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서지반출
Development of Novel Itraconazole-loaded Solid Dispersion without Crystalline Change with Improved Bioavailability
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취소
  • Development of Novel Itraconazole-loaded Solid Dispersion without Crystalline Change with Improved Bioavailability
  • Development of Novel Itraconazole-loaded Solid Dispersion without Crystalline Change with Improved Bioavailability
저자명
Park. Young-Joon,Xuan. Jing-Ji,Oh. Dong-Hoon,Balakrishnan. Prabagar,Yang. Ho-Joon,Yeo. Woo-Hyun,Lee. Mi-Kyung,Choi. Han-Gon,Yong
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2010년|33권 8호|pp.1217-1225 (9 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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기타
이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

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.