發(fā)布時間：2018-11-06 11:11

【摘要】：目的:研究替格瑞洛原料藥粒徑對其片劑體外溶出行為的影響。方法:取替格瑞洛原料藥及其經粉碎不同時間(15、30、40、60 s)后得到的不同粒徑的粉末A、B、C、D、E,以濕法制粒法制備成片劑;采用紫外分光光度法在300 nm波長處測定上述各自制片在60 min內的體外累積溶出度(以0.2%聚山梨酯溶液為溶出介質,槳法),并以原研片為參比制劑,用相似因子(f2)法比較5種自制片與原研片體外溶出行為的相似性。結果:粉末A、B、C、D、E的d(0.9)分別為69.181、40.778、24.805、12.611、3.083μm,f2值分別為27.77、36.79、50.06、67.68、79.99。結論:替格瑞洛原料藥粒徑越小,所制片劑溶出行為越接近原研片。原料藥經粉碎后可顯著提高替格瑞洛片的體外溶出度。為獲得與原研片生物等效的制劑,建議替格瑞洛原料藥粉末粒徑分布宜控制在d(0.9)≤20μm。
[Abstract]:Aim: to study the effect of the particle size of tigrilol on the dissolution behavior of tigrilol tablets in vitro. Methods: the tablets were prepared by wet granulation method by taking tigrilol and its powder with different particle size after being pulverized at different time (1530 ~ 4060 s). UV spectrophotometry was used to determine the in vitro dissolution of the respective tablets at the wavelength of 300 nm (using 0.2% polysorbate solution as the dissolution medium, paddle method), and the original laminated tablets were used as reference preparation. Similarity factor (f 2) method was used to compare the similarity of dissolution behavior between 5 kinds of homemade tablets and original tablets in vitro. Results: the d _ (0.9) of the powder of Amphixobenzylcholine was 40.778 ~ 24.805 ~ (12.611113.083) 渭 m F _ 2 = 27.777 ~ 36.79 ~ 50.06 ~ (67.68) ~ 79.99, respectively, and the d _ (0.9) of the powder was 69.181U _ (40.778) ~ 24.805 ~ 12.61111 ~ 3.083 渭 m ~ (-1). Conclusion: the smaller the particle size of tigrilol, the closer the dissolution behavior of the tablets is. The dissolution rate of tigrilol tablets was significantly increased after crushing. In order to obtain the bioequivalent preparation, it is suggested that the particle size distribution of tigrilol powder should be controlled at d (0.9) 鈮，

本文編號：2314097