Journal
MOLECULES
Volume 26, Issue 15, Pages -Publisher
MDPI
DOI: 10.3390/molecules26154427
Keywords
pharmaceutical solids; cyclodextrins; fluconazole; inclusion complexes; dehydration; thermal analysis; X-ray diffraction; crystal structure; stability; phase solubility
Funding
- NRF (Pretoria)
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This study highlights the importance of identifying the multiple forms of a cyclodextrin API complex and controlling crystallization conditions. It also emphasizes the need to characterize these crystal forms in order to determine the extent of their potential physicochemical differences.
Inclusion complexes between cyclodextrins (CDs) and active pharmaceutical ingredients (APIs) have potential for pharmaceutical formulation. Since crystallization of a given complex may result in the isolation of multiple crystal forms, it is essential to characterize these forms with respect to their structures and physicochemical properties to optimize pharmaceutical candidate selection. Here, we report the preparation and characterization of two crystallographically distinct hydrated forms of an inclusion complex between beta-cyclodextrin (beta-CD) and the antifungal API fluconazole (FLU) as well as temperature-concentration conditions required for their individual isolation. Determination of crystal water contents was achieved using thermoanalytical methods. X-ray analyses revealed distinct structural differences between the triclinic (TBCDFLU, space group P1) and monoclinic (MBCDFLU, space group C2) crystal forms. Removal of the crystals from their mother liquors led to rapid dehydration of the MBCDFLU crystal, while the TBCDFLU crystal was stable, a result that could be reconciled with the distinct packing arrangements in the respective crystals. This study highlights (a) the importance of identifying possible multiple forms of a cyclodextrin API complex and controlling the crystallization conditions, and (b) the need to characterize such crystal forms to determine the extent to which their physicochemical properties may differ.
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