摘要
目的评价国产和进口司他夫定胶囊在健康人体的生物等效性。方法18名健康志愿者自身交叉、单剂量口服司他夫定胶囊参比(40mg)和被试制剂(45mg)后,用高效液相色谱法测定血浆司他夫定浓度。用3P97药代动力学软件进行参数计算及生物等效性评价。结果2种司他夫定的药时曲线均符合一房室模型,参比制剂、被试制剂的主要药代动力学参数如下。Cmax分别为(1033.85±225.63)和(1047.51±282.13)μg·L-1;tmax分别为(0.75±0.21)和(0.96±0.34)h;t1/2ka分别为(0.16±0.16)和(0.38±0.32)h;t1/2ke分别为(1.49±0.22)和(1.38±0.23)h;AUC0-t分别为(2.23±0.40)和(2.33±0.51)mg·h·L-1;AUC0-∞分别为(2.34±0.46)和(2.42±0.54)mg·h·L-1。与参比制剂相比,被试制剂的相对生物利用度F0-t为(94.20±21.13)%,F0-∞为(93.82±21.89)%。结论2种司他夫定胶囊具有生物等效性。
Objective To evaluate the bioequivalence of stavudine capsules in Chinese healthy volunteers. Methods A single oral dose 40 mg and 45 mg of two stavudines, reference and test capsules was given to 18 healthy volunteers in a randomized cross - over study. The concentration of stavudine in plasma were determined by HPLC method with UV detector. Results Finding revealed that the data of two formulations were fitted to a one - compartment open model. The main pharmacokinetic parameters of two formulations, reference and test capsules, were as follws ： Cmax were （ 1033.85 ± 225.63 ） and （ 1047.51 ± 282.13 ） μg · L^ - 1 ; tmax were （ 0.75 ± 0.21 ） and （0.96 ±0.34）h;t1/2kaa were（0.16 ±0.16）and（0.38 ±0.32） h;t1/2ke were （1.49±0.22） and （1.38±0.23）h; AUC0-t were （2.23±0.40） and （2.33±0.51） mg· h· L^-1;AUC0-∞ were （2.34±0.46） and （2.42± 0.54） mg· h · L^-1, respectively. The relative bioavalability of F0-t and F0-∞ were （94.20±21. 13）% and （93.82 ±21.89）%, respectively. Conclusion The results of ANOVA and two one - sided t test statistical analysisshowed that two formulations were bioequivalent.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2005年第4期275-278,共4页
The Chinese Journal of Clinical Pharmacology
