Preparation method for granula made of alpha-alcoholic acid resin ,and its use

Abstract

The present invention belongs to the field of resin particle preparation. The resin particle is prepared with polylactic acid, polyglycolic adid, low molecular weight lactic acid-glycolic acid copolymer or their mixture as base material. The resin particle may be used in coating or carrying hydrophilic or hydrophobic medicine, bioactive macro molecule, cell, vaccine, and other chemical matter, such as cosmetics, pesticide, paint and dye. The present invention makes it possible to realize the control release of coated medicine in the period of one week to one month or even to one year with the low molecular weight poly-alpha-hydroxy acid resin to prepare medicine carrying particle.

Description

technical field [0001] The invention relates to a preparation method and application of poly-alpha-hydroxy acid resin micron particles, belonging to the preparation technology of resin particles. Background technique [0002] Drug-loaded microparticles prepared with resin as the base material are a new type of drug dosage form with broad application prospects. The drug-loaded particles produce synergistic effects through the water-absorbing swelling of the particles, the degradation of the resin and the elimination of degradation products, and control the diffusion of the drug from the particles to the release medium, so that the drug can be released slowly within a certain time range to achieve long-term sustained release and control of the drug. freed. [0003] So far, a variety of degradable polymer resins have attracted attention in the field of drug delivery systems. However, poly-alpha-hydroxyacid resins are the most extensively researched and have related preparatio...

AI Technical Summary

Problems solved by technology

[0004] (1) The release cycle of high molecular weight poly-α-hydroxyacid resin drug-loaded particles is at least one month, and it is impossible to achieve controlled release of drugs with a short release cycle (days to weeks): in clinical medication, the drug is Controlled release within a few days to a few weeks has high application value in many occasions: for example, injecting painkillers into patients after surgery, depending on the specific situation, it is most reasonable for the drug to be released within a few days to a few weeks

The release cycle of drug-loaded particles based on high-molecular-weight poly-alpha-hydroxyacid resin is at least one month. Only by disintegration can the drug contained in the microparticles be completely released, and it takes at least a month for the high molecular weight resin to degrade to a sufficiently low molecular weight to disintegrate the microparticles. Therefore, it is impossible to provide controlled release of drugs with a short release period

[0005] (2) Drugs encapsulated in high molecular weight polyα-hydroxyacid resin particles cannot maintain a stable release rate during the release period, especially the sudden release of drugs at the initial stage is serious, and the drug release performance cannot meet the requirements of clinical medication: During clinical administration, in order for the drug to exert its normal efficacy, the concentration of the drug in the blood must be kept within the effective blood concentration range (higher than the minimum effective concentration, lower than the poisoning limit concentration), which requires that the drug-loaded particles must remain relatively stable drug release rate

The drug release of high-molecular-weight polyα-hydroxyacid resin drug-loaded particles generally includes three stages: initial burst release stage, diffusion-controlled release stage, and degradation-controlled release stage. The release rate of each stage is different and the release rate of each stage is different. It cannot be kept stable, especially in the early stage of sudden drug release, which often makes the blood drug concentration greatly exceed the poisoning limit concentration in a short period of time, causing drug poisoning in the human body.

Therefore, this kind of drug-loading system cannot realize the stable release of drugs in the release cycle, and it is difficult to be widely promoted and applied in clinical drug administration.

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