通过液态核磁共振预测成功的无形固体分散对
Ana L Coutinho1, Kellie Hom1, James E Polli1
1Department of Pharmaceutical Sciences, University of Maryland School of Pharmacy, Baltimore, Maryland 21201, United States.
Molecular pharmaceutics
|November 1, 2024
概括
核磁共振 (NMR) 可以预测聚合物适合于无形固体分散 (ASD). 通过NMR识别的强药聚合物相互作用与长时间的药物超和和降低的沉相关,简化了ASD的发展.
科学领域:
- 制药科学 制药科学
- 材料科学 材料科学 材料科学
- 分析化学 分析化学
背景情况:
- 无形固体分散 (ASDs) 提高了药物的溶解性和生物可用性.
- 这是一个很棒的节目,这是一个很棒的节目.
- 降落效应的降落效应
- 在ASD中依赖于聚合物介导的药物超和.
- 了解药物聚合物相互作用对于ASD配方至关重要.
研究的目的:
- 评估液态核磁共振 (NMR) 作为ASD发展中的聚合物选择工具.
- 在超和研究中,将NMR检测到的药物聚合物相互作用与药物沉动力学相关联.
- 简化识别适合ASDs的聚合物的过程.
主要方法:
- 使用和转移差异NMR (STD-NMR),放松时间和2D-H NOESY实验来评估药物聚合物相互作用.
- 超和研究使用溶剂转移方法进行,以测量沉抑制.
- 1H NMR发现与实验超和数据进行比较,以埃特拉维林与HPMC,HPMCAS-M和PVP-VA.
主要成果:
- STD-NMR和T1放松时间表明埃特拉维林与HPMCAS-M>HPMC ≫ PVP-VA.的优先结合.
- 核磁共振数据提供了对特定药物聚合物结合部位的见解.
- 与PVP-VA不同,HPMC和HPMCAS-M表现出强烈的相互作用,有效地抑制了埃特拉维林沉并保持了超和度.
- 超和研究证实,与PVP-VA相比,HPMC和HPMCAS-M延长了埃特拉维林的溶解时间.
结论:
- 液态H NMR是一种有希望的,非破坏性的方法,用于预测ASD中的聚合物性能.
- 通过NMR检测到的强药聚合物相互作用与增强的药物超和和降低的沉相关.
- 核磁共振可以显著简化用于ASD发展的聚合物选择,节省时间和资源.
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