Combining two antitubercular drugs, clofazimine and 4-aminosalicylic acid, in order to improve clofazimine aqueous solubility and 4-aminosalicylic acid thermal stability

Laurie BODART, Amélie Derlet, Xavier Buol, Tom Leyssens, Nikolay Tumanov, JOHAN WOUTERS (Supervisor)

Research output: Contribution to journalArticlepeer-review

Abstract

Four forms of a salt combining two antitubercular drugs, clofazimine and 4-aminosalicylic acid, are reported and the crystal structure of two of these forms are described. TG/DSC analysis of all four forms demonstrate an increase in the temperature at which degradation (upon decarboxylation) occurs in comparison to pure 4-aminosalicylic acid. Water solubility evaluation indicates a significant increase of the amount of clofazimine detected in water (10.26 ± 0.52 µg/mL for form I, 12.27 ± 0.32 µg/mL for form II, 7.15 ± 0.43 µg/mL for form III and 8.50 ± 1.24 µg/mL for form IV ) in comparison to pure clofazimine (0.20 ± 0.03 µg/mL).
Translated title of the contributionCombiner deux antituberculeux, la clofazimine et l'acide 4-aminosalicylique pour améliorer la solubilité aqueuse de la clofazimine et la stabilité thermique de l'acide 4-aminosalicylique
Original languageEnglish
JournalJournal of Pharmaceutical Sciences
Early online date22 Sep 2020
DOIs
Publication statusE-pub ahead of print - 22 Sep 2020

Keywords

  • 4-Aminosalicylic acid
  • Clofazimine
  • Differential scanning calorimetry
  • Polymorph
  • Salts
  • Solid-state
  • Solubility
  • Thermogravimetric analysis

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