Recent development on the microencapsulation of hydrophilic small molecular drugs

doi:10.16085/j.issn.1000-6613.2016.01.027

Abstract

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 self-assembly method and solvent evaporation method with magnetic particles were analyzed. It was pointed out that the development of encapsulating hydrophilic small molecule drugs would favor simple, safe and effective and intelligent target operation.

Key words: pharmaceuticals, preparation, support, sustained release microspheres, hydrophilic small molecule, intelligent target

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

CLC Number:

R944.9

LI Jinghan, WEI Zhenping. Recent development on the microencapsulation of hydrophilic small molecular drugs[J]. Chemical Industry and Engineering Progree, 2016, 35(01): 204-209.

李静涵, 魏振平. 亲水性小分子药物缓释微球制备方法的研究进展[J]. 化工进展, 2016, 35(01): 204-209.

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