Low-molecular-weight polysaccharide sulfate and preparation method and application thereof

A technology of diester sodium alginate and low molecular weight, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve problems such as adverse reactions and weakness, achieve improved solubility, reduce bleeding side effects, and prepare The method is simple and fast, and the effect

Active Publication Date: 2012-03-21
MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Because of this, PSS is relatively weak in basic research on the material basis of its drug effects, quality control, and structure-activity relationship, which leads to the diversity of drug effects...

Method used

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  • Low-molecular-weight polysaccharide sulfate and preparation method and application thereof
  • Low-molecular-weight polysaccharide sulfate and preparation method and application thereof
  • Low-molecular-weight polysaccharide sulfate and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0020] Example 1: Preparation of Low Molecular Weight Sodium Alginate Diester

[0021] 9 g of sodium alginate diester (weight average molecular weight about 14kDa) was weighed and dissolved in 120 mL of distilled water to prepare a 7.5% sodium alginate diester solution. Add 0.1mol·L -1 FeSO 4 solution and 30% H 2 O 2 Aqueous solution, so that Fe in the reaction system 2+ and H 2 O 2 The concentrations reached the indicated final concentrations shown in Table 1. The reaction was sealed and shaken at 60 °C for 0.5 h. After the reaction was completed, follow 3 mg·mL -1 The amount of reaction system is added ascorbic acid to consume H 2 O 2 The reaction was terminated, rapidly cooled, 3 volumes of 95% ethanol were added, and the mixture was allowed to stand overnight at 4°C. Centrifuge at 3000r·min-1 for 20min to separate the precipitate and supernatant. Dissolve the precipitate in a small amount of water, pass through 732 cation exchange resin for desalting and purif...

Embodiment 2

[0029] Example 2: The main pharmacological activity experiment of low molecular weight sodium alginate diester

[0030] The main pharmacological activity test results of the low molecular weight sodium alginate diester prepared by the method of the present invention are as follows.

[0031] A: Anticoagulant activity test of low molecular weight sodium alginate diester

[0032] Insert a glass capillary tube into the posterior venous plexus of the mouse medial canthus to collect blood, and record the time from blood collection to the appearance of blood coagulation as an indicator for testing the coagulation time; after the tail of the mouse is decapitated, the time from the natural outflow of blood to the natural stop of blood is recorded. For testing the indicators of bleeding time. The above two indicators were used to detect and compare the anticoagulant effect and bleeding risk of low molecular weight sodium alginate diester with different molecular weights. The test resul...

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Abstract

The invention provides a low-molecular-weight polysaccharide sulfate and a preparation method and application of the low-molecular-weight polysaccharide sulfate. The constitutional formula of the low-molecular-weight polysaccharide sulfate includes that the molecular skeleton of the constitutional formula is a binary linear block polymer composed of beta-D-(1,4)-mannuronic acid and alpha-L-(1,4)-guluronic acid. In the constitutional formula, R=Na or CH2CHOHCH3, R1=H or SO3Na, in each saccharide link, at least one R1=SO3Na, m+n is smaller than or equal to 25, the weight-average molecular weight of the low-molecular-weight polysaccharide sulfate ranges from 3kDa to 9kDa, and dispersion of molecular weight distribution ranges from 1.20 to 1.70. The low-molecular-weight polysaccharide sulfatecan be applied to treatment of anticoagulation and anti-thrombus diseases, reduces risk of haemorrhagia and avoids anaphylaxis, and supplies raw materials for wide bioactivity of a series of low-molecular-weight PSS (polysaccharide sulfate) products.

Description

technical field [0001] The invention relates to the field of antithrombotic and anticoagulant drugs, in particular to a low molecular weight sodium alginate diester and a preparation method and application thereof. Background technique [0002] Propylene glycol alginate sodium sulfate (PSS) is based on the oligomeric sodium alginate molecule, and propylene glycol ester group and sulfonyl group are modified on the 6-position carboxyl group and the 2, 3-position hydroxyl group of the sugar ring, respectively. The weight-average molecular weight of the PSS API is generally 10-20kDa, the molecular weight distribution width is less than 1.80, and the organic sulfur content is 9%-13%. As a heparin-like drug, PSS has the functions of lowering blood viscosity, anticoagulation, lowering blood lipids, improving microcirculation, etc. It plays an important role in the prevention and treatment of ischemic cardiovascular and cerebrovascular diseases, hyperviscosity syndrome and other hyp...

Claims

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Application Information

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IPC IPC(8): C08B37/04A61K31/734A61P7/02
Inventor 李春霞管华诗孙杨李海花何小溪于广利
Owner MARINE BIOMEDICAL RES INST OF QINGDAO CO LTD
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