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A heparin-derived polysaccharide mixture and its preparation method and pharmaceutical composition

A technology for mixtures and polysaccharides, which is applied in the directions of drug combinations, medical preparations containing active ingredients, and pharmaceutical formulations, can solve the problems of increased cost, harm, and easy residues of guanidine organic bases.

Active Publication Date: 2015-12-09
SHANGHAI SEANPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the secondary salt formation will increase the cost, and the guanidine organic base is easy to remain in the finished product, causing harm

Method used

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  • A heparin-derived polysaccharide mixture and its preparation method and pharmaceutical composition
  • A heparin-derived polysaccharide mixture and its preparation method and pharmaceutical composition
  • A heparin-derived polysaccharide mixture and its preparation method and pharmaceutical composition

Examples

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preparation example Construction

[0037] In a preferred example of the present invention, the preparation method comprises the steps of:

[0038] 1. React heparin with a quaternary ammonium salt (preferably phenethylammonium salt, such as benzethonium chloride) in an inert solvent (such as water) to form a salt, thereby obtaining heparin benzethonium salt.

[0039] The weight ratio of heparin to quaternary ammonium salt (such as benzethonium chloride) is about 1:4, preferably 1:2.5-2.8.

[0040] Wherein, the reaction temperature and time are not particularly limited, usually the reaction temperature can be 4°C-60°C, preferably 10-50°C; the reaction time is usually 5 minutes-24 hours.

[0041] 2. In an inert solvent (such as dichloromethane), react heparin ammonium salt (such as heparin benzylethoxylate) with benzyl chloride to form heparin ester. Usually the degree of esterification of the formed heparin ester is 60%-99%, preferably 75%-95%. After the heparin ester is formed, it can be further reacted with a...

Embodiment 1

[0073] Preparation of heparin benzethonium salt

[0074] To an aqueous solution (1250 ml) of benzethonium chloride (270 g) was added a solution of commercially available heparin sodium (100 g) in water (1000 ml) (Note: heparin derived from porcine). After stirring for 30 minutes, a precipitate of heparin benzethonium salt formed. Then, the reaction mixture was filtered at room temperature to obtain a filter cake, which was washed with water and dried in vacuo to obtain heparin benzethonium salt (about 310 g).

Embodiment 2

[0076] Preparation of heparin-derived polysaccharide mixture

[0077] 1. Preparation of heparin benzyl ester sodium salt

[0078] Benzyl chloride (15ml) was added to a solution of heparin benzethonium salt (15g) in dichloromethane (75ml). The solution was heated to 35°C for 36 hours. Then 10% sodium acetate methanol solution (90ml) was added to precipitate the sodium heparin benzyl ester. The reaction mixture was filtered to obtain a filter cake which was rinsed with methanol and dried. Thus was obtained heparin benzyl ester (7.1 g) in the form of a sodium salt (abbreviated as "heparin benzyl ester sodium salt"). After determination, the degree of esterification was 91%.

[0079] 2. Heparin-derived polysaccharide mixture

[0080] The heparin benzyl ester (5 g) obtained above in the form of its sodium salt was dissolved in water (125 ml) and heated to 75°C. Sodium hydroxide (0.45 g) was added to this solution and the temperature was maintained at 75°C for 1.5 hours to deg...

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Abstract

A mixture of oligosaccharides of heparin derivatives and its preparation and medicament. The mixture is characterised by a molecular weight lying between 3100 and 4500 Daltons, a high anti factor Xa activity, a low anti factor IIa activity and anti-thrombotic activity.

Description

technical field [0001] The invention relates to a polysaccharide mixture derived from heparin, a preparation method thereof and a pharmaceutical composition containing the polysaccharide mixture. Background technique [0002] Heparin is a mixture of sulfated polysaccharides of animal (pig or bovine) origin. Because of their good antithrombotic properties, they have been widely used, such as the preparation of antithrombotic drugs, drugs for the treatment of cardiovascular diseases, and drugs for the treatment of cerebrovascular diseases. drugs etc. [0003] However, natural heparin has many drawbacks which limit the application of heparin. A major drawback is that excessive use of heparin can cause spontaneous bleeding, so the clotting time should be measured before each injection. In addition, heparin can cause allergic reactions, thrombocytopenia, osteoporosis, and spontaneous fractures. [0004] Heparin sodium has a high risk of spontaneous bleeding, and the coagulatio...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/727A61P7/02A61P9/00
CPCA61K31/715A61K31/727C08B37/0078C08L5/10A61P7/02A61P9/00
Inventor 徐学明
Owner SHANGHAI SEANPHARM
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