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    • 2. 发明授权
    • Irinotecan preparation
    • 伊立替康制剂
    • US07846473B2
    • 2010-12-07
    • US11597435
    • 2005-05-31
    • Keisuke YoshinoShigenori NozawaMasashi IsozakiSeigo SawadaIkuo KatoTakeshi Matsuzaki
    • Keisuke YoshinoShigenori NozawaMasashi IsozakiSeigo SawadaIkuo KatoTakeshi Matsuzaki
    • A61K9/127
    • A61K9/1271A61K31/4745
    • Provided is an irinotecan formulation capable of supporting irinotecan and/or a salt thereof in a closed vesicle carrier at a high concentration and existing in blood for a long period of time by dramatically improved retentivity in blood compared to a conventionally known irinotecan liposome formulation. That is, an irinotecan formulation including a closed vesicle formed by a lipid membrane, in which irinotecan and/or a salt thereof is encapsulated at a concentration of at least 0.07 mol/mol (drug mol/membrane total lipid mol). There is an ion gradient between an inner aqueous phase and an outer aqueous phase in the irinotecan formulation. The closed vesicle is preferably liposome, in which only the outer surface of the liposome is preferably modified with a surface-modifying agent containing a hydrophilic polymer.
    • 本发明提供了一种伊立替康制剂,其能够通过显着提高血液中的保留性,与常规已知的伊立替康脂质体制剂相比,可以高密度地在密闭囊泡载体中以高浓度和血液中长时间地支持伊立替康和/或其盐。 也就是说,包括由脂质膜形成的封闭囊泡的伊立替康制剂,其中伊立替康和/或其盐以至少0.07mol / mol(药物mol /膜总脂质摩尔)的浓度包封。 伊立替康制剂中的内部水相和外部水相之间存在离子梯度。 封闭的囊泡优选为脂质体,其中仅脂质体的外表面优选用含有亲水性聚合物的表面改性剂改性。
    • 3. 发明申请
    • Liposome Preparation Containing Slightly Water-Soluble Camptothecin
    • 含有轻微水溶性喜树碱的脂质体制备
    • US20080193509A1
    • 2008-08-14
    • US11629869
    • 2005-06-17
    • Keisuke YoshinoShigenori NozawaYoshitaka OgataYasuo KurosakiSeigo SawdaIkuo KatoTakeshi Matsuzaki
    • Keisuke YoshinoShigenori NozawaYoshitaka OgataYasuo KurosakiSeigo SawdaIkuo KatoTakeshi Matsuzaki
    • A61K9/127A61K31/4375
    • A61K9/1272A61K31/4745
    • The present invention aims at providing a slightly water-soluble camptothecin liposome preparation with an excellent retention in blood for a drug, which can stably hold a slightly water-soluble camptothecin compound for a long period of time, whereby hydrolysis of an α-hydroxylactone ring in blood is suppressed and the slightly water-soluble camptothecin compound is kept in a structure in which the ring is not opened and which makes the compound effective as an antitumor-active drug, and, moreover, the liability of the drug to leave a liposome is advantageously reduced, so that it is possible to maintain the drug concentration in plasma for a long period of time after administration. This object is achieved by the liposome preparation as described in the specification. The liposome preparation according to the present invention includes a liposome preparation including as lipid components for forming a membrane a phospholipid and a fatty acid, and containing as a drug a lightly water-soluble camptothecin compound.
    • 本发明的目的在于提供一种在血液中具有优异的药物保留性的轻微水溶性喜树碱脂质体制剂,其能够长时间稳定地保持轻微的水溶性喜树碱化合物,从而水解α-羟基内酯环 在血液中被抑制,轻微的水溶性喜树碱化合物保持在不打开环的结构中,并且使得化合物作为抗肿瘤活性药物有效,此外,药物离开脂质体的责任 有利地减少,使得可以在施用后长时间维持血浆中的药物浓度。 该目的通过如说明书中所述的脂质体制备来实现。 根据本发明的脂质体制剂包括脂质体制剂,其包含作为形成磷脂和脂肪酸的膜的脂质成分,并且作为药物含有轻度水溶性的喜树碱化合物。