Oligose polysulfate and preparation process thereof

A sulfuric acid oligosaccharide and sulfate-based technology, applied in the field of biomedicine, can solve the problems of narrow effective dose range, difficulty in conventional heparin treatment, and uneven composition, and achieve no bleeding side effects, low anticoagulant potency, and anti-asthma effect Effect

Inactive Publication Date: 2003-10-22
SHANDONG UNIV
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Problems solved by technology

Although heparin has a potential role in the treatment of asthma, it is difficult to use heparin in conventional treatment because of its shortcomings such as narrow effective dose range, uneven composition, and strong anticoagulant activity leading to bleeding, which limits its use. applications in this

Method used

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Embodiment Construction

[0015] A preferred embodiment of the present invention is given below.

[0016] Polysulfated oligosaccharides are products obtained by deacetylating and degrading heparin, followed by polysulfating. The specific implementation steps are as follows:

[0017] (1) Heparin deacetylation: Take 10g of heparin, dissolve it in 100ml of anhydrous hydrazine-hydrazine sulfate (99:1) mixture, heat up to 95-100°C, react for 5-6 hours, after cooling, lyophilize, and then Soluble in water at 10% concentration, precipitate with 70% ethanol;

[0018] (2) Degradation: Dissolve the ethanol precipitate in step (1) in water at a concentration of 10%, adjust pH 2 to 3.5, add 0.3% sodium nitrite to react at room temperature for 2 hours, adjust pH to 7.0, and use 80% ethanol precipitation;

[0019] (3) Reduction of degradation products: the ethanol precipitate in step (2) was formulated into a 10% aqueous solution, and 0.1% sodium borohydride was added for reduction reaction for 15 hours. Adjust ...

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Abstract

The present invention belongs to the field of bio-medicine technology, in particular, it relates to a oligose polysulfate and its preparation method. The average molecular weight of the oligose polysulfate prepared by said method is about 300 dalton, and the molecular weight distribution range is between 1000-5500 dalton, and its sulfating extent in the molecule is high, the ratio value of sulfuric acid radical and carboxylic acid radical is 3-5, and its anticoagulant titer is less than 30 IU/mg. Said preparation method adopts hydrazinolysis to make heparin undergo the process of deacetylation, after it is chemically degraded, it is sulfonated so as to obtain the invented product with stronger action of resisting inflammation and resisting asthma.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a polysulfated oligosaccharide for treating asthma and a preparation method thereof. Background technique [0002] Through the research on the pathogenesis of asthma, it has been established that anti-inflammatory treatment is the primary treatment principle of bronchial asthma in the world. Currently used anti-asthma drugs include bronchodilators and hormonal anti-inflammatory drugs. The former can only relieve symptoms, while hormonal anti-inflammatory drugs can only be used in emergencies due to their relatively large side effects. In recent years, it has been reported that glycosaminoglycans such as heparin have anti-inflammatory and immunomodulatory effects, and the inhalation therapy of low-dose heparin has been used in anti-asthma research. Ahmed et al once reported the treatment of asthma with low molecular weight heparin in the US Patent "Therapeutic Method for As...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H3/06C07H11/00C08B37/00
Inventor 姬胜利崔慧斐迟延青石峰
Owner SHANDONG UNIV
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