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A preparation method of heparin-derived polysaccharide mixture

A technology of heparin and bemiparin sodium, applied in the field of medicine, can solve the problems of complicated process, low yield, multiple separation steps, etc.

Active Publication Date: 2015-11-25
SHANGHAI SEANPHARM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, its preparation method has the following disadvantages: the process is cumbersome, requires multiple separation steps, and / or the yield is low

Method used

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  • A preparation method of heparin-derived polysaccharide mixture

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[0037] After extensive and in-depth research, the inventors unexpectedly found that by adding quaternary ammonium hydroxide base in batches for degradation reaction in the same system by improving the preparation method of the heparin-derived polysaccharide mixture, the heavy polysaccharide can be prepared efficiently, simply and stably. Low molecular weight heparin with an average molecular weight of 3000-4200 Daltons and does not necessarily include a step of separating the heparin between batch additions. The present invention has been accomplished on this basis.

[0038] As used herein, the terms "mixture of the invention" and "heparin-derived polysaccharide mixture of the invention" are used interchangeably. The term "heparin" refers to a polysaccharide with a molecular weight ranging from 2000 to 30000 Daltons.

[0039] Preparation

[0040] The invention provides a method for preparing a heparin-derived polysaccharide mixture, comprising the steps of:

[0041] (a) pro...

Embodiment 1

[0074] Preparation of heparin benzylethoxylate ammonium salt (raw material)

[0075] To an aqueous solution (1250 ml) of benzethonium chloride (250 g), a solution of commercially available heparin sodium (100 g) in water (1000 ml) was added. 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 then vacuum-dried to obtain 295 g of heparin benzethonium salt (white).

Embodiment 2

[0077] Preparation of heparin-derived polysaccharide mixture

[0078] 1. Heparin-derived polysaccharide mixture

[0079] The heparin benzethonium salt (10 g) obtained in Example 1 was dissolved in dichloromethane (50 ml), heated to 20° C. and maintained at the reaction temperature. Add benzyltrimethylammonium hydroxide (40%, w / v) methanol solution 9.6ml altogether to this solution, adding method is to add in 6 times, each adds 1.6ml, and the time interval of batching is 24 hours, thereby makes Heparin gradually degrades. After the last addition, the reaction was continued for 24 hours, so the total reaction time was 144 hours.

[0080] Add 60ml of 10% sodium acetate methanol solution to the reaction mixture, and stir to precipitate a precipitate, filter to obtain a filter cake, wash with methanol, and vacuum-dry to obtain a heparin-derived polysaccharide mixture (light yellow, 2.9g).

[0081] 2. Purification

[0082] Carry out purification with conventional method, the met...

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Abstract

The invention relates to a preparation method of a heparin-derived polysaccharide mixture. The preparation method comprises the following steps: 1, preparing a heparin quaternary ammonium salt solution which can be dissolved in an inertia medium; 2, adding a quaternary ammonium hydroxide to the heparin quaternary ammonium salt solution in a batch mode to carry out a degradation reaction; and 3, separating or purifying to obtain low molecular weight heparins with the weight-average molecular weight of 3000-4200 Daltons. The invention also provides the heparin-derived polysaccharide mixture prepared with the method of the invention. The method of the invention allows the low molecular weight heparins to be simply, efficiently and stably prepared.

Description

technical field [0001] The invention relates to the field of medicine, more specifically, to a preparation method of a heparin-derived polysaccharide mixture. Background technique [0002] Heparin is a mixture of sulfated polysaccharides of animal origin (pig or bovine), which has been widely used due to their good antithrombotic properties, 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, heparin has a number of deficiencies that 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 has a high risk of spontaneous bleeding, and the coagulation time must be monitored in clinical use, which b...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C08B37/10A61P7/02A61P9/10
Inventor 徐学明王海青贾龙顾玉兰
Owner SHANGHAI SEANPHARM