Formulation Optimization and Drug Release Evaluation of pH-triggered Colon Specific Pellets of Sophora Flavescens
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Formulation Optimization and Drug Release Evaluation of pH-triggered Colon Specific Pellets of Sophora Flavescens
Chinese Journal of Experimental Traditional Medical FormulaeVol. 17, Issue 4, Pages: 1-4(2011)
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Published:2011
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XIE Xing-liang, YANG Ming, HAN Li, 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:
XIE Xing-liang, YANG Ming, HAN Li, 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:
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 flavescens 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.