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    • 5. 发明公开
    • 수불용성 쿠르쿠민의 수용화 방법
    • 水不溶性曲霉素的溶出方法,其细胞内没有损伤或损害其药物效力
    • KR1020040080385A
    • 2004-09-18
    • KR1020040017091
    • 2004-03-12
    • 주식회사 앤씨비아이티현대약품 주식회사
    • 정광회정인학
    • C07H15/20
    • C07C49/255C07H15/203C07H1/00
    • PURPOSE: A solubilization method of water-insoluble curcumin is provided, thereby effectively solubilizing the water-insoluble curcumin without loss of or damage to its pharmaceutical efficacy within a cell. CONSTITUTION: The solubilization method of water-insoluble curcumin represented by the formula(1) comprises sugar conjugation of water-insoluble curcumin with sugar selected from monosaccharide, disaccharide and polysaccharide. The solubilization method of water-insoluble curcumin comprises the steps of: independently reacting curcumin as a glucosyl adaptor with a compound of the formula(14), (15), (16), or (17) as glucosyl donor to prepare curcumin-tetraacetyl glucoside of the formula(4), curcumin-bis(tetraacetyl glucoside) of the formula(6), curcumin-triacetyl riboside of the formula(8), curcumin-heptaacetylmaltoside of the formula(10), or curcumin-bis(heptaacetylmaltoside) of the formula(11); and deprotecting curcumin-tetraacetyl glucoside of the formula(4), curcumin-bis(tetraacetyl glucoside) of the formula(6), curcumin-triacetyl riboside of the formula(8), curcumin-heptaacetylmaltoside of the formula(10), or curcumin-bis(heptaacetylmaltoside) of the formula(11) to prepare curcumin-monoglucoside of the formula(5), curcumin-diglucoside of the formula(7), curcumin-monoriboside of the formula(9), curcumin-monomaltoside of the formula(12) or curcumin-dimaltoside of the formula(13).
    • 目的:提供不溶于水的姜黄素的溶解方法,从而有效增溶不溶于水的姜黄素,而不会损坏细胞内药物的功效。 构成:由式(1)表示的水不溶性姜黄素的溶解方法包括水不溶性姜黄素与选自单糖,二糖和多糖的糖的糖缀合。 水不溶性姜黄素的溶解方法包括以下步骤:将作为葡糖基衔接剂的姜黄素与式(14),(15),(16)或(17)的化合物作为葡糖基供体独立地反应,制备姜黄素 - 四乙酰 式(4)的葡萄糖苷,式(6)的姜黄素双(四乙酰葡萄糖苷),式(8)的姜黄素 - 三乙酰基核糖,式(10)的姜黄素 - 七乙酰基麦芽糖苷,或姜黄素 - 双(七乙酰基麦芽糖苷) 的式(11); 和式(4)的姜黄素 - 四乙酰基葡萄糖苷,式(6)的姜黄素 - 双(四乙酰基葡萄糖苷),式(8)的姜黄素 - 三乙酰基核糖,式(10)的姜黄素 - 七乙酰基麦芽糖苷或姜黄素 (7)的姜黄素 - 二葡萄糖苷,式(9)的姜黄素 - 单二糖苷,式(9)的姜黄素 - 单甘露糖苷,式(11)的姜黄素 - 单葡萄糖苷,式 12)或式(13)的姜黄素 - dimaltoside。