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High-purity sodium rabeprazole compound

A technology of rabeprazole sodium and rabeprazole, which is applied in the field of medicine, can solve the problems of rabeprazole sodium purification cost, low yield and purity, difficulty in purification, low purity, etc., and achieve the improvement of clinical drug effect and simple method , high yield and high purity

Inactive Publication Date: 2010-05-12
HAINAN MEILAN SMITH KLINE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0013] Therefore, compared with the prior art, the present invention solves the difficult problem brought by the dehydration and crystallization of rabeprazole sodium in the purification process, overcomes the shortcomings of low purity and difficult purification of rabeprazole sodium prepared in the prior art, The purification cost of rabeprazole sodium used in the present invention is low and the yield and purity are extremely high, and rabeprazole sodium refined product with a purity of more than 99.8% can be obtained, and the yield exceeds 90%.

Method used

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Examples

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Embodiment 1

[0038] The refining of embodiment 1 rabeprazole sodium

[0039] (1) 100g rabeprazole and 12.5g sodium hydroxide were stirred and reacted in water for 2 hours, spray-dried to generate 104.3g rabeprazole sodium;

[0040](2) Dissolve 100 g of rabeprazole sodium crude product in 2000 ml of water, add 20% sodium dihydrogen phosphate solution to adjust the pH value to 5.5, stir to precipitate insoluble matter, filter, and wash with 200 ml of purified water to obtain a solid;

[0041] (3) Dissolving the solid obtained in step (2) with a mixture of 1500ml dichloromethane and ethanol (1: 4), adsorbed by D101 macroporous adsorption resin, and eluted and purified with a mixture of 500ml chloroform and acetone (3: 2), Collect the eluate;

[0042] (4) The eluent obtained in step (3) is adjusted to a pH value of 9.0 with 5% sodium bicarbonate solution, and a solid is precipitated, centrifuged for 10 min, washed with 200 ml of ethanol, and vacuum-dried at 40° C. for 8 hours to obtain rabep...

Embodiment 2

[0043] The refining of embodiment 2 rabeprazole sodium

[0044] (1) 100g rabeprazole and 12.8g sodium hydroxide were stirred and reacted in water for 2 hours, freeze-dried to generate 103.8g rabeprazole sodium;

[0045] (2) Dissolve 100 g of rabeprazole sodium crude product in 2000 ml of water, add 5% sodium bisulfate solution to adjust the pH to 7.5, stir to precipitate insoluble matter, filter, and wash with 200 ml of purified water to obtain a solid;

[0046] (3) Dissolve the solid obtained in step (2) with a mixture of 1500ml of dichloromethane and ethanol (1:4), absorb through AB-8 macroporous resin, and elute and purify with a mixture of 500ml of chloroform and acetone (3:2) , to collect the eluate;

[0047] (4) The eluate obtained in step (3) is adjusted to a pH value of 11.0 with 10% potassium bicarbonate solution, and a solid is precipitated, centrifuged for 10 min, washed with 200 ml of ethanol, and vacuum-dried at 50° C. for 5 hours to obtain rabeprazole The pur...

Embodiment 3

[0048] The refining of embodiment 3 rabeprazole sodium

[0049] (1) 100g rabeprazole and 13.2g sodium hydroxide were stirred and reacted in water for 2 hours, spray-dried to generate 105.1g rabeprazole sodium;

[0050] (2) Dissolve 100g of rabeprazole sodium crude product in 2000ml of water, add 5% potassium hydrogen tartrate solution to adjust the pH to 6.8, stir to precipitate insoluble matter, filter, and wash with 200ml of purified water to obtain a solid;

[0051] (3) Dissolve the solid obtained in step (2) with a mixture of 1500ml of dichloromethane and ethanol (1:4), absorb through AB-8 macroporous resin, and elute and purify with a mixture of 500ml of chloroform and acetone (3:2) , to collect the eluate;

[0052] (4) The eluent obtained in step (3) is adjusted to a pH value of 10.0 with 5% potassium carbonate solution, and a solid is precipitated, centrifuged for 10 min, washed with 200 ml of ethanol, and vacuum-dried at 45° C. for 6 hours to obtain rabeprazole sodi...

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Abstract

The invention relates to a high-purity sodium rabeprazole compound, belonging to the technical field of medicine. The method includes the following steps: dissolving crude sodium rabeprazole synthesized by the reaction of rabeprazole and sodium hydroxide in water, adjusting pH value to be faintly acid to neutral by using solid acid salt, and collecting precipitated solid; after dissolving the solid with organic solvent, conducting elution and purification by using eluting agent through macroporous adsorption resin, and collecting eluent; and adjusting the pH value of the eluent to be alkaline, and collecting the precipitated solid to obtain the pure sodium rabeprazole.

Description

technical field [0001] The invention relates to a high-purity rabeprazole sodium compound, which belongs to the technical field of medicine. Background technique [0002] Rabeprazole sodium, its chemical name is: 2-{[4-(3-methoxypropoxy)-3-methylpyridin-2-yl]methylsulfinyl}-1H-benzimidazole sodium , molecular formula: C 18 h 20 N 3 NaO 3 S, molecular weight: 381.43, structural formula: [0003] [0004] Rabeprazole sodium, a benzimidazole compound, is a second-generation proton pump inhibitor that specifically inhibits gastric parietal cell H + 、K + -ATPase system to block the final step of gastric acid secretion. The effect is dose-dependent, and can inhibit both basal and stimulated gastric acid secretion. This product is against choline and histamine H 2 No receptor antagonistic effect. [0005] The salification of rabeprazole sodium, the patent literature reports all adopt the aqueous solution reaction of rabeprazole and sodium hydroxide, because contain wat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
Inventor 陶灵刚
Owner HAINAN MEILAN SMITH KLINE PHARMA
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