Citicoline sodium compound and new method thereof

A technology of citicoline sodium and citicoline, which is applied in the medical field, can solve the problems of undisclosed purification of citicoline sodium compounds, and achieve the effects of simple and easy process, high yield and optimized product quality

Inactive Publication Date: 2011-04-13
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] For these impure products, prior art does not disclose the method for purifying citicoline sodium compound, in fact, those skilled in the art have general experience clearly Knowing the various di

Method used

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  • Citicoline sodium compound and new method thereof
  • Citicoline sodium compound and new method thereof
  • Citicoline sodium compound and new method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Example 1 Purification of Citicoline Sodium

[0036] (1) Dissolve 100g of crude citicoline sodium with a purity of 96.8% in 120ml of water, heat for 10min, add 0.24g of activated carbon, keep at 60℃ and stir for 10min, filter and decarburize, and collect the filtrate;

[0037] (2) Slowly add 1mol / L hydrochloric acid to the obtained filtrate, stir the reaction until the pH of the solution is 2.2, and let it stand overnight in refrigeration to produce citicoline precipitation, and suction filtration to obtain 89.5g of citicoline;

[0038] (3) Put the 89.5g citicoline obtained in the previous step on the column, and apply the stationary phase filler to a preparative chromatographic column selected from silica gel for separation and purification, with a volume ratio of 1:3 chloroform and pH 9.0 hydroxide The mixed solution of sodium solution is the mobile phase for elution; the flow rate is 3.8ml / min, the column temperature is 35°C; the fractions are collected in sections, and the...

Embodiment 2

[0040] Example 2 Purification of Citicoline Sodium

[0041] (1) Dissolve 100g of crude citicoline sodium with a purity of 96.8% in 120ml of water, heat for 30min, add 0.6g of activated carbon, keep at 60℃ and stir for 20min, filter and decarburize, and collect the filtrate;

[0042] (2) Slowly add 1.5 mol / L phosphoric acid to the obtained filtrate, stir the reaction until the pH of the solution is 1.5, and let it stand overnight in cold storage to produce citicoline precipitation, and suction filtration to obtain 89.8 g of citicoline;

[0043] (3) The 89.8g citicoline obtained in the previous step was applied to the column, and the stationary phase filler was selected from the preparative chromatographic column of alumina for separation and purification. The volume ratio was 1:3 chloroform and pH 8.0 carbonic acid The mixed solution of sodium hydrogen solution is the mobile phase for elution; the flow rate is 3.0ml / min, the column temperature is 30°C; the fractions are collected in s...

Embodiment 3

[0045] Example 3 Purification of Citicoline Sodium

[0046] (1) Dissolve 100g of crude citicoline sodium with a purity of 96.8% in 120ml of water, heat for 20min, add 0.48g of activated carbon, keep at 60℃ and stir for 30min, filter and decarburize, and collect the filtrate;

[0047] (2) Slowly add 2.0 mol / L of oxalic acid to the obtained filtrate, and stir the reaction until the pH of the solution is 3.0 to produce citicoline precipitation, and suction filtration to obtain 89.2 g of citicoline;

[0048] (3) The 89.2g citicoline obtained in the previous step was applied to the column, and the stationary phase filler was selected from the preparative chromatographic column of alumina for separation and purification. The volume ratio was 1:3 chloroform and pH 10.0 hydrogen. The mixed solution of sodium oxide solution is the mobile phase for elution; the flow rate is 5.0ml / min, the column temperature is 35°C; the fractions are collected in sections, and the eluents with a content greate...

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Abstract

The present invention provides a citicoline sodium compound and new method thereof, wherein purification is performed via active carbon adsorption, acidification reaction and preparing chromatographic column, finally a citicoline sodium compound with high purity is obtained; the shortage of low raw material purity in the prior production is recovered, simultaneously the quality of preparation product is improved, and side effects are reduced. Compared with the prior art, the method has the advantages of simple and easy technology, low cost, high yield and high product purity; the method is suitable for industrial production; and the citicoline sodium prepared by the refining method of the present invention is suitable for being used in preparation of neural activation agent pharmaceuticals.

Description

Technical field [0001] The invention relates to a citicoline sodium compound and a new method thereof, and belongs to the technical field of medicine. Background technique [0002] Citicoline sodium is the abbreviation of cytosine diphosphate choline. It is the precursor substance of phospholipid phosphatidylcholine and is an essential coenzyme for the synthesis of lecithin. Its molecular formula is C 14 H 25 N 4 NaO 11 P 2 , The structural formula is: [0003] [0004] Citicoline sodium is an intermediate for the endogenous synthesis of phosphatidylcholine and an important component in the construction of biological membranes. After central nerve injury, citicoline sodium participates in repair and regeneration, and plays a neuroprotective role; it also plays an important role in the transfer of nerve media and the conduction of bioelectricity. Citicoline sodium is mainly used clinically for head trauma and brain surgery accompanied by disturbance of consciousness, cerebral infar...

Claims

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Application Information

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IPC IPC(8): C07H19/10C07H1/06A61K31/7068A61P25/00A61P25/28A61P25/16A61P27/06
Inventor 胡建荣
Owner HAINAN MEIDA PHARMA
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