The purpose of this study was to investigate the formation of solid molecular dispersions of Itraconazole (ITZ) in a number of glassy polymers including PVP, crospovidone, PVP-EC, HPMCAS and HPMCAS-PEO to enhance its dissolution and achieve release control. Polarizing light microscopy was found to be more sensitive than DSC and XRD for detecting crystallinity. PVP, PVP-EC & crospovidone generated loading levels of ~20%, substantially greater than that of HPMCAS and HPMCAS-PEO (5%). The loaded ITZ was stabilized though molecular interactions with the polymer and reduced molecular mobility in a glassy polymer matrix. Overall, immediate release was achieve d using PVP and crospovidone, enteric delivery provided by HPMCAS, and controlled release generated with EC and PEO. Among all polymers studied, only ITZ in PVP failed to generate sufficient stability in the presence of moisture. In general, solid molecular dispersion is a useful approach to improve the poor solubility and bioavailability of Itraconazole.
| Identifer | oai:union.ndltd.org:TORONTO/oai:tspace.library.utoronto.ca:1807/18761 |
| Date | 12 February 2010 |
| Creators | Hong, Liu |
| Contributors | Lee, Ping I. |
| Source Sets | University of Toronto |
| Language | en_ca |
| Detected Language | English |
| Type | Thesis |
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