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Dexrabeprazole sodium monohydrate crystal form and preparation method thereof

A technology of dex-rabeprazole sodium and rabeprazole sodium, which is applied in the field of dex-rabeprazole sodium monohydrate crystal form and its preparation, can solve the problems of poor stability and solubility, unsatisfactory dissolution rate, Problems such as strong hygroscopicity, to achieve good stability, good product quality, and low hygroscopicity

Active Publication Date: 2013-02-13
JIANGSU CHENGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Existing documents and patents all involve various crystal forms prepared by racemic rabeprazole sodium, and there is no literature report on the crystal form of dex-rabeprazole sodium, and amorphous dex-rabeprazole sodium has hygroscopic However, due to the disadvantages of strong solubility, poor stability and solubility, and unsatisfactory dissolution rate, there are certain technical difficulties in preparing stable dex-rabeprazole sodium crystal forms in the prior art. Therefore, from the perspective of industrial production, a stable dex-rabeprazole sodium The crystal form of rabeprazole sodium is very necessary

Method used

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  • Dexrabeprazole sodium monohydrate crystal form and preparation method thereof
  • Dexrabeprazole sodium monohydrate crystal form and preparation method thereof
  • Dexrabeprazole sodium monohydrate crystal form and preparation method thereof

Examples

Experimental program
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Embodiment 1

[0049] Synthesis of dex-rabeprazole sodium monohydrate crystals

[0050] Add 3.9g of sodium hydroxide into 80ml of ethanol, stir to dissolve it, add 35g of dex-rabeprazole and 3.5g of activated carbon into the solution, stir at room temperature for 1h, filter with suction, rinse the filter cake twice with 30ml of ethanol, The obtained filtrates were combined, and the solvent in the filtrate was evaporated with a rotary evaporator to obtain a white solid. The obtained solid was vacuum-dried at 40°C for 24 hours, added to 80ml of ethyl acetate, stirred to dissolve, added 240ml of methyl tert-butyl ether and a small amount of Seed crystals, stir at room temperature for 8 h, filter, and rinse the obtained white solid with 30 ml of methyl tert-butyl ether twice, and dry the obtained solid in vacuum at 45° C. for 24 h to obtain the crystalline form of dex-rabeprazole sodium monohydrate. The X-ray powder diffraction pattern of the solid obtained is as follows figure 1 , and the dif...

Embodiment 2

[0052] Synthesis of dex-rabeprazole sodium monohydrate crystals

[0053] Add 3.9g of sodium hydroxide into 80ml of ethanol, stir to dissolve it, add 35g of dex-rabeprazole and 3.5g of activated carbon into the solution, stir at room temperature for 1h, filter with suction, rinse the filter cake twice with 30ml of ethanol, The obtained filtrates were combined, and the solvent in the filtrate was evaporated with a rotary evaporator to obtain a white solid. The obtained solid was vacuum-dried at 40 ° C for 24 h, added to 80 ml of ethyl acetate, stirred to dissolve, and 240 ml of methyl tert-butyl ether was added. Stir for 16 h, filter, and rinse the obtained white solid twice with 30 ml of methyl tert-butyl ether. The obtained solid is vacuum-dried at 45° C. for 24 h to obtain the crystalline form of dex-rabeprazole sodium monohydrate. The resulting solid had the same physical properties as the product obtained in Example 1.

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Abstract

The invention provides a dexrabeprazole sodium monohydrate crystal form. The invention is characterized in that the dexrabeprazole sodium monohydrate crystal form has characteristic diffraction peaks at 10.5, 13.4, 17.1, 18.0, 18.5, 18.9, 19.5, 23.0, 23.3, 27.1 and 31.6 degrees in an X-ray powder diffraction spectrum represented by Cu-Kalpha radiation and 2theta; and an absorption peak exists at about 148.27 DEG C in a differential thermal analysis atlas of the dexrabeprazole sodium monohydrate crystal form. The crystal form has relatively high stability, solubility and dissolution, and relatively low hygroscopicity. The invention also provides a preparation method for the dexrabeprazole sodium monohydrate crystal form. The preparation method is simple, high in yield and low in preparation cost, and the quality of products is high.

Description

technical field [0001] The present invention relates to a crystal form of rabeprazole sodium, in particular to a crystal form of dex-rabeprazole sodium monohydrate and a preparation method thereof. Background technique [0002] Rabeprazole sodium is a new type of proton pump inhibitor, which can be used in the treatment of gastric acid-related diseases, such as peptic ulcer, gastroesophageal reflux disease, Zoller's syndrome and so on. Compared with omeprazole, rabeprazole sodium has a stronger inhibitory effect on H+ / K+-ATPase, and the inhibition can be restored; it has less effect on plasma gastrin levels; it has selective and strong inhibition of Helicobacter pylori (HP ) role. [0003] Rabeprazole sodium (Sodium rabeprazole) is the sodium salt of rabeprazole, chemical name: Na-2-[[[4-(3-methoxypropoxy)-3-methylpyridine]-2 -base] methylsulfinyl] -1H-benzimidazole, rabeprazole sodium includes two optical isomers, left-handed and right-handed, and studies have shown that ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12A61K31/4439A61P1/04
Inventor 刘凤伟李伟余秀峰张马丽朱敏泽马东亚施斌邢将军彭立军
Owner JIANGSU CHENGXIN PHARMA
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