Title: Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, Part II
Authors: Six, Karel ×
Berghmans, Hugo
Leuner, Christian
Dressman, Jennifer
Van Werde, Kristof
Mullens, Jules
Benoist, Luc
Thimon, Mireille
Meublat, Laurent
Verreck, Geert
Peeters, J
Brewster, Marcus
Van den Mooter, Guy #
Issue Date: Jul-2003
Series Title: Pharmaceutical Research vol:20 issue:7 pages:1047-1054
Abstract: PURPOSE: This study was done to elucidate the physical and pharmaceutical properties of itraconazole-HPMC dispersions and the influence of water on the phase separation. METHODS: Extrudates were prepared using a corotating twin-screw hot-stage extruder with fixed process parameters. Modulated-temperature differential scanning calorimetry (MTDSC) and DSC 111 were used to examine the mixing behavior of itraconazole and the carrier by evaluation of the glass transition region. High temperature diffuse reflectance infrared transform spectroscopy (HT-DRIFT) was performed to reveal interactions between itraconazole and HPMC. Dissolution was performed to investigate the pharmaceutical performance of the dispersions. RESULTS: Although the dissolution rate of itraconazole significantly increased, we found that the solid dispersions do not form a homogeneous system. A different picture was obtained depending on the way MTDSC analysis was performed, i.e., using open or closed sample pans. Water can evaporate in open pans, which allows itraconazole to interact with HPMC and leads to a partially mixed phase. Analysis in hermetically closed pans revealed a further phase separation as water remains on the sample and impedes the interaction between drug and polymer. CONCLUSION: Solid dispersions of itraconazole and HPMC do not form a homogeneous phase.
ISSN: 0724-8741
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Molecular Imaging and Photonics
Drug Delivery and Disposition
× corresponding author
# (joint) last author

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