.8±149.3)ng·h·mL-1和(807.5±156.6)ng·h·mL-1。经方差分析、双单侧t检验和[1-2α]%置信区间法进行生物等效性评价。结果表明,受试制剂与参比制剂间各药动学参数的差异无统计学意义(P>0.05)。结论国产与进口阿那曲唑片在人体内具有生物等效性。Objective To study the relative bioavailability of domestic Anastrozole Tablets in healthy volunteers and evaluate the bioequivalence of the domestic and imported Anastrozole Tablets. Methods A randomized crossover design was performed in 20 healthy male volunteers. A single oral dose of 1 mg domestic Anastrozole tablets （test formulation） or imported Anastrozole tablets （reference formulation） was administrated. Plasma concentrations of Anastrozole were measured by high liquid chroma-tography mass spectrometry （HLC-MS）. The pharmacokinetic parameters were calculated by WinNonlin 5.2.1 software and the bioequivalence was evaluated. Results After a single oral dose of 1 mg anastrozole of test or reference formulation, the main phar-macokinetic parameters were as follows： Tmax was 1.45±0.56 h and 1.50±0.63 h, Cmax was 16.962±4.291 ng·mL-1 and 15.928 ±3.799 ng·mL-1, t1/2 was 40.00±7.27 h and 42.50±10.81 h, AUC0-t was 722.7±139.6 ng·h·mL-1 and 730.3±138.6 ng·h·mL-1, AUC0-∞was 791.8±149.3 ng·h·mL-1 and 807.5±156.6 ng·h·mL-1, respectively. There was no significant difference between the two formulations in the pharmaeokinetic parameters by variance analysis, two one sided t-test and[1-2α]%confidence interval method （P〉0.05）. Conclusion Domestic and imported Anastrozole tablets are bioequivalent in healthy volunteers.

关 键 词：阿那曲唑片 高效液相色谱串联质谱法 生物等效性 药代动力学 

分 类 号：R73-3[医药卫生—肿瘤]