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Preparation method for amphiphilic konjac glucomannan cholesterol grafted polymer and application

A konjac glucomannan and cholesterol technology is applied in the preparation field of drug carrier material, carboxymethyl konjac glucomannan cholesterol graft, can solve problems such as unfavorable health, and achieve good biocompatibility and reaction conditions Gentle, easy-to-implement effect

Inactive Publication Date: 2012-04-04
CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

High cholesterol is unhealthy, but low cholesterol is equally deadly. Although medical experts recommend that the cholesterol level be kept below 200 mg / dl, if the value is lower than 160 mg / dl, various health problems will come to the door, including cancer

Method used

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  • Preparation method for amphiphilic konjac glucomannan cholesterol grafted polymer and application
  • Preparation method for amphiphilic konjac glucomannan cholesterol grafted polymer and application
  • Preparation method for amphiphilic konjac glucomannan cholesterol grafted polymer and application

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation of embodiment 1CHCKGM graft

[0028] (1) Synthesis of N-t-butoxycarbonyl-glycine cholesteryl ester (N-t-glycine-CH): cholesterol 1mmol (0.386g), N-tert-butoxycarbonyl-glycine 1.1mmol (0.1925g), 4-dimethylamino Pyridine 0.25mmol (0.031g), dissolved in 5ml of dichloromethane, then added 1.1mmol of dicyclohexylcarbodiimide (0.226g), stirred in an ice bath, reacted for 24h, after the reaction, filtered to remove the white precipitate Dicyclohexylurea, the solvent is removed at room temperature, the product is dissolved in a small amount of acetone, overnight in the refrigerator, the precipitated DCU is removed by filtration, and the solvent is evaporated to dryness to obtain solid N-tert-butoxycarbonyl-glycine cholesterol ester (N-t-glycine- CH).

[0029] (2) Synthesis of glycine cholesteryl ester (Glycine-CH): Dissolve the product in step (1) in 5 milliliters of dichloromethane, add 5 milliliters of trifluoroacetic acid with stirring in an ice bath, and re...

Embodiment 2

[0031] The preparation of embodiment 2CHCKGM graft

[0032] (1) Synthesis of N-t-butoxycarbonyl-glycine cholesteryl ester (N-t-glycine-CH): cholesterol 1mmol (0.386g), N-tert-butoxycarbonyl-glycine 1.5mmol (0.2625g) 4-dimethylaminopyridine 0.25mmol (0.031g), was dissolved in 10 milliliters of dichloromethane, then added 1.1mmol dicyclohexylcarbodiimide (0.226g), stirred in an ice bath, reacted for 24h, after the reaction was over, filtered to remove the white precipitate di Cyclohexylurea, remove the solvent at room temperature, the product is dissolved in a small amount of acetone, and overnight in the refrigerator, the DCU that is separated out is removed by filtration, and the solvent is evaporated to dryness to obtain solid N-tert-butoxycarbonyl-glycine cholesteryl ester (N-t-glycine-CH ).

[0033] (2) Synthesis of glycine cholesteryl ester (Glycine-CH): Dissolve the product in step (1) in 5 milliliters of dichloromethane, add 5 milliliters of trifluoroacetic acid with st...

Embodiment 3

[0035] The preparation of embodiment 3CHCKGM graft

[0036] (1) Synthesis of N-t-butoxycarbonyl-glycine cholesteryl ester (N-t-glycine-CH): cholesterol 1mmol (0.386g), N-tert-butoxycarbonyl-glycine 1.5mmol (0.2625g) 4-dimethylaminopyridine 0.5mmol (0.062g), dissolved in 5-10ml of dichloromethane, then added 1.1mmol of dicyclohexylcarbodiimide (0.226g), stirred in an ice bath, reacted for 18h, after the reaction, filtered to remove the white Precipitate dicyclohexylurea, remove the solvent at room temperature, dissolve the product in a small amount of acetone, overnight in the refrigerator, filter and remove the precipitated DCU, evaporate the solvent to obtain solid N-tert-butoxycarbonyl-glycine cholesteryl ester (N-t-glycine -CH).

[0037] (2) Synthesis of glycine cholesteryl ester (Glycine-CH): the product in step (1) was dissolved in 5 milliliters of dichloromethane, 5 milliliters of trifluoroacetic acid was added under stirring in an ice bath, and reacted for 3 h under st...

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Abstract

The invention specifically relates to a preparation method for an amphiphilic carboxymethyl konjac glucomannan cholesterol grafted polymer and application of the same in drug carrier materials, belonging to the technical field of functional polymer chemistry. According to the invention, the amphiphilic carboxymethyl konjac glucomannan cholesterol grafted polymer is prepared by reacting carboxymethyl konjac glucomannan activated by EDCI in DMF with cholesterylated amine; the grafted polymer forms stable nanometer micelles in a selective solvent through self assembly, and the micelles are used for enwrapping and slow release of drugs. The amphiphilic carboxymethyl konjac glucomannan cholesterol grafted polymer prepared in the invention has good biocompatibility and biodegradation performance and has a very good application prospect in the field of biomedicine.

Description

technical field [0001] The invention belongs to the technical field of functional polymer chemistry, and in particular relates to a preparation method of amphiphilic carboxymethyl konjac glucomannan cholesterol graft and its application in drug carrier materials. Background technique [0002] As a natural polymer material, polysaccharide has good biocompatibility and degradability. In addition, polysaccharides also have the characteristics of abundant resources and low processing costs. More importantly, most natural polysaccharide molecules contain hydrophilic groups such as carboxyl, hydroxyl and amino groups, which can have strong non-covalent bonding with functional macromolecules in organisms such as proteins , thereby affecting life activities. All these advantages endow natural polysaccharides with bright prospects as biomaterials (Macromolecules, 1993, 26:3062-3068). Amphiphilic polymers prepared from aliphatic segments and natural polysaccharides have degradabili...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/02A61K47/36
Inventor 李帮经哈伟张晟丁立生彭树林
Owner CHENGDU INST OF BIOLOGY CHINESE ACAD OF S
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