摘要
目的:制备布洛芬缓释滴丸,考察其体外累积释放度,并验证药物在基质中存在的状态。方法:以含药量、水溶性与难溶性基质比、硬脂酸与单硬脂酸甘油脂用量比为考察因素,以2 h和10 h累积溶出率的综合评分为评价指标,应用Box-Behnken效应面法筛选布洛芬缓释滴丸的最优处方。采用差示扫描量热法(DSC)考察药物在基质中存在的状态。结果:布洛芬缓释滴丸的最优处方为:含药量10%,水溶性与难溶性基质比为4∶1,硬脂酸与单硬脂酸甘油酯用量比为3∶1。制得的布洛芬缓释滴丸10 h的最大累积溶出率可达78.85%。DSC分析表明,在缓释滴丸中药物结晶峰消失,形成了固体分散体。结论:所制得的布洛芬缓释滴丸具有良好的缓释效果,且制备工艺简单。
Objective： To prepare ibuprofen sustained-release dropping pills, to evaluate the accumulative release percentage in vitro and to study the drug state in the base. Methods： With the drug content, mass ratio of water-soluble base to insoluble base and mass ratio of stearic acid to glyceryl monostearate as the investigation factors, and the comprehensive score of 2-hour and 10-hour cumu- lative dissolution rate as the evaluation index, a Box-Behnken response-surface method was used to screen the optimal formula of ibu- profen sustained-release dropping pills. The drug state in the matrix was examined by differential scanning calorimetry （DSC）. Results： The optimal formula of ibuprofen sustained-release dropping pills was as follows： the drug content of 10%, water-soluble and insoluble matrix ratio of 4 ： 1, and stearic acid and glyeeryl monostearate ratio of 3 ： 1. The maximum cumulative dissolution rate of ibuprofen sustained-release dropping pills was 78.85%. The DSC analysis showed that the drug crystallization peak disappeared in the sustained-release dropping pills, and formed a solid dispersion.. Conclusion： The preparation has good sustained-release effect, and the nreDaration process is sim^le.
作者
申延利
陈昊
宋红新
杜伟霞
贾永艳
Shen Yanli Chen Hao Song Hongxin Du Weixia Jia Yongyan(College of Pharmacy, Henan University of Chinese Medicine, Zhenzzhou 450046. Chin)
出处
《中国药师》
CAS
2017年第6期1012-1016,共5页
China Pharmacist
基金
河南中医学院药学院大学生创新学习项目(编号:YXCX【2015】5)
