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阿克西替尼的盐酸盐和多态:特征和相变化
Yinhu Pan1, Tong Xiao1, Yan Wang1
1School of Pharmaceutical Sciences (Shandong Analysis and Test Center), Qilu University of Technology (Shandong Academy of Sciences), Jinan 250014, China.
一种新的晶体形式 (形式Z) 的阿克西替尼 (AXTN) 通过溶解它的溶酸盐被发现. 这些在各种溶剂中形成的溶酸盐可以转化为其他形式,从而提供了对axitinib的洞察力.
科学领域:
- 制药化学 制药化学 制药化学
- 固态化学 固态化学
- 材料科学 材料科学 材料科学
背景情况:
- 亚克西替尼 (AXTN) 是氨酸激酶抑制剂,对于细胞癌治疗至关重要.
- 了解AXTN的固态特性,包括酸盐和多态化合物,对于药物配方和疗效至关重要.
- 之前的研究还没有完全探索了AXTN.的溶盐形成和相变化.
研究的目的:
- 在各种溶剂中准备和表征阿克西替尼 (AXTN) 溶酸盐.
- 调查溶解过程并确定AXTN的新晶体形式.
- 在不同的条件下阐明AXTN溶解物的相变换路径.
主要方法:
- 在乙二,DMF,乙酸,乙酸+水和甲醇中AXTN的溶剂制剂.
- 固相解溶 (加热,溶剂蒸汽,微波) 和溶剂介导相变换 (SMPT).
- 使用PXRD,TGA,DSC,FT-IR和SEM进行表征.
主要成果:
- 五种类型的AXTN溶酸盐已成功准备和表征.
- 在溶解后获得了AXTN的新型晶体形式 (Z形式).
- 通过SMPT观察了溶解物之间的相互转换,受溶剂成分的影响.
结论:
- 该研究成功地确定了新的溶酸盐和西替尼的新型晶体形式 (Z形式).
- 了解AXTN溶解物行为和相位转换对于开发优化药物配方至关重要.
- 这些发现为进一步探索axitinib的多态和固态特性提供了宝贵的指导.
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