马来酸氟吡汀缓释滴丸的制备

发布时间：2018-11-28 13:15

【摘要】：目的:制备马来酸氟吡汀缓释滴丸。方法:应用固体分散体技术,以聚乙二醇6000(PEG6000)和硬脂酸(stearic acid,SA)为药物载体,以缓释和速释两部分配比的方式制备马来酸氟吡汀缓释滴丸;采用相似因子法与现有缓释片剂进行体外溶出比较;将体外平均累积释放数据,分别按零级、一级和Higuichi方程进行拟合;通过加速试验和长期实验进行稳定性考察。结果:马来酸氟吡汀缓释滴丸由缓释和速释两部分以3∶1配比组成,速释体外释药90%时间12 min,缓释部分12 min释药30%;自制马来酸氟吡汀缓释滴丸与同等剂量的国外市售缓释片剂相比药物溶出时间短,溶出曲线出现平顶时间较长,对应的释药量较多,两制剂溶出度试验数据统计计算出相似因子f2为65,自制缓释滴丸中马来酸氟吡汀溶出符合一级释药模型;马来酸氟吡汀及其缓释滴丸在密封和40℃条件下稳定性良好,室温可以长时间贮存。结论:自制马来酸氟吡汀缓释滴丸具有良好的释药效果,可较迅速起效和较长时间持续释药,该滴丸新剂型具有进一步研发和临床应用的意义。
[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，

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