Multi-core adhesive microspheres for loading water soluble low molecular medicament and preparation method thereof

Abstract

The invention discloses multi-core adhesive microspheres capable of loading a water soluble low molecular medicament. The microspheres are ionic cross-linked chitosan / gelatin microspheres, wherein acrylic resin microspheres for wrapping and controlling the releasing of the water soluble low molecular medicament are dispersed in the microspheres. A preparation method comprises the following steps of: dispersing or dissolving the medicament into solution of acrylic resin-containing organic solvent; preparing medicament-loading microsphere cores by an emulsification solvent volatilization method; dispersing the cores in the solution of chitosan and gelatin; preparing W / O type mixture from the mixture and oily ingredients; solidifying the gelatin at a low temperature and separating the microspheres from the oil phase; and finally performing cross linking with ionic cross-linking aqueous solution. The chitosan medicament-loading microspheres have the advantages of controllable particle size distribution, good release control effect of water soluble medicament, adjustable releasing rate, high biological adhesion, simple preparation method, and mild condition.

Description

technical field The invention relates to a multi-core adhesion microsphere which can be used to load water-soluble small molecule drugs and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background of the invention Gastric retention preparations are a class of preparations that can prolong the residence time of drugs in the stomach and increase the local concentration of drugs in the gastric mucosa. Gastric retention preparations are a good means of administration for drugs that are absorbed in the stomach or act locally in the stomach, such as antibacterial drugs used to fight ulcers caused by Helicobacter pylori. Gastric-adhesive preparations, which have been considered as a better gastric-retentive drug delivery system in recent years, have been extensively studied. Chitosan is a copolymer obtained by deacetylation of chitin, which has good biocompatibility. Due to the large number of amino groups in the molecular structure of chit...

AI Technical Summary

Problems solved by technology

Water-insoluble and enteric-soluble acrylic resins can be used as sustained-release materials to control the release of water-soluble small molecule drugs in an acidic environment, but due to their lack of adhesive properties, these two materials are only commonly used as sustained-release materials. Matrix tablet materials and enteric coating materials, but there is no report of using them for gastric retention sustained-release microspheres

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