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    • 2. 发明授权
    • Process for producing water-soluble hyaluronic acid modification
    • 生产水溶性透明质酸改性方法
    • US09394379B2
    • 2016-07-19
    • US13947716
    • 2013-07-22
    • Chugai Seiyaku Kabushiki Kaisha
    • Kenji YasugiTeruo NakamuraTsuyoshi ShimobojiMika Sato
    • C08B37/08C08J3/075A61K47/48C08J3/12C08L5/08
    • C08B37/0072A61K47/61C08J3/075C08J3/122C08L5/08
    • The present invention provides a water-soluble modified HA practically used as a drug carrier and a production method thereof. The present invention provides: a water-soluble modified hyaluronic acid, the residence time in blood of which is elongated to a practical level, which is produced by introducing a substituent into the carboxy group of the glucuronic acid of hyaluronic acid or a derivative thereof, via an amide bond, at a lower limit of an introduction ratio of 5 mole % or more, using a BOP condensing agent in an aprotic polar solvent; and a production method thereof. Moreover, by cross-linking the modified hyaluronic acid, the present invention provides a hyaluronic acid gel capable of extremely long drug sustained-release even at the same cross-linking functional group introduction ratio as that of the conventionally known gel.
    • 本发明提供实际上用作药物载体的水溶性改性HA及其制备方法。 本发明提供:通过将透明质酸的葡糖醛酸或其衍生物的羧基引入取代基而产生的水溶性改性透明质酸,其在血液中的停留时间延长到实用水平, 通过酰胺键,在引发比为5摩尔%以上的下限,使用BOP缩合剂在非质子传递极性溶剂中; 及其制造方法。 此外,通过交联改性透明质酸,本发明提供即使以与常规已知凝胶相同的交联官能团引入比例,能够极长的药物持续释放的透明质酸凝胶。