弹簧和降落伞:共晶如何提高溶解度

IF 4.5 2区 材料科学 Q1 CRYSTALLOGRAPHY Progress in Crystal Growth and Characterization of Materials Pub Date : 2016-09-01 DOI:10.1016/j.pcrysgrow.2016.07.001
Dhara D. Bavishi, Chetan H. Borkhataria
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引用次数: 136

摘要

本文旨在结合有关共结晶的文献-一种提高溶解度和改善原料药理化性质的工具(原料药是负责提供治疗效果的分子),并特别强调其机制。制药行业正在目睹药物开发过程中的危机,这是由于研发部门的成本不断增加,一些重量级候选药物由于水溶性差而失败,以及由于专利限制而无法获得新分子。共结晶是一种新兴的改善原料药溶解度、溶解谱、生物利用度和其他物理化学和机械性能的方法。药物共晶现在是一种新的缩影,它可以在不形成或破坏共价键的情况下使用广泛的活性药物成分。这篇综述文章的主要焦点是机制,如何共晶具有溶解度优势的非晶形式。本文还简要介绍了共晶的性质、作用、晶体工程原理,并重点介绍了共晶中存在的超分子合成子的性质。
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Spring and parachute: How cocrystals enhance solubility

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.

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来源期刊
Progress in Crystal Growth and Characterization of Materials
Progress in Crystal Growth and Characterization of Materials 工程技术-材料科学:表征与测试
CiteScore
8.80
自引率
2.00%
发文量
10
审稿时长
1 day
期刊介绍: Materials especially crystalline materials provide the foundation of our modern technologically driven world. The domination of materials is achieved through detailed scientific research. Advances in the techniques of growing and assessing ever more perfect crystals of a wide range of materials lie at the roots of much of today''s advanced technology. The evolution and development of crystalline materials involves research by dedicated scientists in academia as well as industry involving a broad field of disciplines including biology, chemistry, physics, material sciences and engineering. Crucially important applications in information technology, photonics, energy storage and harvesting, environmental protection, medicine and food production require a deep understanding of and control of crystal growth. This can involve suitable growth methods and material characterization from the bulk down to the nano-scale.
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