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通过挥发性低共熔溶剂技术对结晶性赛沃替尼进行形态控制。

Morphological Control of Crystalline Savolitinib via the Volatile Deep Eutectic Solvent Technique.

作者信息

Symons Jasmine E, Hall Charlie, McCabe James F, Hall Simon R

机构信息

Complex Functional Materials Group, School of Chemistry, University of Bristol, Bristol BS8 1TS, U.K.

Complex Functional Materials Group, School of Chemistry, University of Bristol, Bristol BS8 1TS, United Kingdom; Centre for Doctoral Training in Condensed Matter Physics, HH Wills Physics Laboratory, Bristol BS8 1TL, U.K.

出版信息

Cryst Growth Des. 2024 Mar 1;24(6):2567-2572. doi: 10.1021/acs.cgd.4c00035. eCollection 2024 Mar 20.

Abstract

Savolitinib is a compound that can crystallize in an undesirable, high aspect ratio needle morphology. This morphology type may cause issues in downstream processing. This paper demonstrates a unique method to alter the crystal morphology of savolitinib to make it more processable, resulting in the active pharmaceutical ingredient (API) crystallizing out in considerably more processable stellates. The volatile deep eutectic solvent technique presents a simple and scalable method for changing the crystal morphology while maintaining the polymorph of the API in this case, confirmed via powder X-ray diffraction and differential scanning calorimetry analysis.

摘要

赛沃替尼是一种能够以不理想的高纵横比针状形态结晶的化合物。这种形态类型可能会在下游加工过程中引发问题。本文展示了一种独特的方法来改变赛沃替尼的晶体形态,使其更易于加工,从而使活性药物成分(API)以更易于加工的星状结晶析出。挥发性低共熔溶剂技术提供了一种简单且可扩展的方法来改变晶体形态,同时在这种情况下保持API的多晶型,这通过粉末X射线衍射和差示扫描量热法分析得到了证实。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/284c/10958444/88a2c6bffcc2/cg4c00035_0001.jpg

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