乙amizuril与β-和Hydroxypropyl-β-Cyclodextrin在水溶液和固体中的含有复合物:一项比较研究
Juan Guo1, Lifang Zhang1,2, Mi Wang1,2
1Shanghai Veterinary Research Institute, Chinese Academy of Agricultural Sciences, Shanghai 200241, China.
Molecules (Basel, Switzerland)
|May 25, 2024
概括
乙amizuril (EZL),一种抗菌药物,是复杂的与环氧素 (CDs) 改善其水溶性. propyl-β-cyclodextrin (HP-β-CD) 通过键和性相互作用显示出优异的溶解效应.
科学领域:
- 兽医药理学 兽医药理学
- 药物输送系统 药物输送系统
- 超分子化学 超分子化学
背景情况:
- 乙amizuril (EZL) 是一种具有水溶性差的新型抗菌药物,限制了其配方选择.
- 环极素 (CDs),包括β-环极素 (β-CD) 和基-β-环极素 (HP-β-CD),是已知的增强药物溶解性的辅助剂.
- 了解EZL和CD之间的相互作用机制对于开发有效的药物配方至关重要.
研究的目的:
- 通过与β-cyclodextrin (β-CD) 和hydroxypropyl-β-cyclodextrin (HP-β-CD) 形成包容复合物来提高乙amizuril (EZL) 的水溶性.
- 阐明溶解机制,并比较β-CD和HP-β-CD在形成EZL纳入复合物的有效性.
- 为开发EZL的高度饮用水配方提供基础.
主要方法:
- 用分子对接模拟来预测相互作用.
- 阶段溶解性研究确定了复杂的形成和固态度 (1:1摩尔比率).
- 固态特征使用DSC,PXRD和FT-IR;溶液状态相互作用通过PSA,UV-vis,MS,1H NMR和2D ROESY进行分析.
主要成果:
- 无论是β-CD还是HP-β-CD,都与EZL形成了1:1的纳入复合体.
- 惠普-β-CD表现出更高的稳定常数 (Kf) 和复合效率 (CE),从而产生更大的溶解效应.
- 分子间键和疏水相互作用被确定为驱动复杂形成的关键力量,在实验和计算方法中一致.
结论:
- 与β-CD相比,HP-β-CD是一种更有效的环氧素,可以提高EZL的溶解度.
- EZL/CD纳入复合物的形成是由结和疏水性相互作用驱动的.
- 这项研究支持开发先进的EZL配方,特别是用于饮用水中的口服.
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