药物的球形结晶技术

Spherical Crystallization Technique of Drugs

球结晶是通过控制重结晶中药物分子相互聚合过程,可得到较大粒径球形药物颗粒的技术,作为新型的粒子设计方法,该技术可改善粉体性质(包括流动性、可压缩性、生物利用度等)、控制过程参数(温度、搅拌速率、溶剂种类和用量、辅料种类等)、得到理想粒径分布的球形颗粒。本文综述了国内外药剂学领域球结晶技术的相关研究,着重介绍了经典的球结晶制备方法(球形聚集法、类乳浊液溶剂扩散法、氨扩散法和结晶共聚法),从工业扩大生产的角度,在制备方法、过程参数及粉体性能方面提出了一些想法,为该技术在药物的应用与推广方面提供参考。

Spherical crystallization is a technology to obtain spherical drugs with large particle size by controlling polymerization process of drug molecules during crystallization. As a new method of particle design, this technique can improve powder properties, including flowability, compressibility, bioavailability and so on, control process parameters and obtain spherical particles with desired particle size distribution. Process parameters during crystallization includes temperature, stirring rate, type and amount of solvents etc. This paper focuses on four classical techniques for obtaining spherical particles and give viewpoint on its industrial enlargement.