Synthesis and structural analysis of pharmaceutical co-crystals

doi:10.11949/j.issn.0438-1157.20160928

Abstract

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:

TQ460.1

HUANG Yaohui, YIN Qiuxiang, ZHANG Xia, GUO Mingxia, WANG Chang. Synthesis and structural analysis of pharmaceutical co-crystals[J]. CIESC Journal, 2017, 68(2): 509-518.

黄耀辉, 尹秋响, 张霞, 郭明霞, 王昌. 药物共晶的合成和结构分析[J]. 化工学报, 2017, 68(2): 509-518.

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