【摘要】：目的:制備馬來酸氟吡汀緩釋滴丸。方法:應(yīng)用固體分散體技術(shù),以聚乙二醇6000(PEG6000)和硬脂酸(stearic acid,SA)為藥物載體,以緩釋和速釋兩部分配比的方式制備馬來酸氟吡汀緩釋滴丸;采用相似因子法與現(xiàn)有緩釋片劑進行體外溶出比較;將體外平均累積釋放數(shù)據(jù),分別按零級、一級和Higuichi方程進行擬合;通過加速試驗和長期實驗進行穩(wěn)定性考察。結(jié)果:馬來酸氟吡汀緩釋滴丸由緩釋和速釋兩部分以3∶1配比組成,速釋體外釋藥90%時間12 min,緩釋部分12 min釋藥30%;自制馬來酸氟吡汀緩釋滴丸與同等劑量的國外市售緩釋片劑相比藥物溶出時間短,溶出曲線出現(xiàn)平頂時間較長,對應(yīng)的釋藥量較多,兩制劑溶出度試驗數(shù)據(jù)統(tǒng)計計算出相似因子f2為65,自制緩釋滴丸中馬來酸氟吡汀溶出符合一級釋藥模型;馬來酸氟吡汀及其緩釋滴丸在密封和40℃條件下穩(wěn)定性良好,室溫可以長時間貯存。結(jié)論:自制馬來酸氟吡汀緩釋滴丸具有良好的釋藥效果,可較迅速起效和較長時間持續(xù)釋藥,該滴丸新劑型具有進一步研發(fā)和臨床應(yīng)用的意義。
[Abstract]:Objective: to prepare flupyridine maleate sustained release pills. Methods: flupyridine maleate sustained release dropping pills were prepared by using solid dispersion technique using polyethylene glycol 6000 (PEG6000) and stearic acid (stearic acid,SA) as drug carriers. The method of similarity factor was used to compare in vitro dissolution with the existing sustained-release tablets. The average cumulative release data were fitted according to zero order first order and Higuichi equation respectively. The stability was investigated by accelerated test and long-term experiment. Results: flupyridine maleate sustained release dropping pills consisted of two parts of sustained release and rapid release, which were composed of two parts: 3:1, 90% in vitro release time, 12 min, sustained release part and 30 min drug release. Compared with the same dosage of foreign sustained-release tablets, flupyridine maleate sustained release pills had shorter dissolution time, longer flat-top time and more corresponding release amount. The dissolution test data of the two preparations showed that the similar factor f _ 2 was 65. Flupyridine maleate dissolution in self-made sustained-release dropping pills was in accordance with the first-order release model. Flupyridine maleate and its sustained-release dropping pills were stable at 40 鈩，

本文編號：2362924