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化学进展 2010, Vol. 22 Issue (05): 829-836 前一篇   后一篇

• 综述与评论 •

药物共晶研究进展*

高缘1; 祖卉2; 张建军2**   

  1. (1. 中国药科大学中药学院 南京 210009; 2. 中国药科大学药学院 南京 210009)
  • 收稿日期:2009-07-22 修回日期:2009-09-11 出版日期:2010-05-24 发布日期:2010-05-05
  • 通讯作者: 张建军 E-mail:amicute@163.com

Pharmaceutical Cocrystals

Gao Yuan1; Zu Hui2; Zhang Jianjun2**   

  1. (1. School of Traditional Chinese Medicine, China Pharmaceutical University, Nanjing 210009, China; 2. School of Pharmacy, China Pharmaceutical University, Nanjing 210009, China)
  • Received:2009-07-22 Revised:2009-09-11 Online:2010-05-24 Published:2010-05-05
  • Contact: Zhang Jianjun E-mail:amicute@163.com

相同药物的不同固体形态往往有不同的理化性质、药效以及制剂制备工艺。常见的固体形态如溶剂化物、盐,因为种类少或适用的药物少而在应用上受到一定的限制,所以种类多、适用范围广的共晶作为可设计的药物固体形态近年来逐渐受到关注。本文介绍了药物共晶的研究进展,包括其形成原理、设计思路、性质以及制备方法,共晶在药物研究领域有很好的应用前景。

Different solid forms of identical drug may have diverse physicochemical properties, therapeutic/toxicological effects and formulation profiles. Compared to solvates and salts which are limited to small numbers of nontoxic solvents and ionizable drugs, cocrystals represent the very promising designable solid forms of active pharmaceutical ingredients, due to their extensive species and wide application scope. In this article, progress on pharmaceutical cocrystals, including the formation principles, cocrystal design, physicochemical properties and preparation techniques, is addressed. Cocrystals have great potentials in pharmaceutical sciences.

Contents
1 Introduction
2 Principle of cocrystal formation
3 Design of cocrystals
3.1 Interaction-based design
3.2 Molecular properties-based design
3.3 Host molecule-based design
4 Properties of cocrystals
4.1 Melting point
4.2 Hygroscopicity
4.3 Stability
4.4 Solubility and dissolution
4.5 Bioavailability
4.6 Release
4.7 Mechanical properties
4.8 Phase diagram
4.9 Application in separation and purification
5 Preparation of cocrystals
5.1 Crystallization from solvent
5.2 Solid state grinding
5.3 Sonication
5.4 Supercritical fluid technology
6 Outlook

中图分类号: 

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摘要

药物共晶研究进展*