Development of Novel Itraconazole-loaded Solid Dispersion without Crystalline Change with Improved Bioavailability

Title
Development of Novel Itraconazole-loaded Solid Dispersion without Crystalline Change with Improved Bioavailability
Author(s)
용철순최한곤박영준[박영준]현경희[현경희]오동훈[오동훈]프라바가[프라바가]양호준[양호준]여우현[여우현]이미경[이미경]
Keywords
SPRAY-DRYING TECHNIQUE; GELATIN MICROCAPSULE; BETA-CYCLODEXTRIN; DISSOLUTION; IBUPROFEN; PHARMACOKINETICS; FORMULATION; RATS; PARTICLES; POLYMERS
Issue Date
201008
Publisher
PHARMACEUTICAL SOC KOREA
Citation
ARCHIVES OF PHARMACAL RESEARCH, v.33, no.8, pp.1217 - 1225
Abstract
To develop a novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability, various itraconazole-loaded solid dispersions were prepared with water, polyvinylpyrroline, poloxamer and citric acid. The effect of carriers on aqueous solubility of itraconazole was investigated. Their physicochemical properties were investigated using SEM, DSC, and powder X-ray diffraction. The dissolution, bioavailability in rats and stability of solid dispersions were evaluated. Unlike conventional solid dispersion system, the itraconazole-loaded solid dispersion with relatively rough surface did not change crystalline form of drug. Our DSC and powder X-ray diffraction results suggested that this solid dispersion was formed by attaching hydrophilic carriers to the surface of drug without crystal change, resulting in conversion of the hydrophobic drug to hydrophilic form. The itraconazole-loaded solid dispersion at the weight ratio of itraconazole/polyvinylpyrroline/poloxamer of 10/2/0.5 gave maximum drug solubility of about 20 mu g/mL. It did not change the crystalline form of drug for at least 6 months, indicating that it was physically stable. It gave higher AUC, C(max) and T(max) compared to itraconazole powder and similar values to the commercial product, suggesting that it was bioequivalent to commercial product in rats. Thus, it would be useful to deliver a poorly water-soluble itraconazole without crystalline change with improved bioavailability.
URI
http://hdl.handle.net/YU.REPOSITORY/23881http://dx.doi.org/10.1007/s12272-010-0812-2
ISSN
0253-6269
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약학대학 > 약학부 > Articles
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