pH依赖-时滞型夏枯草有效组分结肠定位微丸的制备及体外释药评价  

Study on preparation and drug release evaluation in vitro of pH dependent and time-lay colon-specific pellets of effective components of Prunella vulgaris L.

作　　者：张建伟[1] 刘力[1] 徐雅 ZHANG Jian-wei;LIULi;XU Ya(Shuguang Hospital Ailiated to Shanghai University of Traditional Chinese Medicne,Shanghai 20021 China)

机构地区：[1]上海中医药大学附属曙光医院,上海200021

出　　处：《中华中医药杂志》2021年第7期3982-3986,共5页China Journal of Traditional Chinese Medicine and Pharmacy

基　　金：上海市科学技术委员会科研计划科技支撑项目(No.13401900302);上海市进一步加快中医药事业发展三年行动计划(No.ZY3-JSFC-2-3004)。

摘　　要：目的:制备pH依赖-时滞型夏枯草有效组分结肠定位微丸,并对其体外释药进行评价。方法:采用流化床包衣法,在淀粉丸芯外依次包裹药物层、时滞层及pH依赖层制备夏枯草有效组分结肠定位微丸;以药物体外释放度为评价指标,考察影响微丸释药行为的处方因素,并设计正交试验优化处方。结果:时滞层包衣液以乙基纤维素20(EC20)、55%聚乙二醇6000(PEG6000)、10%滑石粉为主要包衣材料,包衣增重3%;pH依赖层包衣液以聚丙烯酸树脂尤特奇S100-EC20(10∶1)、20%枸橼酸三乙酯、20%滑石粉为主要包衣材料,包衣增重25%。制得包衣微丸在pH 1.0 HCl中运转2h,pH 6.8 PBS中运转3h,基本不释放药物,在pH 7.6 PBS中运转5h累积释放药物达90%以上。结论:该pH依赖-时滞型结肠定位微丸的制备工艺稳定可行,体外达到结肠定位效果。Objective: To prepare pH dependent and time-lay colon-specific pellets of the effective components of Prunella vulgaris L.(PVB), and to evaluate the pellets release behavior in vitro. Methods: The pellets were coated with PVB, the time-lag film and the pH-dependent film by fluidized bed coater, successively. The release behaviors of coated pellets were investigated in vitro, with drug release as index. The prescription of pellets was optimized by L9(34) orthogonal design. Results: The time-lag layer with 3%(weight) coating level was prepared with EC20 as film-forming agent, 55%PEG6000 and 10% talc added. The pH-dependent layer with 25%(weight) coating level was prepared with Eudragit S100-EC20(10∶1) as filmforming agent, 20%TEC and 20%talc added. In pH 1.0 HCl juice after 2 h and in pH 6.8 PBS juice after 3 h, the coated pellets were cumulatively released no drug, and released more than 90% drug in pH 7.6 PBS juice after 5 h. Conclusion: The preparation method of the pH dependent and time-lay colon-specific pellets is stable and the pellets can achieve the colon targeted release in vitro.

关 键 词：夏枯草有效组分 pH依赖-时滞型 结肠定位微丸 正交试验 体外释放度评价 

分 类 号：R283.6[医药卫生—中药学]