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共晶在药物设计中的作用。

The role of co-crystals in pharmaceutical design.

机构信息

Department of Chemistry, Durham University, Science Site, South Road, Durham DH1 3LE, UK.

出版信息

Trends Pharmacol Sci. 2013 Mar;34(3):185-93. doi: 10.1016/j.tips.2012.12.003. Epub 2013 Jan 21.

Abstract

Pharmaceutical co-crystal formation represents a straightforward way to dramatically influence the solid-state properties of a drug substance, particularly its solubility and hence bioavailability. This short review summarises this highly topical field, covering why the topic is of interest in pharmaceutical formulation, the definitions and practical scope of co-crystals, co-crystal preparation and characterisation, and implications for regulatory control and intellectual property (IP) protection. Concepts are illustrated with highly selected examples of pharmaceutical co-crystal systems within the wider context of crystal engineering and research in molecular solids.

摘要

药物共晶的形成是一种能够显著影响药物物质固态特性的简单方法,尤其是对其溶解度和生物利用度的影响。这篇简短的综述总结了这一非常热门的领域,涵盖了为什么该主题在药物制剂中具有吸引力,共晶的定义和实际范围,共晶的制备和特性,以及对监管控制和知识产权(IP)保护的影响。在分子固体的晶体工程和研究的更广泛背景下,通过高度选择的药物共晶体系的例子来说明这些概念。

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