XIE Xing-liang1, YANG Ming2, HAN Li3, et al. Formulation Optimization and Drug Release Evaluation of pH-triggered Colon Specific Pellets of Sophora Flavescens[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(4): 1-4.
XIE Xing-liang1, YANG Ming2, HAN Li3, et al. Formulation Optimization and Drug Release Evaluation of pH-triggered Colon Specific Pellets of Sophora Flavescens[J]. Chinese journal of experimental traditional medical formulae, 2011, 17(4): 1-4. DOI: 10.13422/j.cnki.syfjx.2011.04.079.
Formulation Optimization and Drug Release Evaluation of pH-triggered Colon Specific Pellets of Sophora Flavescens
摘要
目的:筛选确定pH敏感型苦参结肠靶向微丸的制剂处方
评价其释药性能。方法:采用挤出-滚圆法制备丸芯
以圆整度、脆碎度、得率、粒度分布、溶出度为评价指标
对丸芯处方进行筛选。采用流化床包衣技术
以释药性能为评价指标
对pH敏感包衣处方进行筛选
以浆法对包衣微丸的体外释药性能进行评价。结果:以主药4倍量的微晶纤维素为稀释剂
加入6%羧甲基淀粉钠混匀
加入28%水润湿
制软材
挤出滚圆得丸芯;以Eudragit S100为膜控材料
加入25%滑石粉
20%柠檬酸三乙酯
以95%乙醇为溶剂
配制包衣液
包衣使丸芯增重30%
得包衣微丸。该微丸在人工胃液、小肠液中苦参碱、氧化苦参碱的累积泄漏率为21.6%
结肠液中累积释放率达95.3%。结论:拟定了苦参结肠靶向微丸的制剂处方
制备得微丸质量稳定
具有良好结肠靶向释药性能。
Abstract
Objective:To optimize the prescription of pH-triggered colon specific pellets of Sophora flaves-cens to evaluate drug release.Method: The pellet core was prepared by extrusion-spheronization method
taking sphericity
friability
yield
particle size distribution and dissolution as index to optimize the prescription of the pellet core.The prescription of pH-triggered coat was optimized by fluidized bed coating technology with drug release as index.The drug release in vitro was evaluated with paddle method.Result:The pellet core was prepared by extrusion-spheronization method with 4 times principal agent cellulose microcrystalline as diluent
6% CMS-Na and 28% water added to prepare soft material.The coat solution was prepared with Eudragit S100 as film-forming agent
95% alcohol as solvent
25% talcum powder and 20% triethyl citrate added.The accumulation leakage ratio of matrine and oxymatrine from the coat pellets in gastric juice and small intestinal juice in vitro was 21.6%
and 95.3% in colon juice.Conclusion:The prescription of pH-triggered colon specific pellets of Sophora flavescens was made;the quality of pellets was stable and the drug release of colon target was satisfactory.