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Spring and parachute: How cocrystals enhance solubility
Progress in Crystal Growth and Characterization of Materials ( IF 5.1 ) Pub Date : 2016-09-01 , DOI: 10.1016/j.pcrysgrow.2016.07.001
Dhara D. Bavishi , Chetan H. Borkhataria

Abstract This article is intended to combine literature on cocrystallization – a tool for enhancing the solubility and for improving the physicochemical properties of an API (an API is the molecule which is responsible for providing the therapeutic effect) with special emphasis on the mechanism responsible for the same. The pharmaceutical industries are witnessing a developing crisis in the process of drug development due to the increasing cost of their R&D departments, the failure of some blockbuster drug candidates exhibiting poor aqueous solubility and the unavailability of newer molecules because of patent limitations. Cocrystallization is an emerging approach to improve solubility, dissolution profile, bioavailability, and other physicochemical and mechanical properties of an API. A pharmaceutical cocrystal is now a new epitome which enables the use of a wide range of active pharmaceutical ingredients without the need to form or break the covalent bonds. The prime focus of this review article is the mechanism on how cocrystals have a solubility advantage over the amorphous form. This review also provides a brief introduction to the nature of cocrystals, their role, principles of crystal engineering and also highlights the nature of supramolecular synthons which are present in cocrystals.

中文翻译:

弹簧和降落伞:共晶如何提高溶解度

摘要 本文旨在结合关于共结晶的文献——一种用于提高溶解度和改善 API(API 是负责提供治疗效果的分子)的理化性质的工具,特别强调负责这些作用的机制。相同的。由于研发部门的成本不断增加,一些表现出水溶性差的重磅候选药物的失败以及由于专利限制而无法获得新分子,制药行业正在见证药物开发过程中的发展危机。共结晶是一种新兴方法,可提高 API 的溶解度、溶出度、生物利用度和其他物理化学和机械性能。药物共晶现在是一种新的缩影,它能够使用范围广泛的活性药物成分,而无需形成或破坏共价键。这篇评论文章的主要焦点是共晶如何比无定形形式具有溶解度优势的机制。这篇综述还简要介绍了共晶的性质、它们的作用、晶体工程的原理,并强调了共晶中存在的超分子合成子的性质。
更新日期:2016-09-01
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