替格瑞洛原料药粒径对其片剂体外溶出行为的影响
发布时间：2018-11-06 11:11
【摘要】：目的:研究替格瑞洛原料药粒径对其片剂体外溶出行为的影响。方法:取替格瑞洛原料药及其经粉碎不同时间(15、30、40、60 s)后得到的不同粒径的粉末A、B、C、D、E,以湿法制粒法制备成片剂;采用紫外分光光度法在300 nm波长处测定上述各自制片在60 min内的体外累积溶出度(以0.2%聚山梨酯溶液为溶出介质,桨法),并以原研片为参比制剂,用相似因子(f2)法比较5种自制片与原研片体外溶出行为的相似性。结果:粉末A、B、C、D、E的d(0.9)分别为69.181、40.778、24.805、12.611、3.083μm,f2值分别为27.77、36.79、50.06、67.68、79.99。结论:替格瑞洛原料药粒径越小,所制片剂溶出行为越接近原研片。原料药经粉碎后可显著提高替格瑞洛片的体外溶出度。为获得与原研片生物等效的制剂,建议替格瑞洛原料药粉末粒径分布宜控制在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，
本文编号：2314097
[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，
本文编号：2314097
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