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Preparation of biomedical amino acid-polyether-polyester triblock copolymer

A technology of amino acid and copolymer, which is applied in the field of preparation of amino acid-polyether-polyester triblock copolymer, which can solve problems such as separation, easy exposure of hydrophobic ends, unstable structure, etc.

Inactive Publication Date: 2012-08-01
SUZHOU HAITE BIAO BIOLOGICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] So far, nanopolymer micelles are mainly diblock copolymers of polyether and polyol. This copolymer has the above-mentioned polymer properties, but there are also many shortcomings, mainly in the structure after encapsulating the drug. Not very stable, the main connection method between micelles and drugs is that the hydrophobic end and the insoluble drug form a self-assembled inclusion complex. In order to ensure the size of the particle, the hydrophilic end should not be too long, which will easily expose the hydrophobic end in the encapsulation structure , will cause the drug to separate and precipitate from the hydrophobic end. To solve this problem, CN 96197134.7 discloses a technology based on ordinary micelles to modify the hydrophilic end with end groups. CN 200580018124.1 discloses a technology to add nucleic acid As a stabilizer and other methods to prevent the premature precipitation of drugs
It should be noted that these methods do not change the structure of the micelle itself, so the early precipitation of the encapsulated drug is still not a good solution

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Take 50g of fully dried D,L-lactide and 50g of polyethylene glycol 2000, put them in a reaction kettle, add 0.07g of stannous chloride, vacuumize, heat to 140°C, and react for 12 hours to obtain a yellow liquid. After cooling to room temperature, centrifuge at a speed of 10,000 rpm for 20 minutes, and take the supernatant for the next step of reaction.

[0021] Take 100ml of the light yellow clear liquid obtained in the above steps, add 300ml of dichloromethane to dissolve, then add 15g of lysine and 0.15g of diisopropylethylamine, and stir at room temperature for 24 hours to obtain the reaction product; Anhydrous glacial diethyl ether was then added for precipitation, and the precipitate was concentrated and dried by a rotary evaporator at 55°C to obtain an amino acid-polyether-polyester copolymer.

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PUM

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Abstract

The invention belongs to the technical field of medical biological materials, and particularly relates to a preparation method of a biomedical amino acid-polyether-polyester triblock copolymer. The method comprises the following steps of: initiating lactone ring opening polymerization under a vacuum condition to prepare a polyether-polyester copolymer, and adding a polymer, amino acid, a catalyst and a solvent into a reaction kettle; and reacting to obtain an amino acid-polyether-polyester triblock copolymer, and removing water and the solvent left in a polymerization system to obtain the amino acid-polyether-polyester triblock copolymer. The method is easy to operate and is practicable; reaction conditions are easy to control; and the obtained copolymer has a stable structure, and can be used for entrapping slightly-soluble medicaments to meet the requirements of clinical treatment.

Description

technical field [0001] The invention belongs to the field of synthesis of medical biopolymer materials, in particular to the preparation of an amino acid-polyether-polyester triblock copolymer. Background technique [0002] In recent years, nanotechnology-based polymer micelles have received extensive attention. Compared with other drug carriers, polymer nanomicelle has good encapsulation and stable structure in blood; it is resistant to dilution and has long circulation characteristics; moderate particle size, strong penetration ability and certain targeting Sex; increase the solubility of drugs, and reduce the adverse reactions of poorly soluble drugs caused by solvents, etc. [0003] So far, nanopolymer micelles are mainly diblock copolymers of polyether and polyol. This copolymer has the above-mentioned polymer properties, but there are also many shortcomings, mainly in the structure after encapsulating the drug. Not very stable, the main connection method between mice...

Claims

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Application Information

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IPC IPC(8): C08G63/91C08G63/664A61K47/34
Inventor 不公告发明人
Owner SUZHOU HAITE BIAO BIOLOGICAL TECH
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