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.
提供的是一个包括药理活性物质与
壳聚糖或其衍
生物共价结合的共轭物,以及使用该共轭物进行药理活性物质经粘膜途径传递的方法。具体来说,该共轭物包括通过连接剂与
壳聚糖共价结合的药理活性物质;以及用于经粘膜途径给药的药物组合物包括上述共轭物和药学上可接受的载体。此外,提供了一种通过药理活性物质与
壳聚糖或其衍
生物通过连接剂共价结合的方式,经粘膜途径在体内传递药理活性物质的方法。根据本发明的共轭物在
生物粘膜,特别是消化道(尤其是胃肠道)的粘膜中表现出优异的吸收速率和
生物相容性,在体内可降解性,以及即使口服也具有优越的
生物利用度,从而使得通过口服给药治疗疾病成为可能。