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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。
Objective: To prepare flupirtine sustained-release dropping pills. Methods: Solid dispersions were used to prepare flupirtine maleate by PEG6000 and stearic acid (SA) Sustained-release dropping pills; compared with existing sustained-release tablets in vitro dissolution by similarity factor method; the average cumulative release data in vitro were fitted by zero order, first order and Higuichi equation; stabilized by accelerated test and long-term experiment Sexual investigation. Result: Flupirtine maleate sustained-release dropping pills consisted of sustained-release and immediate-release components in a 3: 1 ratio, immediate-release in vitro 90% of the time for 12 min, and sustained- Flupirtine release sustained-release dripping pills with the same dose of commercially available sustained-release tablets compared to the drug dissolution time is short, dissolution curve appeared flat top longer, corresponding to the release of more, two formulations dissolution test Data calculated that the similar factor f2 is 65. The dissolution of flupirtine maleate in self-made sustained-release dropping pills meets the first-order drug release model. Flupirtine and its sustained-release dropping pills are stable at 40 ℃ Good sexual, room temperature can be stored for a long time. Conclusion: Self-made flupirtine sustained-release dropping pills have a good drug release effect, which can be started rapidly and last for a long time. The new dosage form of drip pills has the significance of further research and clinical application.