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何首乌抗性淀粉促进靶向结肠微丸体外药物释放研究

Study on Resistant Starch of Polygonum Multiflorum for Promoting Drug Release in Vitor of Targeted Colon Pellets

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【作者】 李闻涛; 万科; 杨莹; 阮婧华; 曹佩雪; 杨小生;

【Author】 Li Wentao;Wan Ke;Yang Ying;Ruan Jinghua;Cao Peixue;Yang Xiaosheng;Shaanxi Medical Equipment Quality Supervision and Inspection Institute;Key Laboratory of Chemistry for Natural Products of Guizhou Province and Chinese Academy of Sciences;The First Affiliated Hospital of Guiyang Chinese Medicine University;

【机构】 陕西省医疗器械质量监督检验院; 贵州省中科院天然产物化学重点实验室; 贵阳中医学院第一附属医院;

【摘要】 目的探讨何首乌抗性淀粉(RS)作为靶向结肠微丸材料的可行性。方法考察生理条件下RS与微晶纤维素(MCC)不同比例微丸溶出速率的变化;以苦参碱(MT)为模型药物,挤出滚圆法制备微丸,观察相关指标。结果 RS对微丸的释放有显著的影响。药物体外释放研究表明,当RS/MCC小于0.5时微丸得率、球形和脆碎度分别>80.00%,>0.95,<0.12%。RS高含量的微丸对p H变化和酶解的耐受性显著提高。在微生物大肠杆菌作用下,微丸迅速崩解,在30 min内药物溶出超过82%。结论何首乌抗性淀粉是一种有前途的口服传递系统,可在结肠靶位发挥药效。

【Abstract】 Objective To investigate the feasibility of resistant starch( RS) of Polygonum multiflorum as a targeted colon pellet material.Methods Under the physiological conditions,the dissolution rate of RS and microcrystalline cellulose( MCC) in different proportions of pellets was investigated,with Matrine( MT) as the model drug,the pellets were prepared by extrusion-spheronization technology,and the relevant indexes were observed. Results RS had shown significant effect on the release of pellets. In vitro drug release showed that when the RS/MCC was less than 0. 5,the yield,sphericity and crispness of the pellets were > 80. 00%,> 0. 95 and < 0. 12%,respectively.High content of RS in pellets could significantly improve the tolerance to p H changes and enzymatic hydrolysis. Under the action of microbial Escherichia coli,the pellets rapidly disintegrated and dissolved more than 82% in 30 min. Conclusion RS of Polygonum multiflorum is a promising oral delivery system,which can exert efficacy in the colon target.

【基金】 国家自然科学基金[81360486];贵州省中药现代化科技产业研究开发专项项目[黔科合SY字[2014]3081-2号]
  • 【文献出处】 中国药业 ,China Pharmaceuticals , 编辑部邮箱 ,2017年17期
  • 【分类号】R283.6
  • 【被引频次】4
  • 【下载频次】195
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