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• 영문명: Design of New Ptrenteral Aqueous Formulations of Fluconazole by the Use of Modified Cyclodextrins
• 발행기관: 대한약학회
• 저자명: 이소윤(So Yun Lee) 전인구(In Koo Chun)
• 간행물 정보: 『약학회지』제45권 제4호 (2001년), 357~356쪽, 전체 0쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 2001.08.31

영문 초록

The purpose of this study is to investigate the inf1uence of cyclodextrins (CDs): and different acids on the solubility of fluconazole, and to formulate its more concentrated parenteral aqueous solution. Solubility studies of fluconazole with β- CD, 2-hydroxypropyl-β-CD (HPCD), sulfobutyl ether β-CD (SBCD) and dimethyl-β-CD (DMCD) were performed. The aqueous solubility of fluconazole was measured in different concentrations of different acids with or without addition of CDs. Solubility of fluconazole increased in the rank order of β-CD 1H-NMR studies confined the formation of an inclusion complex of fluconazole with HPCD. It was also shown by the NMR studies that the complex formed was a 1:1 complex. Among the different acids used, maleic acid and phosphoric acid increased solubility of fluconazole. The lower the pH of solution is, the more fluconazole dissolved, regardless of acids. Addition of HPCD (50 mM) to acid solutions increased the solubility about two times. New fluconazole injections at a dose of 10 mg/ml could be prepared in aqueous solutions containing 10% HPCD or 15% SBCD. These parenteral solutions did not form any precipitates at 4oC and was very stable at elevated temperatures. These results demonstrate that it is possible to develop a parenteral aqueous solution of fluconaEole with a smaller injection volume using HPCD or SBCD.

키워드

Fluconazole complexation 2-hydroxypropyl-beta-cyclodextrin sulfobutyl ether beta-cyclodextrin solubilization injections.