19F Solid-state NMR characterization of pharmaceutical solids

Solid State Nucl Magn Reson. 2022 Aug:120:101796. doi: 10.1016/j.ssnmr.2022.101796. Epub 2022 May 25.

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.

Keywords: (19)F NMR; Amorphous solid dispersion; Drug products; Drug substances; Pharmaceuticals; Polymorphism; Quantification; Solid-state analysis.

Publication types

  • Review

MeSH terms

  • Fluorides
  • Fluorine* / chemistry
  • Magnetic Resonance Imaging*
  • Magnetic Resonance Spectroscopy / methods
  • Pharmaceutical Preparations / chemistry

Substances

  • Pharmaceutical Preparations
  • Fluorine
  • Fluorides