摘要
目的:制备5-氨基水杨酸结肠定位缓释微丸胶囊,建立其体外药物释放度分析方法,并研究其体外释放行为。方法:以挤出滚圆法制备微丸丸芯,采用Mini-glatt流化床进行包衣,研究了不同型号MCC、HPMC、硬脂酸镁、枸橼酸、Eudragit NE30D及其用量、包衣增重等对体外释放的影响,采用转篮法[100r·min^(-1),(37±0. 5)℃]测定5-氨基水杨酸结肠定位缓释微丸的体外释放度;以f_2相似因子法评价3批自制制剂与对照制剂Apriso^(TM)的释放相似性。结果:成功筛选出了合理、科学的处方,制备了均一、可控的5-氨基水杨酸结肠定位缓释微丸胶囊。在pH 6. 0 PBS,pH 6. 8 PBS与pH 7. 4 PBS中,自制3批制剂与对照制剂的释放度f_2值均大于50,且释放度无显著性差异(P> 0. 05),重复性良好。结论:该制备方法可行,建立的释放度测定方法操作简便、准确;自制制剂有结肠定位缓释功能,减少了给药次数,增强了患者的顺应性。
Objective: To prepare 5-amino salicylic acid colon specific sustained-release pellet capsules,establish drug release analysis method and study its release behavior in vitro. Methods: The cores of pellet were prepared by extrusion circle method and coated with mini-glatt fluidized bed. The effects of different types of MCC,HPMC and their dosages,dosages of magnesium stearate,citric acid,eudragit NE30D and gaining of coating weight were studied. The release of 5-amino salicylic acid colon specific sustained-release capsules was measured by basket method (100 RMP,37 ± 0. 5 ℃),and the similarity between three batches of self-made preparations and reference pellet capsules AprisoTMwas evaluated by f2 similarity factor method. Results: A reasonable and scientific prescription was successfully screened. Uniform and controllable 5-amino salicylic acid colon specific sustained release pellet capsules were prepared. In pH 6 PBS,pH 6. 8 PBS and pH 7. 4 PBS,the f2 values of the release of three batches of self-made preparations with the original preparation were all greater than 50,the release rates were not significantly different (P > 0. 05),and the reproducibility was good. Conclusion: The established preparation method for 5-amino salicylic acid colon specific sustained release pellet capsules is feasible,simple and accurate.The self-made preparation has the properties of colon-localization and sustained-release,which can reduce the frequency of dosing and enhance patients’ compliance.
作者
钟应淮
刘雪梅
莫传丽
陈挺
唐翠
ZHONG Ying-huai;LIU Xue-mei;MO Chuan-li;CHEN Ting;TANG Cui(Guangxi University of Traditional Chinese Medicine,Nanning 530001,China;Pei Li(Nanning)Pharmaceutical Co.,Ltd.,Nanning 530007,China;Shanghai Zhitong Pharmaceutical Science and Technology Co.,Ltd.,Shanghai 201203,China;School of Life Sciences,Fudan University,Shanghai 200433,China)
出处
《中国新药杂志》
CAS
CSCD
北大核心
2019年第4期492-500,共9页
Chinese Journal of New Drugs
关键词
5-氨基水杨酸
结肠定位
缓释微丸
挤出滚圆
释放度
WEIBULL分布
5-amino salicylic acid
colon specific
sustained release pellet
extrusion round rolling
release degree
Weibull distribution
