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超分子金属-酚凝胶用于活性药物成分的结晶。

Supramolecular Metal-Phenolic Gels for the Crystallization of Active Pharmaceutical Ingredients.

机构信息

ARC Centre of Excellence in Convergent Bio-Nano Science and Technology and the Department of Chemical Engineering, The University of Melbourne, Parkville, Victoria, 3010, Australia.

Department of Chemical Science and Engineering, School of Materials and Chemical Technology, Tokyo Institute of Technology, 2-12-1-H121 Ookayama, Meguro-ku, Tokyo, 152-8550, Japan.

出版信息

Small. 2018 Jun;14(26):e1801202. doi: 10.1002/smll.201801202. Epub 2018 May 28.

DOI:10.1002/smll.201801202
PMID:29808530
Abstract

The use of supramolecular gel media for the crystallization of active pharmaceutical ingredients (APIs) is of interest for controlling crystal size, morphology, and polymorphism, as these features determine the performance of pharmaceutical formulations. In contrast to supramolecular systems prepared from synthetic gelators, herein, supramolecular metallogels based on a natural polyphenol (tannic acid) are used for the crystallization of APIs. The gel-grown API crystals exhibit considerable differences in size, morphology, and polymorphism when compared with those formed in solutions. These physical features can also be tailored by varying the gel composition and additives, suggesting an influence of the gel medium on the crystallization outcomes. Furthermore, these gel-API crystal composites can be used for sustained drug release, indicating their potential as drug delivery systems. The facile preparation of these supramolecular gels and the use of naturally abundant components in their synthesis provide a generic platform for studying gel-mediated crystallization of diverse APIs.

摘要

使用超分子凝胶介质进行活性药物成分(APIs)的结晶对于控制晶体的大小、形态和多晶型具有重要意义,因为这些特性决定了药物制剂的性能。与由合成凝胶剂制备的超分子系统不同,本文使用基于天然多酚(鞣酸)的超分子金属凝胶来结晶 APIs。与在溶液中形成的 API 晶体相比,凝胶生长的 API 晶体在尺寸、形态和多晶型方面表现出显著差异。通过改变凝胶组成和添加剂,这些物理特性也可以进行调整,表明凝胶介质对结晶结果有影响。此外,这些凝胶-API 晶体复合材料可用于控制药物释放,表明其作为药物传递系统的潜力。这些超分子凝胶的制备方法简单,并且在其合成中使用了天然丰富的成分,为研究不同 APIs 的凝胶介导结晶提供了一个通用平台。

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