摘要
目的研究司他夫定片剂的健康人体药动学和相对生物利用度。方法采用高效液相色谱法测定20名健康志愿者自身交叉、单剂量口服司他夫定胶囊和片剂各40mg后血浆司他夫定浓度。用3P97药动学软件进行药动学参数计算及生物等效性评价。结果两种司他夫定的药-时曲线均符合一房室模型,参比制剂、被试制剂的主要药动学参数如下:ρ_(max)分别为(1.01±0.24)和(0.95±0.30)mg·L^(-1);t_(max)分别为(0.78±0.22)和(0.70±0.21)h;t_(1/2ke)分别为(1.47±0.22)和(1.47±0.23)h;AUC_(0～t)分别为(2.21±0.46)和(2.08±0.53)mg·h·L^(-1);AUC_(0～∞)分别为(2.33±0.53)和(2.16±0.58)mg·h·L^(-1)。与标准参比制剂相比,被试制别的相对生物利用度F_(0～t)为(97.02±27.71)%,F_(0～∞)为(96.33±29.51)%。对两制剂间的AUC_(0～t)、AUC_(0～∞)和ρ_(max)进行双向单侧t检验,表明两种制剂具有生物等效性。结论司他夫定胶囊和片剂具有生物等效性。
OBJECTIVE To evaluate the pharmacokinetics and relative bioavailability of two stavudine preparations in healthy volun- teers. METHODS A single oral dose 40 mg of stavudine preparations, capsule and tablet, was given to 20 healthy volunteers in a randomized cross-over study. The concentration of stavudine in plasma was determined by HPLC method with UV detector. RESULTS The concentration- time curves were fitted to a one-compartment open model. The main pharmacokinetic parameters of stavudine capsule and tablet were as follows： ρmax were（ 1.01 ± 0.24） and（0.95 ± 0.30）mg·L^-1 ; tmax were（0.78 ± 0.22） and（0.70 ± 0.21）h; t1/2ke were （1.47 ± 0.22） and （1.47 ± 0.23）h; AUCo-t were （2.21 ± 0.46） and （2.08 ± 0.53） mg·h·L^-1 ;AUC0～∞ were （2.33 ± 0.53） and （2.16 ± 0.58） mg·h·L^-1.The relative bioavalability of F0-∞ and F0- ∞ were （97.02±27.71）% and （96.33 ± 29.51）%, respectively. The results of ANOVA and two onesided t test statistical analysis showed that two formulations were bioequivalen/. CONCLUSION The results showed that two stavudine preparations were biomuivalent.
出处
《中国药学杂志》
EI
CAS
CSCD
北大核心
2005年第21期1650-1652,共3页
Chinese Pharmaceutical Journal
