Method for preparing ibuprofen arginine

A technology of arginine ibuprofen and arginine, which is applied in the preparation of organic compounds, chemical instruments and methods, organic chemistry, etc., can solve the problems of solvents that are difficult to recycle, increase the difficulty of quality control, and consume energy. Achieve the effect of reducing synthesis process steps and reaction equipment, shortening production process and reducing production cost

Active Publication Date: 2008-06-04
安徽华辰制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Its disadvantages are: (1) two reaction tanks are required to dissolve ibuprofen and arginine respectively and because arginine is insoluble in 95% ethanol, it is not easy to make a uniform suspension, and strong stirring equipment is required, otherwise solid precipitation will occur phenomenon at the bottom of the tank, which greatly increases the requirements and costs of reaction equipment
(2) If arginine is dissolved with water-containing alcohol, it will be difficult to crystallize or incomplete crystallization at room temperature
(3) In the disclosed embodiment of CN1246306C, because of the use of hydrous ethanol to dissolve, it is difficult t

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  • Method for preparing ibuprofen arginine

Examples

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Effect test

Embodiment 1

[0020] Get 41g of ibuprofen, dissolve in 230mL of 95% ethanol, get 35g of L-arginine, add to the ibuprofen ethanol solution under stirring. Heat to 70°C, stir and react for 30 minutes, then cool to crystallize at room temperature, filter with suction, dry at 50°C, and weigh to obtain 68.8g of the product. mp165-167°C.

Embodiment 2

[0022] Get 41g of ibuprofen, dissolve in 340mL of 95% ethanol, get 27.7g of L-arginine, add to the ibuprofen ethanol solution under stirring. Heat to reflux, reflux and stir for 20 minutes, then cool to crystallize at room temperature, filter with suction, dry at 50°C, and weigh to obtain 52.4 g of the product. mp165-167°C.

Embodiment 3

[0024] Get 206g of ibuprofen, be dissolved in 760mL of 95% ethanol, get 174g of L-arginine, add in the ibuprofen ethanol solution under stirring. Heat to 50°C, stir and react for 50 minutes, then cool to crystallize at room temperature, filter with suction, dry at 50°C, and weigh to obtain 330 g of the product. mp165-167°C.

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Abstract

The invention discloses a preparation method of an arginine ibuprofen salt. The method is that ibuprofen is adopted to dissolve into ethanol with 95 percent concentration and added with solid arginine while stirring, and then heated to 40 to 80 DEG C, stirred for 15 to 60 minutes, after reaction, cooled to room temperature and crystallized. The preparation method of the invention adopts that the solid arginine is directly added to the ibuprofen solution and no solvent is added before the solid arginine addition, thus shortening production technique steps and reducing reaction equipment. The process that directly crystallization from mother liquid in room temperature, need not be added with other solvent to dilute, thus reducing consumption of solvent and kinds, shortening production technique flow; as the solvent can be recycled and reused, thus reducing production cost and saving energy.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical synthesis chemistry, and relates to a preparation method for increasing water-soluble derivatives of an antipyretic and analgesic drug ibuprofen, more specifically a new preparation method for an antipyretic and analgesic drug arginine ibuprofen salt. Background technique [0002] Ibuprofen is a commonly used non-steroidal anti-inflammatory and analgesic drug in clinical practice. Its analgesic effect is significant, and its tolerance is stronger than that of aspirin. It has become the mainstay product of antipyretic and analgesic drugs in many countries. But because of its low water solubility, the development and application of its quick-acting water-soluble preparations have been limited. Therefore, a large amount of alcohol or a reducing substance that is several times that of ibuprofen are all added to the syrup formulations reported in the existing literature. to increase its water ...

Claims

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Application Information

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IPC IPC(8): C07C279/14C07C57/30C07C277/00
Inventor 王润玲
Owner 安徽华辰制药有限公司
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