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    • 2. 发明申请
    • TRANSMUCOSAL DELIVERY OF PHARMACEUTICAL ACTIVE SUBSTANCES
    • 药物活性物质的转运
    • US20070292387A1
    • 2007-12-20
    • US11847237
    • 2007-08-29
    • Sangyong JONEunhye LEEJin Ju LEEIn-Hyun LEE
    • Sangyong JONEunhye LEEJin Ju LEEIn-Hyun LEE
    • A61K38/21A61K38/20A61K38/22A61K38/19A61K38/28A61K38/26A61K31/722C07K9/00C07K14/52C07K14/54C07K14/56C08B37/08
    • A61K47/61A61K9/0034A61K9/0043A61K9/0048A61K9/0053A61K9/006C07K14/62
    • Provided is a conjugate including a pharmacologically active substance covalently bound to chitosan or its derivative and a method for transmucosal delivery of a pharmacologically active substance using the same. Specifically, a conjugate includes a pharmacologically active substance covalently bound via a linker to chitosan; and a pharmaceutical composition for transmucosal administration of a drug includes the aforementioned conjugate and a pharmaceutically acceptable carrier. Further provided is a method for in vivo delivery of a pharmacologically active substance via a transmucosal route, by covalent binding of the active substance with chitosan or its derivative via a linker. The conjugate in accordance with the present invention exhibits excellent absorption rate and biocompatibility in biological mucous membranes, particularly mucous membranes of the alimentary canal (especially the gastrointestinal tract), in vivo degradability, and superior bioavailability even with oral administration, thus enabling treatment of diseases via oral administration of a drug.
    • 提供了包含与壳聚糖或其衍生物共价结合的药理活性物质的缀合物和使用其的药理活性物质的经粘膜递送的方法。 具体地,缀合物包括通过连接体与壳聚糖共价结合的药理活性物质; 并且用于药物的经粘膜给药的药物组合物包括上述缀合物和药学上可接受的载体。 进一步提供了通过经粘膜途径体内递送药理活性物质的方法,通过活性物质与壳聚糖或其衍生物通过接头共价结合。 根据本发明的缀合物在生物粘膜,特别是消化道粘膜(特别是胃肠道)中表现出优异的吸收速率和生物相容性,体内降解性和即使口服给药也具有优异的生物利用度,因此能够治疗疾病 通过口服给药。