首页> 外国专利> Conjugate in which pharmacologically active substance and mucoadhesive polymer are covalently bonded, and method for transmucosal delivery of pharmacologically active substance using the same

Conjugate in which pharmacologically active substance and mucoadhesive polymer are covalently bonded, and method for transmucosal delivery of pharmacologically active substance using the same

机译:药理活性物质和粘膜粘附性聚合物共价结合的共轭物,以及使用其的经粘膜递送药理活性物质的方法

摘要

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.
机译:提供一种缀合物,其包括与壳聚糖或其衍生物共价结合的药理活性物质,以及使用其的经粘膜递送药理活性物质的方法。具体而言,缀合物包括经由接头与壳聚糖共价结合的药理活性物质;和用于透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。还提供了通过活性物质与壳聚糖或其衍生物经由连接体的共价结合,经由透粘膜途径体内递送药理活性物质的方法。根据本发明的缀合物在生物粘膜,特别是消化道(特别是胃肠道)的粘膜中显示出优异的吸收率和生物相容性,即使在口服给药时,体内降解性和优异的生物利用度,因此能够治疗疾病通过口服药物。

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