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Preparation method and application of amphiphilic polymer

An amphiphilic polymer and preparation technology, applied in the field of medicine, can solve the problems of many adverse reactions, poor absorption of insoluble drugs, and low bioavailability, achieve good tumor inhibition, improve bioavailability, and reduce toxic and side effects Effect

Inactive Publication Date: 2017-02-22
ZHENGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In view of the above situation, in order to solve the defects of the prior art, the purpose of the present invention is to provide a preparation method and application of an amphiphilic polymer, which can effectively solve the problems of poor absorption, poor curative effect, poor quality stability, and bioavailability of insoluble drugs. Low degree of pain, strong pain when using, and many adverse reactions

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] The preparation method of amphiphilic polymer of the present invention comprises the following steps:

[0023] (1) Mix 8.4g of maleic anhydride and 30ml of 2-octyl-dodecane Guerbet alcohol, stir magnetically at 60°C, and freeze the product at -20°C after 5 hours of reaction. After solidification, wash with methanol Mix 50ml of the mixed solution with water at a volume ratio of 4:6, wash the reaction product, remove excess unreacted maleic anhydride, and dry to obtain Guerbet eicosanol monoester maleate;

[0024] (2) Take 0.1g of initiator lauroyl peroxide, 9g of N-vinylpyrrolidone and 1g of Guerbet eicosanol monoester maleate obtained in step (1), add 150ml of n-heptane, and protect it under nitrogen for 70 ℃, mechanical stirring, a white precipitate was obtained;

[0025] (3) The white precipitate obtained in step (2) was washed 5 times with 150 ml of n-heptane at 40°C, filtered with suction, and dried at room temperature for 48 hours to obtain an amphiphilic polymer....

Embodiment 2

[0027] The preparation method of amphiphilic polymer of the present invention comprises the following steps:

[0028] (1) Mix 5.6g of maleic anhydride and 20ml of 2-octyl-dodecane Guerbet alcohol, stir magnetically at 80°C, and freeze the product at -10°C after reacting for 7 hours. After solidification, wash with methanol Mix 150ml of the mixed solution with water at a volume ratio of 2:8, wash the reaction product, remove excess unreacted maleic anhydride, and dry to obtain Guerbet eicosanol monoester maleate;

[0029] (2) Take 0.02g of the initiator lauroyl peroxide, 7g of N-vinylpyrrolidone and 3g of Guerbet eicosanol monoester maleate obtained in step (1), add 250ml of n-heptane, and protect it under nitrogen at 90 ℃, mechanical stirring, a white precipitate was obtained;

[0030] (3) The white precipitate obtained in step (2) was washed three times with 50 ml of n-heptane at 60°C, filtered with suction, and dried at room temperature for 24 hours to obtain an amphiphilic...

Embodiment 3

[0032] The preparation method of amphiphilic polymer of the present invention comprises the following steps:

[0033] (1) Mix 15g of maleic anhydride and 60ml of 2-octyl-dodecane Guerbet alcohol, stir magnetically at 70°C, and freeze the product at 0°C after 6 hours of reaction. After solidification, wash with methanol and water According to the volume ratio of 2:8 mixed solution 250ml, rinse the reaction product, remove excess unreacted maleic anhydride, dry to obtain Guerbet eicosanol monoester maleate;

[0034] (2) Take 0.2g of the initiator lauroyl peroxide, 8g of N-vinylpyrrolidone and 2g of Guerbet eicosanol monoester maleate obtained in step (1), add 170ml of n-heptane, and protect it under 80 ℃, mechanical stirring, a white precipitate was obtained;

[0035] (3) Wash the white precipitate obtained in step (2) with 250 ml of n-heptane at 70°C for 4 times, filter it with suction, and dry it at room temperature for 36 hours to obtain an amphiphilic polymer.

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Abstract

The invention relates to a preparation method and application of an amphiphilic polymer. The problems that an insoluble drug is poor in absorption and treatment effect and low in bioavailability and has more adverse effects can be effectively solved. According to the technical scheme, the amphiphilic polymer is formed by connecting a N-vinyl pyrrolidone monomer with maleic acid Guerbet eicosanol monoester, the maleic acid Guerbet eicosanol monoester is generated through esterification of maleic anhydride and 2-octyl-dodecane Guerbet alcohol, a free radical polymerization reaction is conducted in n-heptane by taking lauroyl peroxide as an initiating agent and taking N-vinyl pyrrolidone and the maleic acid Guerbet eicosanol monoester as monomers, and then the amphiphilic polymer is obtained. According to the preparation method and application of the amphiphilic polymer, the insoluble drug is embedded into polymeric micelles by taking the amphiphilic polymer as a carrier material to prepare an insoluble drug-loaded micelle injection, a very good tumor inhibiting effect is achieved, the toxicity is low, the water solubility of the insoluble drug can be enhanced, the bioavailability of the drug can be improved, and the toxic and side effects of the drug can be reduced.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a preparation method and application of an amphiphilic polymer. Background technique [0002] At present, carrier drug delivery systems, such as liposomes, nanoparticles and polymer micelles, have made gratifying progress in clinical practice as a new drug delivery system. As a member of the carrier drug delivery system, polymer micelles developed from amphiphilic copolymers have been favored in the past decade. It can not only be used as a micro-reservoir for many insoluble drugs, but also prevent the drug from being inactivated in the biological environment. Drug-loaded micelles are thermodynamically and kinetically stable systems with many excellent properties such as stability, long-term effect, and safety, which make polymer micelles an ideal delivery system for insoluble drugs, and are widely used in drug release, gene carriers and diagnostic preparations. It has been widely used ...

Claims

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Application Information

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IPC IPC(8): C08F226/10C08F222/16A61K31/4375A61K31/337A61K47/32A61K9/107A61P35/00
CPCA61K9/0019A61K9/1075A61K31/337A61K31/4375A61K47/32C08F226/10C08F222/165
Inventor 胡玉荣牛振喜陈杰张宁霞姚兴段少峰黄胜楠张军霞王卫萍刘莹吉梦飞李慧丽李元敏袁金秀徐鑫王娟赵建辉
Owner ZHENGZHOU UNIV
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