马来酸氟吡汀滴丸的药动学研究

发布时间：2018-11-07 14:35

【摘要】：目的:以市售马来酸氟吡汀胶囊为参比制剂,评价自制马来酸氟吡汀滴丸的相对生物利用度。方法:采用高效液相色谱法测定马来酸氟吡汀缓释滴丸和胶囊剂单剂量灌胃(ig)给药后大鼠的血药浓度变化,DAS 2.0软件计算分析其药动学参数和相对生物利用度。结果:马来酸氟吡汀自制缓释滴丸与市售胶囊的药动学参数间均有显著性差异,其中:Tmax分别为(3.400±0.548)和(2.200±0.447)h;Cmax分别为(3.996±0.199)和(3.236±0.141)μg·m L-1,在胶囊剂达峰时间T2.2h处Cmax(滴丸)远大于Cmax(胶囊);AUC0~∞分别为(48.503±2.749)和(33.889±3.195)μg·m L-1·h;MRT分别为(9.212±1.752)和(7.160±0.563)h,马来酸氟吡汀缓释滴丸相对于胶囊剂的生物利用度为(144.388±18.400)%。结论:同样剂量给药,马来酸氟吡汀滴丸较市售胶囊血浓度高、起效快、药效作用时间长、生物利用度高,可以为马来酸氟吡汀滴丸的药效学实验及缓释制剂的研发提供参考。
[Abstract]:Aim: to evaluate the relative bioavailability of flupyridine maleate capsules as reference preparation. Methods: the plasma concentrations of flupyridine maleate sustained release dropping pills and capsules were determined by high performance liquid chromatography (HPLC). The pharmacokinetic parameters and relative bioavailability of flupyridine maleate were calculated and analyzed by DAS 2.0 software. Results: there were significant differences in pharmacokinetic parameters between flupidine maleate self-made sustained-release dropping pills and commercial capsules, in which the Tmax was (3.400 卤0.548) h and (2.200 卤0.447) h, respectively. Cmax was (3.996 卤0.199) 渭 g ml ~ (-1) and (3.236 卤0.141) 渭 g mL ~ (-1) respectively. Cmax (dropping pills) was much larger than Cmax (capsule) at T2.2 h. AUC0~ 鈭，

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