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Method for preparing heparinoid polysaccharide

A technology of heparin and polysaccharides, applied in the field of medical polymers, can solve the problems of difficulty, influence, and comparison of anticoagulant activity

Inactive Publication Date: 2011-08-24
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 (usually commercially available chitin is sufficient, in the embodiment of the present invention, 60 mesh chitin with a degree of deacetylation of 9%) is dispersed into 200ml of phosphoric acid with a concentration of 85%, and stirred until the chitin After all is dissolved, add this solution to 4000ml of distilled water, stir quickly while adding, precipitate white gelatinous chitin, centrifuge to remove water, wash with distilled water to neutrality, and obtain acid-treated product. Disperse the acid-treated product in 1000ml of distilled water, stir under ice-water bath conditions, add 240mg Tempo and 8g NaBr to completely dissolve Tempo and NaBr, then add 480ml of 4% NaClO solution, continue to 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 50ml ethanol was added, the pH value was adjusted to neutral with 2M acetic acid, the solution wa...

Embodiment 2

[0021] Disperse 5g chitin powder (60 mesh, deacetylation degree 15%) in 90ml 65% phosphoric acid, stir until all the chitin is dissolved, add this solution to 300ml distilled water, stir quickly while adding, and precipitate white gum After the chitin is formed, the water is removed by centrifugal separation, and the precipitate is washed with distilled water to neutrality to obtain the acid-treated product. Disperse the acid-treated product in 150ml distilled water, stir under ice-water bath conditions, add 75mg Tempo and 1.5g NaBr to completely dissolve Tempo and NaBr, then add 40ml 10% NaClO solution, and continue to add 2M KOH solution dropwise to make During the reaction, the pH value of the solution stabilized at 9.6, reacted for 0.5h, and then added 10ml of methanol, adjusted the pH value to neutral with 4M HCl, the solution was purified by ultrafiltration, concentrated by distillation under reduced pressure, precipitated with acetone, and dried in vacuum to obtain 6-posi...

Embodiment 3

[0024] Disperse 2g of chitin powder (60 mesh, deacetylation degree 15%) in 38ml of 70wt% phosphoric acid, stir until all the chitin is dissolved, add this solution to 200ml of distilled water, stir quickly while adding, and precipitate white gum After the shape of chitin is centrifuged to remove water, it is washed with distilled water to neutrality to obtain an acid-treated product. Disperse the acid-treated product in 50ml of distilled water, stir under ice-water bath conditions, add 16mg Tempo and 0.8g NaBr to completely dissolve Tempo and NaBr, then add 16ml of 8% NaClO solution, and continue to add 2M Na 2 CO 3 The solution makes the pH of the solution 10.0 during the reaction, react for 0.5h, add 4.5ml of ethanol, adjust the pH to neutral with 3M phosphoric acid, dialyze the solution against distilled water for 72h, concentrate by distillation under reduced pressure, precipitate with anhydrous methanol, and dry in vacuum The 6-position selective oxidation reaction product ...

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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 method for preparing heparin-like polysaccharides, in particular to a method for preparing heparin-like polysaccharides with chitin as a raw material, a polymer compound similar in structure to heparin, and belongs to the field of medical polymers. Background technique [0002] Cardiovascular and cerebrovascular diseases are one of the three highest mortality diseases announced by the World Health Organization. The use of anticoagulant drugs is the main treatment for cardiovascular and cerebrovascular diseases. As a commonly used anticoagulant drug, heparin has been clinically used 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 also problems such as animal origin and easy to be contaminated during the preparation process. Therefore, the search for alternative heparin anticoagulant drugs has been It is a resear...

Claims

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Application Information

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