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Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability.
Arch Pharm Res. 2010 Aug; 33(8):1217-25.AP

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 microg/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.

Authors+Show Affiliations

Research Center, Samil Pharmaceutical Co. Ltd., Anyang, 431-060, Korea.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Comparative Study
Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

20803125

Citation

Park, Young-Joon, et al. "Development of Novel Itraconazole-loaded Solid Dispersion Without Crystalline Change With Improved Bioavailability." Archives of Pharmacal Research, vol. 33, no. 8, 2010, pp. 1217-25.
Park YJ, Xuan JJ, Oh DH, et al. Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability. Arch Pharm Res. 2010;33(8):1217-25.
Park, Y. J., Xuan, J. J., Oh, D. H., Balakrishnan, P., Yang, H. J., Yeo, W. H., Lee, M. K., Choi, H. G., & Yong, C. S. (2010). Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability. Archives of Pharmacal Research, 33(8), 1217-25. https://doi.org/10.1007/s12272-010-0812-2
Park YJ, et al. Development of Novel Itraconazole-loaded Solid Dispersion Without Crystalline Change With Improved Bioavailability. Arch Pharm Res. 2010;33(8):1217-25. PubMed PMID: 20803125.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Development of novel itraconazole-loaded solid dispersion without crystalline change with improved bioavailability. AU - Park,Young-Joon, AU - Xuan,Jing Ji, AU - Oh,Dong Hoon, AU - Balakrishnan,Prabagar, AU - Yang,Ho-Joon, AU - Yeo,Woo Hyun, AU - Lee,Mi-Kyung, AU - Choi,Han-Gon, AU - Yong,Chul Soon, Y1 - 2010/08/28/ PY - 2010/03/10/received PY - 2010/05/20/accepted PY - 2010/05/11/revised PY - 2010/8/31/entrez PY - 2010/8/31/pubmed PY - 2010/12/14/medline SP - 1217 EP - 25 JF - Archives of pharmacal research JO - Arch Pharm Res VL - 33 IS - 8 N2 - 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 microg/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. SN - 0253-6269 UR - https://www.unboundmedicine.com/medline/citation/20803125/Development_of_novel_itraconazole_loaded_solid_dispersion_without_crystalline_change_with_improved_bioavailability_ L2 - https://dx.doi.org/10.1007/s12272-010-0812-2 DB - PRIME DP - Unbound Medicine ER -