Diversity in Itraconazole Cocrystals with Aliphatic Dicarboxylic Acids of Varying Chain Length

Research output: Contribution to journalArticleScientificpeer-review

Researchers

Research units

  • University of Helsinki
  • Orion Corporation
  • Harvard University
  • University of Jyväskylä

Abstract

The cocrystal formation potential of itraconazole, a potent antifungal drug, with C2-C10 aliphatic dicarboxylic acids has been investigated. Using two experimental screening techniques (solvent-assisted grinding and evaporation-based crystallization), the cocrystals of itraconazole with C2-C7 dicarboxylic acids have been successfully synthesized and characterized by powder X-ray diffraction, solid state nuclear magnetic resonance, Raman spectroscopy, and thermal analysis. The characterized multicomponent compounds include anhydrous cocrystals (malonic, succinic, glutaric, and pimelic acids), a cocrystal hydrate (adipic acid), and cocrystal solvates with acetone and tetrahydrofuran (oxalic acid). This study is the first to demonstrate the diversity in itraconazole cocrystals with a range of aliphatic dicarboxylic acids of variable carbon chain lengths.

Details

Original languageEnglish
Pages (from-to)4877-4884
Number of pages8
JournalCrystal Growth and Design
Volume13
Issue number11
Publication statusPublished - Nov 2013
MoE publication typeA1 Journal article-refereed

    Research areas

  • SOLID-STATE PROPERTIES, PHARMACEUTICAL COCRYSTALS, CO-CRYSTAL, SOLUBILITY ADVANTAGE, CARBOXYLIC-ACIDS, HYDROGEN-BONDS, DRUG, DISSOLUTION, IMPROVE, PHARMACOKINETICS

ID: 8688457