阿尼西坦胶囊的相对生物利用度研究

目的 研究阿尼西坦胶囊的相对生物利用度。方法 12 名志愿受试者单剂量口服400 mg 阿尼西坦胶囊供试品与标准参比制剂三乐喜后, 采用反相高效液相色谱法, 测定阿尼西坦主要活性代谢产物对甲氧基苯甲酰氨基丁酸(ABA) 的血药浓度经时变化情况, 使用3p87 软件计算药代动力学参数, 并进行统计学分析。结果 受试药(T) 与参比药(R) 的药-时曲线下面积(AUC_0~t) 分别为(781.0 ±169.5) 和(792.3 ±156.6) μg·min ·ml^-1, 实测达峰时间(t_max) 分别为(40.9 ±9.7) 和(37.3 ±11.5) min, 实测峰浓度(c_max) 分别为(10.4 ±3.0) 和(10.5 ±3.0) μg·ml^-1。配对t 检验结果表明, 两制剂的AUC_0~t、c_max及t_max均无显著性差异(P >0.05), 生物等效性检验结果, 两制剂的A UC_0~t、c_max有显著性差异(P <0.05)。阿尼西坦胶囊的相对生物利用度(F) 为(99.4 ±14.4) %。结论 阿尼西坦胶囊和三乐喜为生物等效制剂。

Study on relative bioavailability of aniracetam capsules

Aim The relative bioavailabilities of aniracetam capsules were studied. Methods The blood concentrations of the main metabolite of aniracetam, Nanisoyl- GABA (ABA), were determined by RPHPLC after a single oral dose of 400 mg aniracetam of test(capsules) or reference(capsules) drugs was given separately to 12 volunteers in an open randomized cross-over test. Statistical software’s 3p87 w ere used for the calculation of results. Results After taking a single oral dose of 400 mg aniracetam test capsules and reference capsules, thd AUC_0~t of aniracetam of the two formulations were (781.0 ±169.5) μg·min· ml^-1 and (792.3 ±156.6) μg·min·ml^-1; t_max were (40.9 ±9.7) min and (37.3 ±11.5) min; c_max of ABA were (10.4 ±3.0) μg ·ml -1 and (10.5 ± 3.0) μg ·ml^-1. The result s of statistical analysis showed that there were no significant difference in the AUC_0~t, t_max and c_max of ABA between the formulations (P <0.05). The relative bioavailability of aniracetam capsule was (99.4 ±14.4) %. Conclusion The two aniracetam capsules were bioequivalent.