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Esomeprazole sodium compound and preparation method thereof

A technology of esomeprazole sodium and compound, applied in the field of medicine, can solve the problems of low purity of esomeprazole sodium and the like

Inactive Publication Date: 2012-01-25
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In order to overcome the low-purity defect of esomeprazole sodium prepared by the prior art, the invention provides esomeprazole sodium and a method for refining and purifying it

Method used

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  • Esomeprazole sodium compound and preparation method thereof
  • Esomeprazole sodium compound and preparation method thereof
  • Esomeprazole sodium compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Get 10g crude esomeprazole sodium to be purified, the content of esomeprazole sodium recorded by high performance liquid chromatography is 92%. This esomeprazole sodium crude product is dissolved in 100ml water, fully stirs, and esomeprazole sodium is dissolved, crosses D1300 type macroporous adsorption resin, is the 1M sodium hydroxide solution elution purification of 12.5 with pH, ​​collects containing esomeprazole sodium eluate.

[0053] Add 50 ml of 15% ammonia water to the above-mentioned aqueous eluting solution for treatment, the treatment time is 2 hours, stir during the treatment, and filter out the precipitated precipitate.

[0054] The obtained aqueous solution of esomeprazole sodium was raised to 60-70° C. to remove residual ammonia in the solution while concentrating to obtain a solution with a volume of 120 ml. Then add 75% ethanol to the aqueous solution, whose volume accounts for 65% of the aqueous solution volume, and slowly cool down to 12°C. Optiona...

Embodiment 2

[0057] Get 10g esomeprazole sodium crude product, the content of esomeprazole sodium recorded by high performance liquid chromatography is 93%. Dissolve the crude product of esomeprazole sodium in 120ml of water and stir fully, then dissolve the esomeprazole sodium, pass through BS-55 type macroporous adsorption resin, use pH 11.5 for elution and purification of 2M sodium carbonate solution, collect Eluate containing esomeprazole sodium.

[0058] Continuously feed ammonia gas into the above-mentioned aqueous eluting solution for treatment, the treatment time is 2.5 hours, stirring is carried out during the treatment, and the precipitated precipitate is filtered off.

[0059] Raise the obtained aqueous solution of esomeprazole sodium to 55-65°C, remove the remaining ammonia in the solution, and concentrate at the same time to obtain a solution volume of 90ml, then add absolute ethanol to the aqueous solution, the volume of which accounts for 1% of the aqueous solution The volu...

Embodiment 3

[0062] Get 10g of esomeprazole sodium crude drug (AstraZeneca AB, batch number: 20080503) with a longer production date, and the content of esomeprazole sodium recorded by high performance liquid chromatography is 91%. This esomeprazole sodium crude product is dissolved in 150ml water, after fully stirring, esomeprazole sodium is dissolved, cross BS-55 type macroporous adsorption resin, be 10 sodium bicarbonate solution elution purification with pH, The eluate containing esomeprazole sodium was collected.

[0063] Continuously feed ammonia gas into the above-mentioned aqueous eluting solution for treatment, the treatment time is 3 hours, stirring is carried out during the treatment, and the precipitated precipitate is filtered off.

[0064] The obtained esomeprazole sodium aqueous solution is raised to 70-80° C., removes the remaining ammonia in the solution, and concentrates at the same time to obtain a solution volume of 150 ml. Then, 90% ethanol is added to the aqueous solu...

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Abstract

The invention relates to a purified esomeprazole sodium compound and a preparation method thereof. The preparation method comprises the following steps: 1) dissolving the crude products of esomeprazole sodium in water, stirring the materials fully to dissolve esomeprazole sodium, ensuring the solution to pass through a macroporous adsorption resin, using mobile phase for elution and purification and collecting the eluent; 2) pumping ammonia into or adding ammonia water to the eluent to process the eluent for several minutes to 8 hours, carrying out stirring in the processing course, filteringout the separated precipitate to obtain filtrate which is aqueous solution containing esomeprazole sodium and optionally heating the aqueous solution to remove the residual ammonia; 3) adding alcoholsolvents to the aqueous solution, controlling the temperature for recrystallization, centrifuging and washing the separated crystals and drying the crystals to obtain the fine products of esomeprazole sodium; and 4) optionally returning the crystallization mother solution to the step 3), namely adding the crystallization mother solution to the aqueous solution obtained in the step 2) together with the alcohol solvents. By adopting the method, the purity of the crude products of esomeprazole sodium can be substantially improved, the quality of the preparation product can be improved and the toxic and side effects can be reduced.

Description

technical field [0001] The invention relates to an esomeprazole sodium compound and a method for purifying it, belonging to the technical field of medicine. Background technique [0002] Esomeprazole sodium (Esomeprazole sodium) is the world's first single isomer proton pump inhibitor developed by AstraZeneca, and its chemical name is: 5-methoxy-2-((S)-((4- Methoxy-3,5-dimethyl-2-pyridyl)methyl)sulfinyl-1H-benzimidazole sodium, molecular formula: C 17 h 19 N 3 o 3 S Na, molecular weight: 369.41, Cas number: 161796-78-7, structural formula: [0003] [0004] Hydrochloric acid is a major component of gastrointestinal secretions and is necessary for the digestion of food. However, excessive hydrochloric acid secretion will damage the gastric mucosa and submucosa, leading to gastrointestinal ulcers, especially gastric ulcers and duodenal ulcers, so adjusting the balance between hydrochloric acid and acid neutralizing mucus is important for the stomach System is very imp...

Claims

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Application Information

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IPC IPC(8): C07D401/12
Inventor 陶灵刚
Owner HAINAN LINGKANG PHARMA CO LTD
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