使用共晶来系统调节抗癌药物的水溶性和化行为
Christer B Aakeröy1, Safiyyah Forbes, John Desper
1Department of Chemistry, Kansas State University, 211 CBC Building, Manhattan, Kansas 66506, USA. aakeroy@ksu.edu
Journal of the American Chemical Society
|November 10, 2009
概括
研究人员使用超分子方法制造了抗癌药物的五个共晶体. 这些共晶体通过改变二碳酸成分,表现出可调整的物理性质,如增强水溶性.
科学领域:
- 固态化学 固态化学
- 超分子化学 超分子化学
- 制药科学 制药科学 制药科学
背景情况:
- 抗癌药物开发需要优化固态特性以获得有效性.
- 晶形成是一种修改药物的物理化学特性的策略.
- 基于键的超分子组件可以控制固态结构.
研究的目的:
- 为了组装和表征抗癌化合物的共晶与酸二碳酸酸.
- 研究共晶结构与物理性质之间的关系.
- 通过共结晶来证明调整药物特性的潜力.
主要方法:
- 超分子方法利用结合用于共晶组装.
- 随着链条长度的增加,异形偶数二碳酸的系统变化.
- 共同晶体物理性质的表征,包括点和水溶性.
主要成果:
- 成功合成了五个具有结构一致性的共晶体.
- 晶的点与构成二碳酸的点有很强的相关性.
- 抗癌化合物的水溶性在同晶体形式上增强了2.5倍.
结论:
- 使用二氧化酸的晶工程提供了一种系统修改药物的物理性质的方法.
- 观察到的结构-特性关系使药物固体形式的有针对性的优化成为可能.
- 晶为开发改进的抗癌药物配方提供了一个多功能平台.
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