19F Solid-state NMR characterization of pharmaceutical solids

IF 1.8 3区 化学 Q4 CHEMISTRY, PHYSICAL
Yong Du , Yongchao Su
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引用次数: 7

Abstract

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.

Abstract Image

19F药物固体的固体核磁共振表征
固体核磁共振作为一种高分辨率和多用途的光谱工具,已越来越多地被认为是表征原料药和产品的工具。然而,药物材料的分析通常是在天然同位素丰度和多组分系统中相对较低的药物负荷下进行的,因此受到低灵敏度的挑战。氟化疗法在管道药物和商业产品中很有代表性,这一事实为利用氟作为分子探针进行药物分析提供了极好的机会。本文综述了19F魔角自旋核磁共振方法在现代药物研究和开发中的最新进展。将讨论在微摩尔水平上的多晶筛选、结构解析以及在Ångström到亚微米分辨率下分子相互作用在药物传递、稳定性和质量方面的应用。
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来源期刊
CiteScore
5.30
自引率
9.40%
发文量
42
审稿时长
72 days
期刊介绍: The journal Solid State Nuclear Magnetic Resonance publishes original manuscripts of high scientific quality dealing with all experimental and theoretical aspects of solid state NMR. This includes advances in instrumentation, development of new experimental techniques and methodology, new theoretical insights, new data processing and simulation methods, and original applications of established or novel methods to scientific problems.
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