Medicine-carring particulates composed of hydrophilic resin and hydrophobic resin and its preparation method

Abstract

The present invention belongs to medicine carrying resin particle and its preparation technology. The medicine carrying particle has matrix of hydrophobic resin and hydrophilic resin particles, which is dispersed inside the matrix, has medicine carried and is capable of forming aquogel. The preparation process of the medicine carrying particle includes preparing medicine carrying grain with aquogel of hydrophilic resin, preparing medicine carrying particle with matrix of hydrophobic resin and aquogel grain of hydrophilic resin, and freeze drying to form solid medicine carrying particle. The present invention has the advantages of high hydrophilic medicine enclosing rate up to 95 %, controlled and stable medicine release with period as long as half a month to one year, and well maintenance of the stability and bioactivity of protein and peptide during particle preparation, storage and medicine throwing.

Description

technical field [0001] The invention relates to a drug-loaded particle composed of a hydrophilic resin and a hydrophobic resin and a preparation method thereof, belonging to the drug-loaded resin particle and the preparation technology thereof. Background technique [0002] Drug-loaded microparticles based on polymer resins are a new type of drug delivery system, and have received extensive attention in the research and application of drug sustained and controlled release technology. At present, in scientific research and production practice, polymer resin drug-loaded particles have provided excellent slow-release or controlled-release properties for chemical drugs or genetic engineering drugs, showing broad application prospects. [0003] Nevertheless, there are still some unresolved problems in polymer resin-based drug-loaded particles, mainly in the following aspects: [0004] 1. The encapsulation efficiency of hydrophilic drugs (including chemical drugs and genetic engi...

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Problems solved by technology

Due to the high water solubility of the drug, in the process of extracting the oil phase solvent by the solvent evaporation method, according to the principle of distribution balance, a large amount of water-soluble drug will diffuse from the oil phase droplet to the outer water phase, which greatly reduces the oil phase liquid. Drug content in drug-loaded microparticles after droplet and solvent extraction, the encapsulation efficiency of microparticles is very low

[0006] 2. The controllability of drug release is not ideal, and the drug release performance is difficult to meet the requirements of clinical drug administration

At the same time, due to the degradation of the resin, the diffusion rate of the release medium in the microparticles is difficult to maintain stable. Therefore, the drug release rate varies greatly during the release cycle, and the release rate and cycle controllability are poor, and it is difficult to achieve the requirements of clinical administration. The drug release rate maintains a stable controlled release

[0008] 3. It is difficult to maintain drug stability and biological activity during the preparation, storage and administration of resin-loaded particles containing genetically engineered drugs

[0011] The disadvantage of resin drug-loaded microparticles carrying genetically engineered drugs is that it is difficult to maintain the stability of proteins and peptides during the preparation, storage and administration of drug-loaded microparticles: the internal water phase of drug-loaded microparticles in oil-in-water type during the preparation process is Protein aqueous solution, the protein surface is active, tends to adsorb on the interface formed by water / oil, this adsorption on the surface causes the expansion, inactivation and irreversible aggregation of the protein structure; the initial stage of the oil-in-oil-in-solid drug-loaded particles The sudden release of drugs is serious, which affects the controlled drug release effect of the microparticles and limits the application of drug-loaded microparticles; while the drug encapsulation efficiency of solid drug-loaded microparticles in water-in-oil-in-water is often low, which increases the drug loss during the preparation of microparticles. thus increasing the production cost of microparticles

During the storage of drug-loaded microparticles, the hydrophobic resin in the microparticles can easily lead to protein unfolding or aggregation: the hydrophobicity of the resin can reverse the conformation of the protein, and the acidic microenvironment of some resins (such as lactic acid-glycolic acid copolymers) can The acid-catalyzed hydrolysis of the protein changes the structure and conformation of the protein; the adsorption of the drug on the resin surface during the administration process is also likely to cause the unfolding of the protein molecule, which affects the stability and biological activity of the protein

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