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서지반출
Preparation and Characterization of Solid Dispersions of Itraconazole by using Aerosol Solvent Extraction System for Improvement in Drug Solubility and Bioavailability
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  • Preparation and Characterization of Solid Dispersions of Itraconazole by using Aerosol Solvent Extraction System for Improvement in Drug Solubility and Bioavailability
  • Preparation and Characterization of Solid Dispersions of Itraconazole by using Aerosol Solvent Extraction System for Improvement in Drug Solubility and Bioavailability
저자명
Lee. Si-Beum,Nam. Kyung-Wan,Kim. Min-Soo,Jun. Seoung-Wook,Park. Jeong-Sook,Woo. Jong-Soo,Hwang. Sung-Joo
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2005년|28권 7호|pp.866-874 (9 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

The objective of this study was to elucidate the feasibility to improve the solubility and bioavailability of poorly water-soluble itraconazole via solid dispersions by using supercritical fluid (SCF). Solid dispersions of itraconazole with hydrophilic polymer, HPMC 2910, were prepared by the aerosol solvent extraction system (ASES) under different process conditions of temperature/pressure. The particle size of solid dispersions ranged from 100 to 500 nm. The equilibrium solubility increased with decrease (15 to 10 MPa) in pressure and increase (40 to $60^{circ}C$) in temperature. The solid dispersions prepared at $60^{circ}C$/15 MPa showed a slight increase in equilibrium solubility (approximately 27-fold increase) when compared to pure itraconazole, while those prepared at $60^{circ}C$/10MPa showed approximately 610-fold increase and no endothermic peaks corresponding to pure itraconazole were observed, indicating that itraconazole might be molecularly dispersed in HPMC 2910 in the amorphous form. The amorphous state of itraconazole was confirmed by DSC/XRD data. The pharmacokinetic parameters of the ASES-processed solid dispersions, such as $T_{max},;C_{max},;and;AUC_{0-24h}$ were almost similar to $Sporanox_{circledR}$ capsule which shows high bioavailability. Hence, it was concluded that the ASES process could be a promising technique to reduce particle size and/or prepare amorphous solid dispersion of drugs in order to improve the solubility and bioavailability of poorly water-soluble drugs.