齐多夫定片剂人体生物等效性研究

Bioequivalence of zidovudine tablets and capsules in healthy volunteers

目的:研究齐多夫定片剂与胶囊在健康人体的生物等效性。方法:20名健康志愿者采用双周期交叉试验,单剂量空腹口服齐多夫定片剂和胶囊剂各300mg,HPLC法测定其血清中齐多夫定浓度,血药浓度-时间数据经DAS2.0统计软件处理,计算主要药代动力学参数,并进行两种制剂的生物等效性评价。结果:齐多夫定片剂与胶囊的主要药代动力学参数分别为:t1/2(0.909±0.308)h和(0.987±0.234)h、Cmax(1.723±0.870)μg/ml和(1.457±0.578)μg/ml、Tmax(0.90±0.69)h和(0.80±0.41)h、AUC0-8h(2.302±0.503)μg·h-1·ml-1和(2.361±0.567)μg·h-1·ml-1。片剂与胶囊比较相对生物利用度为(100.8±25.8)%。结论:齐多夫定片剂与胶囊具有生物等效性。

Objective： To investigate the bioequivalence of zidovudine tablets and capsules in healthy volunteers, Methods： Twenty volunteers were randomly divided into two groups （ test and reference）, with double cross-over design. The concentration of zidovudine in serum was determined by HPLC, and pharmacokinetic parameters were calculated with DAS 2.0 practical pharmacokinetics program. Results：The pharmacokinetic parameters of zidovudine tablets and capsules were as follows： t1/2 （0. 909±0. 308 ） h and （0. 987 ± 0.234） h, Cmax （ 1. 723 ± 0.870） μg/ml and （ 1. 457 ± 0. 578 ）μg/ml, Tmax （ 0.90 ± 0.69） h and （ 0.80 ± 0.41 ） h, AUC0-8h （ 2. 302 ±0.503）μg·h^-1·ml^-1 and （2. 361 ± 0. 567）μg·h^-1·ml^-1. The relative bioavallbility of zidovudine tablets was （100. 8 ± 25.8） %. Conclusions：The statistical analysis shows that the test and reference preparation are bioequivalent.