【摘要】：目的:以市售馬來酸氟吡汀膠囊為參比制劑,評價自制馬來酸氟吡汀滴丸的相對生物利用度。方法:采用高效液相色譜法測定馬來酸氟吡汀緩釋滴丸和膠囊劑單劑量灌胃(ig)給藥后大鼠的血藥濃度變化,DAS 2.0軟件計算分析其藥動學參數(shù)和相對生物利用度。結(jié)果:馬來酸氟吡汀自制緩釋滴丸與市售膠囊的藥動學參數(shù)間均有顯著性差異,其中:Tmax分別為(3.400±0.548)和(2.200±0.447)h;Cmax分別為(3.996±0.199)和(3.236±0.141)μg·m L-1,在膠囊劑達峰時間T2.2h處Cmax(滴丸)遠大于Cmax(膠囊);AUC0~∞分別為(48.503±2.749)和(33.889±3.195)μg·m L-1·h;MRT分別為(9.212±1.752)和(7.160±0.563)h,馬來酸氟吡汀緩釋滴丸相對于膠囊劑的生物利用度為(144.388±18.400)%。結(jié)論:同樣劑量給藥,馬來酸氟吡汀滴丸較市售膠囊血濃度高、起效快、藥效作用時間長、生物利用度高,可以為馬來酸氟吡汀滴丸的藥效學實驗及緩釋制劑的研發(fā)提供參考。
[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 鹵0.548) h and (2.200 鹵0.447) h, respectively. Cmax was (3.996 鹵0.199) 渭 g ml ~ (-1) and (3.236 鹵0.141) 渭 g mL ~ (-1) respectively. Cmax (dropping pills) was much larger than Cmax (capsule) at T2.2 h. AUC0~ 鈭，

本文編號：2316663