Gastric targeted drug carrier and preparation method thereof

Abstract

The invention relates to the field of drug carrier preparation, in particular to a gastric targeted drug carrier and a preparation method thereof. The gastric targeted drug carrier is prepared from the following raw materials: drug-containing emulsion and a crosslinking agent, wherein the drug-containing emulsion contains chitosan, chitosan quaternary ammonium salt and sodium glycerophosphate; and the crosslinking agent is used for crosslinking the emulsion into microspheres. The preparation method comprises the following steps: 1) preparing the drug-containing emulsion: with a aqueous solution of chitosan, chitosan quaternary ammonium salt and sodium glycerophosphate as an aqueous phase W, preparing the drug-containing emulsion with the aqueous phase, drugs and an oil phase containing anemulsifying agent; and 2) heating and stirring the drug-containing emulsion prepared in the step 1), crosslinking the chitosan quaternary ammonium salt and sodium glycerophosphate contained in the drug-containing emulsion to obtain gel microsphere suspension, heating the suspension and adding the crosslinking agent to carry out secondary crosslinking to solidify the gel microspheres. The drug carrier has the advantages of uniform and controllable grain size, high embedding rate and good dispersibility and simultaneously meets the requirements of the gastric targeted drug delivery carrier.

Description

technical field [0001] The invention relates to the field of drug carrier preparation, in particular, the invention relates to a stomach-targeting drug carrier and a preparation method thereof. Background technique [0002] Chitosan is a polysaccharide composed of glucosamine and N-acetylglucosamine copolymer, which is the product of deacetylation of chitin. Chitosan can be dissolved in dilute acid solution due to the free amino group on the molecular chain, so It has a wider range of uses than chitin. As a cationic biopolymer, chitosan has bioadhesion, biocompatibility and biodegradability, and its degradation products are non-toxic, non-immunogenic and non-carcinogenic. These unique properties of chitosan Its uniqueness makes it a biomedical carrier with broad application prospects. In the literature Chitosan-cellulose composite membrane for affinity purification of biopolymers and immunoadsorption, Journal of Membrane Science, 2002, 197: 185-197. L. Yang, W. W. Hsiao, P....

AI Technical Summary

Problems solved by technology

Although chitosan quaternary ammonium hydrogel microspheres have good bioadhesiveness, they disintegrate rapidly in the acidic environment of the stomach as a gastric drug delivery carrier. In the acidic release medium (pH=5.0), due to Dissociation and dissolution of chitosan quaternary ammonium salt microspheres, the drug embedded in it is also rapidly released into the surrounding medium, and all the drug embedded in it is released within 1 hour, which does not achieve good drug sustained release performance, and the shell Although polysaccharide has good pH sensitivity, it loses its targeting effect after reacting with the cross-linking agent, so chitosan and chitosan quaternary ammonium salt alone cannot meet the requirements of gastric targeted drug delivery carrier

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