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http://hdl.handle.net/1942/2528
Title: | Characterization of solid dispersions of itraconazole and hydroxypropylmethylcellulose prepared by melt extrusion, part II | Authors: | Van den Mooter, G Brewster, M Peeters, J Verreck, G Meublat, L Thimon, M Benoist, L. MULLENS, Jules VAN WERDE, Kristof Dressman, J Leuner, C Berghmans, H. Six, K |
Issue Date: | 2003 | Publisher: | KLUWER ACADEMIC/PLENUM PUBL | Source: | PHARMACEUTICAL RESEARCH, 20(7). p. 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. Conclusions. Solid dispersions of itraconazole and HPMC do not form a homogeneous phase. | Notes: | Katholieke Univ Leuven, Lab Farmacotechnol & Biofarm, Louvain, Belgium. Katholieke Univ Leuven, Lab Polymeerchem, Louvain, Belgium. Univ Frankfurt, Dept Pharmaceut Technol, D-6000 Frankfurt, Germany. LUC, Lab Anorgan & Fys Scheikunde, Diepenbeek, Belgium. Setaram Grp KEP, Lab Applicat, F-69300 Caluire Et Cuire, France. Johnson & Johnson Pharmaceut Res & Dev, Beerse, Belgium.Van den Mooter, G, Katholieke Univ Leuven, Lab Farmacotechnol & Biofarm, Louvain, Belgium. | Keywords: | itraconazole; solid dispersions; phase separation; MTDSC; dissolution | Document URI: | http://hdl.handle.net/1942/2528 | ISSN: | 0724-8741 | e-ISSN: | 1573-904X | DOI: | 10.1023/A:1024414423779 | ISI #: | 000183788900013 | Category: | A1 | Type: | Journal Contribution | Validations: | ecoom 2004 |
Appears in Collections: | Research publications |
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