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Method for separating and purify dermatansulfate and low-molecular heparan sulfate from sodium heparan product

A technology of heparan sulfate and dermatan sulfate, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve the problem that it is difficult to obtain a single component of mucopolysaccharide, and there is no pure dermatan sulfate. Heparan sulfate products come out and other problems, to achieve the effect of simple method

Active Publication Date: 2008-04-30
NANJING KING FRIEND BIOCHEM PHARMA CO LTD
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  • Summary
  • Abstract
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  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this method is difficult to obtain a single component of high-purity mucopolysaccharide
[0011] At present, there is no good method for the purification and separation of dermatan sulfate and heparan sulfate suitable for industrial production, so there is no pure dermatan sulfate or pure low molecular weight heparan sulfate products.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] (1) The raw material is 100g of by-products produced by heparin sodium, the measured optical rotation is -2.5 degrees, and the potency is 28USP u / mg. Dissolve the raw material in 1200ml of water, add 36g of sodium chloride, adjust the pH to neutral, add ethanol until the volume content reaches 36.5%, let stand for 3 hours, collect the precipitate and dehydrate and dry to obtain 55.4g of crude heparan sulfate.

[0023] The measured optical rotation of the crude heparan sulfate was +22.25 degrees, and the anticoagulant potency was 38 USPu / mg.

[0024] (2), add ethanol in the supernatant liquid that step (1) separates gained, make ethanol volume content reach 50%, leave standstill overnight, collect precipitation, add ethanol dehydration, dry, obtain dermatan sulfate crude product 40.9g.

[0025] The measured optical rotation of crude dermatan sulfate was -32.75 degrees, and the potency was 8USP u / mg.

[0026] (3), take 5 g of the dermatan sulfate crude product obtained i...

Embodiment 2

[0031] (1) The raw material is 100 g of by-products produced by heparin sodium, the measured optical rotation is +1.55 degrees, and the potency is 30 USP u / mg. Dissolve the raw material in 1200ml of 3% NaCl solution, adjust the pH to neutral, add ethanol until the volume content reaches 36.0%, let stand for 4 hours, collect the precipitate, dehydrate and dry to obtain 44.4g of crude heparan sulfate.

[0032] The measured optical rotation of the crude heparan sulfate was +27.25 degrees, and the anticoagulant potency: 40USP u / mg.

[0033] (2) Add ethanol to the supernatant obtained in step (1) until the volume content reaches 51%, overnight, collect the precipitate, dehydrate with ethanol, and dry to obtain 49.9 g of crude dermatan sulfate.

[0034] The measured optical rotation of the crude dermatan sulfate was -26.25 degrees, and the potency was 10 USP u / mg.

[0035] (3) Take 5 g of crude dermatan sulfate, dissolve it in 45 ml of water, adjust the pH to 2.7, add 0.03 gram of ...

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Abstract

The invention relates to a method to separate and purify dermatan sulfate and low molecule heparan sulfate from sodium heparin by-product. It uses the by-product of producing sodium heparin as raw material taking fractional precipitation through alcohol to gain raw dermatan sulfate; uses nitrite and nitrous acid ester compounding as oxidant to degrade the heparan sulfate into low molecule heparan sulfate and taking fractional precipitation through alcohol to separate high purity dermatan sulfate and low molecule heparin sulfate.

Description

technical field [0001] The invention relates to a method for separating and purifying dermatan sulfate and low molecular weight heparan sulfate from by-products of heparin sodium, and belongs to the field of mucopolysaccharide biopharmaceuticals. Background technique [0002] Dermatan sulfate is a mucopolysaccharide, usually mixed with other mucopolysaccharides in animal tissues. Dermatan sulfate is composed of (1-4)-iduronic acid-(1-3)-acetylamino-2-deoxy-4-O-sulfate-β-D-galactobiose basic unit, optical rotation-55 ~-63 degrees, anticoagulant potency ≤10USP u / mg, ratio of sulfate group to carboxylic acid group is 0.8~1.2. [0003] Pure dermatan sulfate has low anticoagulant potency, high activity of activated heparin cofactor II, and no bleeding side effects, so it has a good prospect as an antithrombotic drug. [0004] Heparan sulfate is a subcomponent of heparin, which exists in unseparated heparin and is called fast-moving heparin. Compared with slow-moving heparin, he...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/10C08B37/00A61K31/727
Inventor 唐明龙吴桂萍
Owner NANJING KING FRIEND BIOCHEM PHARMA CO LTD
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