阿德福韦酯胶囊人体生物等效性研究  

Bioequivalence of Adefovir Dipivoxil Capsules in Healthy Volunteers

作　　者：孙斌[1] 毕京峰[1] 李文淑[1] 王敏[1] 段锋[1] 朱珍真[1] 屠舒[1] 魏振满[1] 

机构地区：[1]解放军第302医院新药临床试验中心,北京100039

出　　处：《中国医院用药评价与分析》2012年第10期927-929,共3页Evaluation and Analysis of Drug-use in Hospitals of China

摘　　要：目的:评价国产阿德福韦酯胶囊与进口阿德福韦酯片(贺维力)的生物等效性。方法:20位健康男性志愿者随机交叉口服单剂量受试制剂(阿德福韦酯胶囊)和参比制剂(贺维力);用LC-MS/MS法,分别测定药物血浆浓度,DAS2.0计算药代动力学参数,评价生物等效性。结果:受试制剂和参比制剂的主要药代动力学参数,AUC0-t分别为(207.92±45.80)ng.h-1.mL-1和(221.25±54.18)ng.h-1.mL-1,AUC0-∞分别为(217.16±45.93)ng.h-1.mL-1和(230.63±53.80)ng.h-1.mL-1,Cmax分别为(17.61±3.21)ng.mL-1和(19.76±4.64)ng.mL-1,Tmax分别为(1.70±0.64)h和(1.33±0.61)h,t1/2分别为(8.10±1.12)h和(8.11±1.34)h。AUC0-t、AUC0-∞和Cmax90%可信区间分别为89.8%～99.2%、90.2%～98.9%和82.4%～98.0%;相对生物利用度为(95.1±11.9)%(以AUC0-t计)、(95.1±11.1)%(以AUC0-∞计)。结论:2种制剂具有生物等效性。OBJECTIVE：To study the bioequivalence of adefovir dipivoxil capsules in healthy volunteers.METHODS：A single oral dose of tested（adefovir dipivoxil capsules） and reference（Hepsera） formulation were given to 20 healthy volunteers in a randomised crossover study.The concentrations of adefovir in plasma were determined by LC-MS/MS.The pharmacokinetic parameters were calculated and the bioavailability and bioequivalence of adefovir were evaluated by DAS 2.0 program.RESULTS：After a single dose,the pharmacokinetic parameters for adefovir were as follows： AUC0-t were（207.92±45.80）ng·h-1·mL-1 and（221.25±54.18）ng·h-1·mL-1,AUC0-∞ were（217.16±45.93）ng·h-1·mL-1 and（230.63±53.80）ng·h-1（mL-1,Cmax were（17.61±3.21）ng·mL-1 and（19.76±4.64）ng·mL-1,Tmax were（1.70±0.64）h and（1.33±0.61） h,t1/2 were（8.10±1.12） h and（8.11±1.34）h for tested and reference formulation,respectively.The 90% CIs for the ratios of AUC0-t,AUC0-∞,Cmax were 989.8%-99.2%、90.2%-98.9%和82.4%-98.0%,respectively.The relative bioavailability was（95.1±11.9）%（for AUC0-t）、（95.1±11.1）%（for AUC0-∞）.CONCLUSION：The results of the statistic analysis showed that the two formulations were bioequivalence.

关 键 词：阿德福韦酯 LC-MS MS 生物等效性 

分 类 号：R965[医药卫生—药理学]