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.
Original language | English |
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Pages (from-to) | 4877-4884 |
Number of pages | 8 |
Journal | Crystal Growth and Design |
Volume | 13 |
Issue number | 11 |
DOIs | |
Publication status | Published - Nov 2013 |
MoE publication type | A1 Journal article-refereed |
Keywords
- SOLID-STATE PROPERTIES
- PHARMACEUTICAL COCRYSTALS
- CO-CRYSTAL
- SOLUBILITY ADVANTAGE
- CARBOXYLIC-ACIDS
- HYDROGEN-BONDS
- DRUG
- DISSOLUTION
- IMPROVE
- PHARMACOKINETICS