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Capturing two new salts of the anticancer drug gefitinib
Molecular Crystals and Liquid Crystals ( IF 0.7 ) Pub Date : 2022-09-28 , DOI: 10.1080/15421406.2021.1912689
Lihai Zhai 1, 2 , Zhiying Zhu 1 , Lihong Guo 1, 2 , Junhou Yu 1 , Huaimin Dong 1 , Guimin Zhang 1, 2
Affiliation  

Abstract

In this text, the new crystal forms of geffitinib were explored through evaporation solution crystallization experiment. The formation of salts was confirmed by the single crystal X-ray diffraction, powder X-ray diffraction, thermo gravimetric analysis and differential scanning calorimetry, Raman spectroscopy, hot-stage microscopy and Hirshfeld surface analysis. Furthermore, Hirshfeld surface analysis confirmed that the driving force and supporting force for the formation of crystals were C-C, C-H, N-H, H-H, O-H and Cl-H interactions. The dissolution rate of the new salts of gefitinib in phosphate buffer of pH 6.8 was evaluated, and the results showed a significant increase in solubility.



中文翻译:

捕获抗癌药物吉非替尼的两种新盐

摘要

本文通过蒸发溶液结晶实验探索了吉非替尼的新晶型。通过单晶 X 射线衍射、粉末 X 射线衍射、热重分析和差示扫描量热法、拉曼光谱、热台显微镜和 Hirshfeld 表面分析证实了盐的形成。此外,Hirshfeld 表面分析证实,晶体形成的驱动力和支持力是 CC、CH、NH、HH、OH 和 Cl-H 相互作用。评估了吉非替尼新盐在 pH 6.8 磷酸盐缓冲液中的溶解速率,结果显示溶解度显着增加。

更新日期:2022-09-28
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