A micro-block polymer for long-acting sustained-release preparations and its preparation method and use

Abstract

The invention discloses a micro-block polymer for long-acting sustained-release preparations and a preparation method thereof. The micro-block polymer includes a glycolide block and A with a weight ratio of 1-5:4-8 Component block; the A component is lactide, caprolactone, trimethylene carbonate or p-dioxanone; the molecular weight of the micro-block polymer is 5000~500000; glycolide block The average sequence length of glycolide in the segment is 3 to 5; the micro-block polymer used for long-acting sustained-release preparations of the present invention adjusts the microstructure of the entire polymer by adjusting the segment sequence length and distribution of glycolide The degradation rate and solubility of the long-acting sustained-release preparation can be adjusted accordingly; the LGG used in this application is between 3 and 5, the structure of the polymer is regular, the degradation rate is moderate, and there will be no sudden release of the drug , and the blockiness of the polymer is moderate, the solubility in most organic solvents is good, and it is suitable for the preparation process of most pharmaceutical 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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