关于以泽提米布与环极素复合物的纳入方法:通过分子对接增强可溶性和相互作用分析的策略
Dae-Yeong Cho1, Jeong-Gyun Lee1, Moon-Jung Kim1
1Department of Pharmaceutical Engineering, Gyeongsang National University, 33 Dongjin-ro, Jinju 52725, Republic of Korea.
International journal of molecular sciences
|February 26, 2025
概括
通过使用β-cyclodextrin (β-CD) 衍生物增强了埃泽胺 (EZT) 的溶解性,形成稳定的包容复合物. 这些综合体显著改善了EZT.
科学领域:
- 制药科学 制药科学
- 物理化学 物理化学
- 材料科学 材料科学 材料科学
背景情况:
- 埃泽胺 (EZT) 具有较差的水溶性,限制了其口服生物可用性.
- 已知β-cyclodextrin (β-CD) 和其衍生物形成包容复合物,增强难溶性药物的可溶性.
研究的目的:
- 通过与各种β-cyclodextrin (β-CD) 衍生物形成包含复合物来提高ezetimibe (EZT) 的水溶性和溶解率.
- 描述EZT/β-CD衍生品含有复合物的物理化学性质,并评估其体外性能.
主要方法:
- 阶段溶解性研究和乔布的图形分析,以确定静态测量和稳定常数.
- 喷雾干燥技术用于制备EZT/β-CD衍生物的含有复合物.
- 使用SEM,PXRD,FT-IR进行表征,并评估和溶解度和体外溶解度.
主要成果:
- 证实了EZT与β-CD及其衍生物的1:1稳定比,其明显稳定常数很高.
- 与纯EZT相比,包括复合物,特别是RM-β-CD和DM-β-CD,显示了显著提高的和溶解度和溶解率.
- 分子对接模拟支持将EZT纳入β-CD腔和相关的结合能量,并观察到可溶性改善.
结论:
- 用β-CD衍生物,特别是RM-β-CD和DM-β-CD复合是一种有效的策略,可以增强ezetimibe的溶解性和溶解性.
- 开发的EZT/β-CD衍生体含有复合物显示出改善高脂血症治疗的口服固体配方的前景.
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