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Method for preparing rabeprazole sodium by virtue of supercritical anti-solvent technique

A technology of rabeprazole sodium and solution, which is applied in the field of drug synthesis, can solve the problems of easy degradation of rabeprazole sodium, unstable crystallization process, incomplete crystallization, etc., so as to save drug cost, product yield and The effect of high purity and no solvent residue

Inactive Publication Date: 2017-07-18
SHANDONG YUXIN PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because rabeprazole sodium solution viscosity is big, and rabeprazole sodium is easily degraded, so cause the crystallization process of rabeprazole sodium unstable, be easy to various problems, as separating out oily matter, not crystallizing, or Incomplete crystallization, precipitated crystals redissolved, etc.

Method used

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  • Method for preparing rabeprazole sodium by virtue of supercritical anti-solvent technique
  • Method for preparing rabeprazole sodium by virtue of supercritical anti-solvent technique
  • Method for preparing rabeprazole sodium by virtue of supercritical anti-solvent technique

Examples

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Effect test

Embodiment 1

[0027] The preparation of embodiment 1 rabeprazole sodium

[0028] Add 100 g of rabeprazole to the reaction vessel, add 40 L of methanol and stir to dissolve, to prepare solution A. Add 111.29g of 10% sodium hydroxide solution, stir for 30 minutes, add 10g of activated carbon to decolorize for 30 minutes, filter, and the filtrate is for later use;

[0029] The temperature of the high-pressure sedimentation kettle is set to 40 ° C, the pressure is 80 bar, the steel cylinder is opened, and the carbon dioxide is introduced from the top of the sedimentation kettle at a flow rate of 15 g / min with a high-pressure pump. When the temperature and pressure in the reaction kettle reach the above-mentioned set values, Use another high pressure pump to pass methanol through the sedimentation kettle at a rate of 0.25ml / min. After 15 minutes, the system in the reaction kettle reaches an equilibrium state, stop feeding methanol, and feed the rabeprazole sodium solution prepared above at the s...

Embodiment 2

[0030] The preparation of embodiment 2 rabeprazole sodium

[0031] Add 100 g of rabeprazole into the reaction vessel, add 4 L of ethanol and stir to dissolve, and make solution A. Add 55.65 g of 10% sodium hydroxide solution, stir for 30 minutes, add 10 g of activated carbon for decolorization for 30 minutes, filter, and set aside the filtrate;

[0032] Set the temperature of the high-pressure settling tank to 35°C and the pressure to 90 bar, open the steel cylinder, and use a high-pressure pump to feed carbon dioxide from the top of the settling tank at a flow rate of 25g / min. When the temperature and pressure in the reactor reach the above-mentioned set value, Use another high-pressure pump to pass ethanol through the settling tank at a rate of 1.0ml / min. After 15 minutes, the system in the reactor reaches an equilibrium state, stop feeding ethanol, and feed the rabeprazole sodium solution prepared above at the same rate , after completion, continue to feed carbon dioxide for...

Embodiment 3

[0033] The preparation of embodiment 3 rabeprazole sodium

[0034] Add 100 g of rabeprazole into the reaction vessel, add 2 L of acetone and stir to dissolve, and make solution A. Add 37.10 g of 30% sodium hydroxide solution, stir for 30 minutes, add 10 g of activated carbon for decolorization for 30 minutes, filter, and set aside the filtrate;

[0035] Set the temperature of the high-pressure settling tank to 37°C and the pressure to 120 bar, open the steel cylinder, and use a high-pressure pump to feed carbon dioxide from the top of the settling tank at a flow rate of 20g / min. When the temperature and pressure in the reactor reach the above-mentioned set value, Use another high-pressure pump to pass acetone through the settling tank at a rate of 2.0ml / min. After 15 minutes, the system in the reactor reaches an equilibrium state, stop feeding acetone, and feed the rabeprazole sodium solution prepared above at the same rate. , after completion, continue to feed carbon dioxide...

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Abstract

The invention discloses a method for preparing rabeprazole sodium by virtue of a supercritical anti-solvent technique. The final product rabeprazole sodium is prepared by virtue of the method. The method has the beneficial effects that a preparation manner is different from a traditional preparation process, rabeprazole sodium is prepared by virtue of the novel supercritical anti-solvent technique, the process is simple, conditions are mild, the reproducibility is good, the obtained product is relatively small in crystal form particle size, relatively narrow in size distribution and relatively high in solubility, the traditional solvent-out crystallization crystallization defects (disadvantages of difficulty in crystallization, easiness in formation of oily substances and the like) are avoided, the prepared product is high in purity and has no solvent residue, and any pollution is avoided.

Description

technical field [0001] The invention belongs to the technical field of drug synthesis, in particular to a method for preparing rabeprazole sodium by supercritical anti-solvent technology. Background technique [0002] Rabeprazole sodium, whose chemical name is 2-{4-(3-methoxypropoxy)-3-methylpyridin-2-ylmethanesulfinyl}-1H-benzimidazole sodium, is an inhibitor of Secreted drug, an alternative to benzimidazole, no anticholinergic and anti-H 2 Histamine properties, but can attach to the surface of gastric parietal cells by inhibiting H + / K + -ATPase to inhibit gastric acid secretion. This enzyme system is regarded as an acid proton pump, so rabeprazole sodium acts as a proton pump inhibitor in the stomach to block the production of gastric acid, and this effect is dose-related. Animal experiments have confirmed that rabeprazole sodium can be excreted from the plasma and gastric mucosa shortly after administration. [0003] Rabeprazole sodium is a novel proton pump inhibi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/12
CPCC07B2200/13C07D401/12Y02P20/54
Inventor 李晓峰谢娜王金星
Owner SHANDONG YUXIN PHARMA CO LTD
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