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시클로덱스트린과의 포접에 의한 케토코나졸의 용해성 및 용출 증가
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  • 시클로덱스트린과의 포접에 의한 케토코나졸의 용해성 및 용출 증가
저자명
박기배,안홍직,장영수,서보연,이광표,Park. Gee-Bae,Ann. Hong-Jik,Chang. Young-Soo,Seo. Bo-Youn,Lee. Kwang-Pyo
간행물명
藥劑學會誌
권/호정보
1994년|24권 2호|pp.85-94 (10 pages)
발행정보
한국약제학회
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정기간행물|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
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기타언어초록

Inclusion complexes of ketoconazole (KT) with ${alpha}-$, ${eta}-cyclodextrin$ (CD) and dimethyl-${eta}-cyclodextrin$ $(DM{eta}CD)$ in a molar ratio of 1:2 were prepared by freeze-drying and solvent evaporation methods. The interactions of KT with ${alpha}-CD$, ${eta}-CD$ and $DM{eta}CD$ in aqueous solution and in solid state were investigated by solubility study, infrared (lR) spectroscopy and differential scanning calorimetry (DSC). The stability constant of $KT-DM{eta}CD$ inclusion complex (lC) was found to be the largest among three inclusion complexes. Clear differences in IR spectra and DSC curves were observed between inclusion complexes and physical mixtures (PM) of KT-CDs. It was also shown by IR spectra and DSC curves that solvent evaporation method might be. superior to the freeze-drying method in preparing the inclusion complexes of KT-CDs. The dissolution rate of KT was markedly increased by inclusion complex formation with CDs in the buffer solution at pH 4.0 and pH 6.8. The mean dissolution time (MDT,min), which represents the rapidity of dissolution, was in the order of $KT-DM{eta}CD$ IC (3.20) < $KT-{eta}-CD$ IC (4.36) < $KT-{alpha}-CD$ IC (6.99) < $KT-{alpha}-CD$ PM (17.46)< $KT-{eta}-CD$ PM (19.36) < $KT-{eta}-CD$ PM (28.53). The dissolution rates of KT-CD ICsprepared by solvent evaporation method were faster than those of KT-CD ICs prepared by freeze-drying method.