Method for preparing heparinoid polysaccharide

A technology of heparin and polysaccharide, applied in the field of medical polymers, can solve the problems of influence, heparin is too different, and the content of 2-position acetyl group is not considered.

Inactive Publication Date: 2010-06-02
WUHAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since heparin also contains 2-position acetyl and 6-position carboxyl groups, simply introducing sulfate groups into chitosan cannot imitate heparin to the greatest extent, and there are also groups at the 6-position or 2-position of chitin or chitosan. The carboxymethyl group is introduced, but the large volume of the carboxymethyl group affects its function. In addition, the content of the 2-position acetyl group is not considered in the preparation of heparanoids using chitin / chitosan as raw materials. The structure of the heparin-like product obtained is too different from that of heparin, so its anticoagulant activity is difficult to match that of heparin

Method used

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  • Method for preparing heparinoid polysaccharide
  • Method for preparing heparinoid polysaccharide
  • Method for preparing heparinoid polysaccharide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Disperse 20g of chitin powder (commercially available chitin can be used, and in the embodiment of the present invention, chitin with 60 mesh and 9% degree of deacetylation) is dispersed in 200ml of phosphoric acid with a concentration of 85%, stirred, and the chitin is treated. After all the solution is dissolved, add this solution to 4000ml distilled water, stir rapidly while adding, precipitate white colloidal chitin, centrifuge to remove water, wash with distilled water until neutral, and obtain the acid-treated product. Disperse the acid-treated product in 1000ml of distilled water, stir in an ice-water bath, add 240mg Tempo and 8g NaBr to completely dissolve Tempo and NaBr, then add 480ml of 4% NaClO solution, and continuously add 0.5M NaOH solution dropwise to make the reaction During the process, the pH value of the solution was stabilized at 10.8, reacted for 1 hour, then added 50ml of ethanol, adjusted the pH value to neutral with 2M acetic acid, purified the s...

Embodiment 2

[0021]Disperse 5g of chitin powder (60 mesh, deacetylation degree 15%) into 90ml of 65% phosphoric acid, stir until the chitin is completely dissolved, add this solution to 300ml of distilled water, stir rapidly while adding, and precipitate a white gum After the chitin was formed, it was centrifuged to remove water, and the precipitate was washed with distilled water until neutral to obtain the acid-treated product. This acid treatment product is dispersed in 150ml distilled water, under ice-water bath condition, stir, add 75mg Tempo and 1.5g NaBr, Tempo and NaBr are completely dissolved, then add 40ml 10% NaClO solution, continue dripping the KOH solution of 2M to make During the reaction, the pH value of the solution was stabilized at 9.6, reacted for 0.5h, then added 10ml of methanol, adjusted the pH value to neutral with 4M HCl, purified the solution by ultrafiltration, concentrated by distillation under reduced pressure, precipitated with acetone, and dried in vacuo to ob...

Embodiment 3

[0024] Disperse 2g of chitin powder (60 mesh, deacetylation degree 15%) into 38ml of 70wt% phosphoric acid, stir until the chitin is completely dissolved, add this solution to 200ml of distilled water, stir rapidly while adding, and precipitate a white gum Centrifuge the chitin to remove water, wash with distilled water until neutral, and obtain the acid-treated product. Disperse the acid-treated product in 50ml of distilled water, stir in an ice-water bath, add 16mg of Tempo and 0.8g of NaBr to completely dissolve Tempo and NaBr, then add 16ml of 8% NaClO solution, and continue to drop 2M of NaBr 2 CO 3 Make the pH value of the solution during the reaction process 10.0, react for 0.5h, then add 4.5ml ethanol, adjust the pH value to neutral with 3M phosphoric acid, and then dialyze the solution against distilled water for 72h, distill and concentrate under reduced pressure, precipitate with anhydrous methanol, and dry in vacuo The 6-position selective oxidation reaction produ...

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Abstract

The invention discloses a method for preparing heparinoid polysaccharide. The heparinoid polysaccharide is prepared by chitin through phosphate treatment, a 6-bit selective oxidation reaction, deacetylation reaction, sulfonation reaction and/or a sulfation reaction, the substitution degree of sulfate groups thereof is between 0.3 and 1.35, and the molecular weight is between 0.40*104 and 1.5*104. The method has good repeatability; and the prepared heparinoid polysaccharide has a structure close to that of heparin, has higher anticoagulant activity, and expects to substitute the heparin to serve as an anticoagulant medicament.

Description

technical field [0001] The invention relates to a preparation method of heparan-like polysaccharides, in particular to a preparation method of heparan-like polysaccharides, which is a macromolecular compound similar in structure to heparin, by using chitin as a raw material, and belongs to the field of medical macromolecules. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the three diseases with the highest mortality rate announced by the World Health Organization, and the use of anticoagulant drugs is the main treatment for cardiovascular and cerebrovascular diseases. As a commonly used anticoagulant drug, heparin has been used clinically for more than 70 years. However, in clinical practice, about 2.6% of heparin users have spontaneous bleeding accidents. In addition, heparin is expensive, and there are problems such as being derived from animals and easy to be contaminated during the preparation process. Therefore, looking for alterna...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C08B37/10
Inventor 杨建红伍康张秋花杜予民
Owner WUHAN UNIV
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