口服5-单硝酸异山梨醇酯胶囊和进口片剂在健康志愿者的药代动力学和生物等效性

PHARMACOKINETICS AND BIOEQUIVALENCE OF DOMESTIC CAPSULE AND IMPORTED TABLET OF ISOSORBIDE 5-MONONITRATE IN HEALTHY VOLUNTEERS AFTER ORAL DOSING

目的：研究国产5－单硝酸异山梨醇酯（IS－5－MN）胶囊及进口IS－5－MN片剂在健康志愿者的药动学特征及其生物等效性。方法：随机双盲实验先后一次口服IS－5－MN胶囊和进口IS－5－MN参比片剂（20mg）后，以高效气相色谱法时检测其血药浓度，采用CAPP软件包计算药动学参数，并做生物等效性分析。结果：一次口服胶囊和片剂的药动学符合二室开放模型，其主要药动学参数Cmax分别为（477．7±103．9）μg／L和（468．1±107．8）μg／L，Tmax分别为（0．77±0．36）h和（0．84±0．24）h，t1／2β分别为（6．99±0．71）h和（7．02±0．51）h（P＞0．05）；胶囊的相对生物利用度为（106．1±10．1）％。结论：两种制剂生物等效。

To study the pharmacokinetics of domestic capsules and imported tablets of IS-5-MN in healthy volunteers and to determine the bioequivalence of the drug. METHODS:A single dose of 20 mg of the drug was given in a randomized two-period crossover study. Plasma drug concentration was assayed by GC with capillary columns. The data were processed with CAPP Cpharmacokinetic pharmacodynamic procedure and the bioequivalence was calculated. RESULTS: The concentration-time courses after medication conformed to a two-compartment open model. The Cmax of domestic capsules and imported tablets were (477. 7±103. 9 ) μg/L and (468. 1±107. 8) μg/L respectively; the Tmax of the above two preparations were (0. 77±0. 36 ) h and (0. 84±0. 24) h respectively and their elimination t1/2 were (6. 99±0. 71 ) h and (7. 02±0. 51 ) h respectively. The difference of the main pharmacokinetic parameters between the two formulations was nonsignificant (P> 0. 05 ).The relative bioavalability of domestic capsules vs imported tablets was (106. 1±10. 1) %. CONCLUSION: These two preparations were bioequivalent.