Application of sulfated polysaccharides in preparing medicament with anticoagulant active

A technology of anticoagulant activity and sulfated polysaccharide, which is applied in the field of biomedicine, can solve the problem of no heparin antiplatelet side effects, and achieve the effect of prolonging the prothrombin time, far-reaching significance, and easy operation of the reaction

Inactive Publication Date: 2008-07-02
DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies in recent years have found that sulfated polysaccharides have the same anticoagulant activity as heparin, but without the antiplatelet side effects of heparin

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Place a 100ml three-necked flask with a condenser and a stirring device in an ice-salt bath, add 16ml of pyridine, stir, make it fully cooled, and slowly add 2ml of chlorosulfonic acid with a dropping funnel. After the dropwise addition is completed, after a large amount of light yellow solid appears in the bottle, add 1.0 g of inulin, quickly move the three-necked bottle into a 60°C water bath, stir at a constant temperature for about 1 hour, cool to room temperature, pour the reaction solution into ice water, and wash with NaOH Adjust the pH value to 7.05, add four times the volume of 95% ethanol, let it stand at 4°C overnight, precipitate out, centrifuge, collect the precipitate, and dissolve the precipitate in a small amount of water. Alcohol precipitation and water dissolution were repeated 3 times. The product was dried under reduced pressure at 60°C to obtain sulfated inulin (SI 1 ).

Embodiment 2

[0023] Place a 100ml three-necked flask with a condenser and a stirring device in an ice-salt bath, add 30ml of pyridine, stir to make it fully cooled, and slowly add 6ml of chlorosulfonic acid with a dropping funnel. After the dropwise addition is complete, after a large amount of light yellow solid appears in the bottle, add 1.0 g of inulin, quickly move the three-necked bottle into a water bath at 100°C, stir at a constant temperature for about 1.5 h, cool to room temperature, pour the reaction solution into ice water, and use Adjust the pH value to 7.08 with NaOH, add four times the volume of 95% ethanol, let it stand at 4°C overnight, precipitate out, centrifuge, collect the precipitate, and dissolve the precipitate in a small amount of water. Alcohol precipitation and water dissolution were repeated 3 times. The product was dried under reduced pressure at 60°C to obtain sulfated inulin (SI 2 ).

Embodiment 3

[0025] 90 μl anticoagulated plasma and 10 μl SI at a final concentration of 1.6 mg / ml respectively 1 、SI 2 After mixing, incubate at 37°C for 1 min, then add 200 μl of PT reagent previously incubated at 37°C for 10 min into the above solution, and record the clotting time. According to the classic anticoagulant test method, SI 1 、SI 2 When the concentration is 1.6 mg / ml, the measured PT times are respectively greater than 600 seconds and 31.4±4.53, both of which are significantly higher than the blank control group’s PT time of 10.6±0.52, thus having significant anticoagulant activity.

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PUM

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Abstract

The invention relates to biomedicines, which is a drug used for the treatment and prevention of thrombosis diseases, in particular to an application of sulfated polysaccharide in the preparation of anti-prothrombin activity drugs. The invention has the advantages that: the inulin sources are rich, the preparation conditions of sulfated inulin derivatives are easy to operate, and the invention is applicable to large-scale production; the anti-prothrombin effect is significant, the development prospect is broad and the significance is far-reaching.

Description

technical field [0001] The invention relates to biomedicine, which is a medicine for treating and preventing thrombosis diseases, in particular the application of sulfated polysaccharides in the preparation of anticoagulant active medicines. Background technique [0002] Thrombosis or embolism is the final key link leading to heart, brain and peripheral vascular events, and is the direct cause of death and disability. The mechanism of arterial and venous system is slightly different. The arterial system is mainly activated by platelets, while the venous thrombosis is mainly activated by the coagulation system. [0003] Thrombosis disease is the most common cardiovascular and cerebrovascular disease, which seriously threatens human health. According to WHO reports, about 17 million deaths are caused by cardiovascular and cerebrovascular diseases each year, accounting for 1 / 3 of all deaths. In 2001, there were 931,108 deaths caused by cardiovascular and cerebrovascular diseas...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/737A61K9/06A61K9/08A61K9/10A61K9/14A61K9/16A61K9/20A61K9/48A61P7/02A23L1/30
Inventor 杜昱光栗衍华谭成玉胡建恩赵静玫白雪芳
Owner DALIAN INST OF CHEM PHYSICS CHINESE ACAD OF SCI
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