一种具有增强溶解性的新型共形乙胺:制备,表征,在中药理动力学,并通过封装控制释放
João G de Oliveira Neto1, Raychiman D S Bezerra1, Francisco N B Domingos1
1Center for Science of Imperatriz, Federal University of Maranhão - UFMA, 65900-410, Imperatriz, MA, Brazil.
International journal of pharmaceutics
|January 2, 2025
概括
这项研究开发了使用缓慢溶剂蒸发的埃西奥纳米德 (ETH) 和曼德利酸 (MND) 的新型共变系统. 这提高了ETH的溶解性和稳定性,显示了改进药物输送系统的潜力.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 计算化学计算化学
背景情况:
- 埃塞奥纳米德 (ETH) 是一种具有不良溶解性的重要药物.
- 同形系统为提高药物溶解性和生物可用性提供了一个有希望的策略.
- 了解分子间相互作用对于设计稳定的同形配方至关重要.
研究的目的:
- 合成和描述一种由乙胺 (ETH) 和曼底酸 (MND) 组成的新型共形系统.
- 研究ETH-MND同形系统的结构,振动,热和药物动力学特性.
- 评估这种共形系统在可控药物输送应用中的潜力.
主要方法:
- 通过缓慢的溶剂蒸发进行同形系统合成.
- 使用粉末X射线衍射 (PXRD),红外 (IR) 光谱和热分析 (DSC) 进行表征.
- 计算建模包括密度函数理论 (DFT) 和希尔什菲尔德表面分析.
主要成果:
- 在1:2和1:3的ETH:MND比率下形成稳定的无形二进制系统,由PXRD证实.
- 同形系统在高温和高湿度下表现出极好的物理稳定性.
- DFT的计算揭示了键作为驱动同形形成的主要相互作用.
- 在封装时,在480分钟内显著增加ETH溶解度3.58倍,并控制药物释放.
结论:
- 通过成功合成ETH-MND同形系统,显示出增强的溶解性和稳定性.
- 结合相互作用是共同形态系统的形成和稳定性的关键.
- 开发的共形系统有望改善药物配方和控制药物输送.
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