亲水性小分子药物缓释微球制备方法的研究进展综述与专论.PDF

化 工 进 展 ·204 · CHEMICAL INDUSTRY AND ENGINEERING PROGRESS 2016 年第35 卷第1 期 综述与专论 亲水性小分子药物缓释微球制备方法的研究进展 李静涵，魏振平 （天津大学化工学院，天津300072 ） 摘要：缓释微球可以延长药物的作用时间，从而能够解决亲水性小分子药物由于半衰期较短需要长期频繁给药 的问题。本文综述了亲水性小分子药物缓释微球制备方法的研究现状和发展方向，分别从使用非水溶性载体材 料和水溶性载体材料两个方面介绍了亲水性小分子微球制备方法的优缺点。使用非水溶性载体材料方面，重点 阐述了乳化溶剂挥发法和相分离法；使用水溶性载体材料方面，重点阐述了乳化交联法和喷雾干燥法。并着重 分析了层层自组装法以及结合磁性粒子的溶剂挥发法的技术原理和制备过程。最后指出亲水性小分子药物缓释 微球的制备方法将朝着操作简单、安全有效和智能靶向的方向发展。 关键词：药物；制备；载体；缓释微球；亲水性小分子；智能靶向 中图分类号：R 944.9 文献标志码：A 文章编号：1000 –6613 （2016 ）01 –0204 –06 DOI ：10.16085/j.issn.1000-6613.2016.01.027 Recent development on the microencapsulation of hydrophilic small molecular drugs LI Jinghan ，WEI Zhenping （School of Chemical Engineering and Technology，Tianjin University ，Tianjin 300072，China ） Abstract ：Because of their short half-life ，hydrophilic small molecule drugs need frequent administration and sustained release microspheres can control the release of drug and therefore overcome this disadvantage. This article reviewed the present preparation status and development direction of microencapsulating hydrophilic small molecule drugs，and introduced the advantages and disadvantages of different preparation methods from the view of using different support materials. Emulsion solvent evaporation method and phase separation method were elaborated for water-insoluble support materials，while for water-soluble support materials ，emulsion crosslinking method and spray drying method were discussed. Then the technical principles and preparation procedures of layer-by-layer