CIESC Journal ›› 2017, Vol. 68 ›› Issue (2): 509-518.DOI: 10.11949/j.issn.0438-1157.20160928

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Synthesis and structural analysis of pharmaceutical co-crystals

HUANG Yaohui1, YIN Qiuxiang1,2, ZHANG Xia1, GUO Mingxia1, WANG Chang1   

  1. 1. State Key Laboratory of Chemical Engineering, School of Chemical Engineering and Technology, Tianjin University, Tianjin 300072, China;
    2. Collaborative Innovation Center of Chemical Science and Chemical Engineering, Tianjin 300072, China
  • Received:2016-06-30 Revised:2016-10-20 Online:2017-02-05 Published:2017-02-05
  • Supported by:

    supported by the Tianjin Research Program of Application Foundation and Advanced Technology (the Key Program of Natural Science Foundation of Tianjin) (11JCZDJC20700).

药物共晶的合成和结构分析

黄耀辉1, 尹秋响1,2, 张霞1, 郭明霞1, 王昌1   

  1. 1. 化学工程联合国家重点实验室, 天津大学化工学院, 天津 300072;
    2. 化学化工协同创新中心, 天津 300072
  • 通讯作者: 尹秋响
  • 基金资助:

    天津市应用基础及前沿技术研究计划项目(天津市自然科学基金重点项目)(11JCZDJC20700)。

Abstract:

Co-crystals have advantages in physiochemical properties over their constituent components and are expected to use in product formulation such as enhanced active pharmaceutical ingredients, food components with improved absorbability, and specialty chemicals with better performance. The development of pharmaceutical co-crystals might offer advantages over the active pharmaceutical ingredients and overcome some of the limitations encountered with classical strategy (polymorph, solvate and salt formation). In recent years, co-crystals have recently gained much attention for pharmaceutical development especially because it has great advantages in improving the solubility, dissolution, melt point and oral bioavailability. Since the co-crystals lattice comprises two or more kinds of molecules, compared with the conventional structure of the drug crystal, intermolecular force comprising more types such as hydrogen, halogen bond, van der Waals forces, π-π interaction, so the structure is more complex. The research on the co-crystals structure can be helpful to understand the formation mechanism. The definition, application, preparation and structure of co-crystals were reviewed, it will provide theoretical guidance for the studies of the following research.

Key words: pharmaceutical co-crystals, synthesis, crystallization, structural study, chemical processes

摘要:

药物的理化性质与其结晶形式相关,药物共晶作为一种新型的固态形式能够在不影响药物内部结构的同时改善药物的多方面性质,提高药效。通过药物共晶的定义、应用、制备方法和结构研究等方面对目前药物共晶的研究现状进行总结,为后续共晶方向的研究提供理论指导。

关键词: 药物共晶, 合成, 结晶, 结构研究, 化学过程

CLC Number: