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19F Solid-state NMR characterization of pharmaceutical solids
Solid State Nuclear Magnetic Resonance ( IF 1.8 ) Pub Date : 2022-05-25 , DOI: 10.1016/j.ssnmr.2022.101796
Yong Du 1 , Yongchao Su 2
Affiliation  

Solid-state NMR has been increasingly recognized as a high-resolution and versatile spectroscopic tool to characterize drug substances and products. However, the analysis of pharmaceutical materials is often carried out at natural isotopic abundance and a relatively low drug loading in multi-component systems and therefore suffers from challenges of low sensitivity. The fact that fluorinated therapeutics are well represented in pipeline drugs and commercial products offers an excellent opportunity to utilize fluorine as a molecular probe for pharmaceutical analysis. We aim to review recent advancements of 19F magic angle spinning NMR methods in modern drug research and development. Applications to polymorph screening at the micromolar level, structural elucidation, and investigation of molecular interactions at the Ångström to submicron resolution in drug delivery, stability, and quality will be discussed.



中文翻译:

药物固体的 19F 固态 NMR 表征

固态 NMR 已越来越被公认为是表征药物和产品的高分辨率和多功能光谱工具。然而,药物材料的分析通常在天然同位素丰度和多组分系统中相对较低的载药量下进行,因此面临灵敏度低的挑战。氟化治疗剂在管道药物和商业产品中得到了很好的体现,这一事实为将氟用作药物分析的分子探针提供了绝佳的机会。我们的目标是回顾19现代药物研发中的F魔角旋转核磁共振方法。将讨论微摩尔水平的多晶型筛选、结构解析以及在 Ångström 到亚微米分辨率的药物递送、稳定性和质量中的分子相互作用研究的应用。

更新日期:2022-05-25
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