富马酸替诺福韦二吡呋酯片在健康人体的生物等效性研究  

Bioequivalence of tenofovir disoproxil fumarate tablets in Chinese healthy volunteers

作　　者：王红艳[1] 郎丽巍[1] 朱珍真[1] 陈贞[1] 段峰[1] 姬慧[1] 王敏[1] 张丽[1] 魏振满[1] 

机构地区：[1]中国人民解放军第三〇二医院药物临床试验中心,北京100039

出　　处：《中国临床药理学杂志》2016年第23期2145-2147,共3页The Chinese Journal of Clinical Pharmacology

摘　　要：目的评价富马酸替诺福韦二吡呋酯片在健康人体的生物等效性。方法 22例健康男性受试者随机分成2组,采用随机、开放、双周期自身交叉试验。单剂量口服富马酸替诺福韦二吡呋酯片受试药品和参比药品300 mg,用LC-MS/MS测定血浆中药物浓度,药代动力学参数用DAS 2.1.1软件处理获得。结果受试药品与参比药品的Cmax分别为(281.04±84.77)和(283.86±80.71)ng·mL^(-1),tmax分别为(1.02±0.44)和(0.90±0.41)h,AUC0-t分别为(2351.80±518.1),(2338.98±524.99)ng·h·mL^(-1),AUC0-∞分别为(2574.25±581.07),(2571.42±574.43)ng·h·mL^(-1),相对于参比药品,受试药品的生物利用度F0-t为(102.11±19.76)%。试验期间未发生严重不良事件。结论富马酸替诺福韦二吡呋酯片受试药品和参比药品具有生物等效性。Objective To study the bioequivalence of 2 kinds of tenofovir disoproxil fumarate tablets in Chinese healthy volunteers. Methods According to the two -crossing design,22 healthy male volun- teers were randomly divided into two groups. They were given single oral dose of test and reference preparation of tenofovir disoproxil fumarate tab- let （each 300 mg）. The plasma concentrations were determined by LC-MS/MS. Pharmacokinetic parameters were obtained using DAS 2. 1.1 program. Results The mainpharmacokinetic parameters of tenofovir disoproxil fumarate tablets test and reference were as follows： Cmax were （ 281.04 ± 84. 77 ）, （ 283.86± 80. 71 ） ng· mL^-1 , tmax were （ 1.02 ± 0. 44）, （0. 90 ± 0.41 ） h, AUC0-1 were （2351.80± 518.14 ）, （2338.98 ±524.99） ng · h· mL^-1,AUC0-1 were （2574.25 ±581.07）, （2571.42 ± 574.43） ng · h · mL^-1. The relative bioavailability was （ 102. 11 ± 19.76） % . Conclusion Two kinds of tenofovir disoproxil fumarate tablets are bioequivalent.

关 键 词：富马酸替诺福韦二吡呋酯片 生物等效性 液相色谱串联质谱法 

分 类 号：R969.1[医药卫生—药理学]