Fluorobenzoic acid coformers to improve the solubility and permeability of the BCS class IV drug naftopidil

Chem Commun (Camb). 2022 May 5;58(37):5582-5585. doi: 10.1039/d1cc07187d.

Abstract

Crystalline salts of the low solubility and low permeability drug naftopidil were investigated with mono-, di-, tri-, and tetrafluorobenzoic acids as coformers to show that 245TFBA (2,4,5-trifluorobenzoic acid) is the optimal salt with faster dissolution and high permeability, thereby opening the study of fluorinated coformers in pharmaceutical cocrystals and salts.

MeSH terms

  • Crystallization
  • Naphthalenes
  • Permeability
  • Piperazines
  • Salts* / chemistry
  • Solubility

Substances

  • Naphthalenes
  • Piperazines
  • Salts
  • naftopidil