Micro-block-polymer used for long-acting slow-releasing preparation, and preparation method and application thereof

Abstract

The invention discloses a micro-block-polymer used for a long-acting slow-releasing preparation and a preparation method thereof. The micro-block-polymer includes a glycolides block and a component Ablock according to weight ratio of 1-5:4-8, wherein the component A is lactide, caprolactone, trimethylene carbonate or p-dioxanone; the molecular weight of the micro-block-polymer is 5,000-500,000; in the glycolides block, the average sequence length of glycolides is 3-5. According to the invention, by adjusting the microstructures, such as length and distribution, of the sequence of the glycolides block, the degradation speed and dissolubility of the polymer can be adjusted, thus adjusting the medicine slow-releasing function of the long-acting slow-releasing preparation. In the application,the selected polymer is 3-5 in LGG, has regular structure and moderated degradation speed, so that burst release of the medicine is avoided. In addition, the block property of the polymer is moderated, so that the polymer has high solubility in most of organic solvents, so that the micro-block-polymer is suitable for majority of preparation processes for medicine preparations.

Description

technical field [0001] The invention relates to the technical field of macromolecules, in particular to a micro-block polymer for long-acting sustained-release preparations, a preparation method and application thereof. Background technique [0002] Sustained-release preparation means that the drug is contained in the carrier matrix in the form of dissolution or dispersion. After acting on the human body, the drug can be released slowly and stably for a long time to achieve the effect of improving curative effect, reducing side effects and improving patient tolerance. The main dosage forms are microspheres, implants, gels, transdermal preparations, liposomes, micelles, etc. Among them, the long-acting sustained-release preparations have the characteristics of targetability, high drug stability, and long sustained-release period. In recent years, it has become a focus of intensive research by scholars from various countries. [0003] Long-acting sustained-release preparation...

AI Technical Summary

Problems solved by technology

[0003] Long-acting sustained-release preparations usually use degradable materials as carriers, and the drug release period can reach 2 weeks, 4 weeks, 12 weeks or even longer. The sustained-release objects are mainly polypeptides, proteins and some small molecule chemical drugs. It is mostly used to treat diseases such as tumors, mental disorders, and degenerative diseases. Although this type of carrier has been widely studied, there are still the following problems, such as long degradation time and poor solubility of the polymer, and the degradation rate is not easy to control, and it is easy to appear drug burst phenomenon

[0004] Due to the influence of the molecular structure and steric hindrance of the current long-acting sustained-release preparations, two different types of monomers uniformly and stably form copolymers, such as glycolide and caprolactone during the polymerization process, due to caprolactone Ester has low reactivity and slow polymerization rate, while glycolide has high reactivity and fast polymerization rate, so the reactivity ratios of the two are quite different. Using the existing preparation method, glycolide will complete polymerization quickly and form a high melting point And refractory polyglycolide, and most of the caprolactone did not participate in the reaction, it is still in the monomer state, and the reaction will form a two-phase separated mixture instead of a uniform and stable copolymer

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