Polysaccharide conjugate of carboxylic acid drug, preparation method thereof and application thereof

Abstract

The invention discloses a polysaccharide conjugate of carboxylic acid drug, a preparation thereof and application thereof. In the technical scheme, sub-alkyl diamine with 2-12 carbon atoms is used as a connecting arm, and a carboxylic acid drug and polysaccharide carboxyl are connected with each other through an amido link. Compared with the original carboxylic acid drug, the conjugate enhances the pharmacological effect, reduces the adverse effect and improve the safety. In addition, the conjugate can have the amphipathic performance through using the hydrophobic carboxylic acid drug, so as to be used as a carrier of a slightly soluble or sparingly soluble drug. The preparation method of the invention is simple, the process is mature, the yield is high, and the preparation method is applicable to industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a carboxylic acid drug-polysaccharide conjugate with good physiological activity and biodegradability as a drug carrier or a polymer prodrug, and the invention also relates to a preparation method of the conjugate and its application. Background technique [0002] In drug research, it is found that nearly 40% of drugs are insoluble in water, which easily leads to problems such as difficult preparation of preparations and low bioavailability. A hot and difficult point. [0003] In the preparation process, technologies such as microemulsion, liposome and solid dispersion are often used, or methods such as preparing the drug into a salt, adding a latent solvent, adding a co-solvent, and adding a surfactant are used to solubilize. However, as a drug carrier, liposomes still have disadvantages such as low encapsulation efficiency, unsatisfactory target distribution, and poor...

AI Technical Summary

Problems solved by technology

Some polysaccharide-drug conjugates are now in the research stage, but these conjugates still have the following defects: the inherent difficulties in the chemical reaction of the polymer make the synthesis conditions relatively harsh and the yield is low; When other functional groups are directly condensed, the linking arms used are more complex, such as amino acids or polypeptides; the grafting rate of some hydrophobic drugs is low, and the drug loading capacity is not high, making it difficult to achieve the dosage and affect the therapeutic effect, etc.

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