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Production method of dalteparin sodium

A technology of darteparin and its production method, which is applied in the field of preparation of biochemical drugs, can solve the problems of poor product stability, high product yield, unqualified structure, etc., and achieve the effect of good stability and high product yield

Active Publication Date: 2011-01-12
DONGYING TIANDONG PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] The purpose of the present invention is to provide a method for producing dalteparin aimed at the above-mentioned defects in the prior art, which overcomes the defects of unqualified product structure and poor product stability produced by the traditional process, and the produced product has the European standard product structure of dalteparin Consistent with properties, good stability and high product yield

Method used

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  • Production method of dalteparin sodium
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Examples

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Embodiment 1

[0014] Example 1: Take high-quality heparin sodium, add purified water to dissolve it to a concentration of 3% to 10%, adjust the pH to 1.0 to 3.0 with 2 to 6 mol / L hydrochloric acid, and then add 0.5 to 2.0 times the volume of dimethoxyethyl ether alkanes, adjust the temperature to 10-30°C, add 1.0%-3.0% sodium nitrite, stir for 30-90 minutes, and control the temperature at 10-30°C; after the degradation is completed, adjust the pH to 8-10, and then add 0.5% ~2% sodium borohydride, stirred for 15 hours. Then adjust the pH to 3.0-4.0 with hydrochloric acid, adjust the pH to 6-8 after reacting for 5-30 minutes, add 1.5-3 times the amount of 92% ethanol for precipitation, and place it for 6-24 hours. Add purified water to dissolve the obtained precipitate to a concentration of 5% to 20%, adjust the pH to 6 to 8, filter with a 0.65um filter membrane, put the filtrate into a UV sterilizer and irradiate it for 5 to 10 minutes, add 1.5 to 3 times the amount of 92% ethanol to precipi...

Embodiment 2

[0015] Example 2: Dalteparin is achieved through the following process, adding heparin sodium into purified water to dissolve to a concentration of 3% to 10%, adjusting the pH to 1.0 to 3.0 with 4mol / L hydrochloric acid, and then adding 0.5 to 2.0 times the volume of the solution Dimethoxyethane, adjust the temperature to 10-30°C, add 1.0%-3% sodium nitrite, stir for 30-90 minutes, and control the temperature at 10-30°C; after the degradation is completed, adjust the pH to 8-10 , Then add 0.5% ~ 2% sodium borohydride, and stir the reaction for 15h. Then adjust the pH to 3.0-4.0 with hydrochloric acid, adjust the pH to 6-8 after reacting for 5-30 minutes, add 1.5-3 times the concentration of 90%-95% ethanol for precipitation, and place it for 6-24 hours. Add the obtained precipitate into purified water to dissolve to a concentration of 5% to 20%, adjust the pH to 6 to 8, filter with a 0.65um filter membrane, put the filtrate into a UV sterilizer and irradiate it for 5 to 10 min...

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Abstract

The invention relates to a production method of dalteparin sodium. The production method comprises the following steps: adding methylic organic solvent into heparin sodium solution; under specific temperature and acidic conditions, reacting with nitrous acid to cause deamination on N-sulfuric-base aminoglucose residues, so that rearrangement reaction occurs, thereby causing glycosidic bond rupture between aminoglucose and uronic acid and forming 2,5-dehydrated mannitose terminal residue; carrying out further treatment to obtain stable 2,5-dehydrated mannitol terminal, thereby obtaining the crude product of dalteparin sodium of which the molecular weight is 5600-6400 Daltons; and decoloring the crude product of dalteparin sodium by oxidizing and hydroxylating, settling with ethanol, and freeze drying or vacuum drying to obtain the finished product of dalteparin sodium. The invention overcomes the defects of disqualified product structure and poor product stability in the traditional production technique; the product of the invention has the uniform structure and properties as the European standard sample structure; and the invention has the advantages of simple operation, high stability and high product yield, and can realize industrial production.

Description

1. Technical field: [0001] The invention relates to a preparation method of biochemical medicines, in particular to a production method of dalteparin. 2. Background technology: [0002] Dalciparin is an anticoagulant and antithrombotic drug, a type of low molecular weight heparin. Dalteparin is produced from heparin through depolymerization of acidic sodium nitrite, sodium borohydride reduction and ultraviolet modification, and decolorization to produce dalteparin. Internationally, the preparation method is relatively simple, all of which are degraded by nitrous acid aqueous solution, but under this condition, the internal structure of the product is damaged, and the structure confirmation is unqualified. The current usual production method is: dissolving the heparin sodium raw material in 1% acetic acid solution, adding a certain amount of sodium nitrite solution, controlling the pH value in the range of 2.3-4.0, stirring and reacting at a certain temperature for 1-4 hours...

Claims

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Application Information

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IPC IPC(8): C08B37/10
Inventor 刘伟李加耀乔德强李艳敏
Owner DONGYING TIANDONG PHARM CO LTD
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