Salifying preparation process of ibuprofen arginine

A preparation process, the technology of arginine, which is applied in the field of arginine ibuprofen salt preparation process, can solve the problems of unfavorable patient safety, difficulty in starting the reaction, long reaction time, etc., and achieve the benefits of patient safety and prevention of explosion-proof problems , the effect of short drying time

Inactive Publication Date: 2020-03-27
北京鑫开元医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the salt-forming process of preparing ibuprofen and arginine generally uses organic solvents for reaction, which not only has the problem of inflammability and explosion, but also is not conducive to patient safety; while adding ibuprofen and arginine first, and then The method of adding water has slow heat transfer, long reaction time, and sometimes it is difficult to start the reaction; the temperature of the sample in the salt-forming reaction can reach 110-120°C, and the temperature is relatively high. If the transfer process is added, it is necessary to consider transferring the sample after cooling down, which takes a long time. Direct transfers need to consider personnel safety issues

Method used

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  • Salifying preparation process of ibuprofen arginine
  • Salifying preparation process of ibuprofen arginine

Examples

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Effect test

Embodiment 1

[0018] A preparation process for arginine ibuprofen salting: comprising the following steps: first heating water to 90°C, adding ibuprofen and heating for 30 minutes until melting, adding arginine at a stirring rate of 25 rpm, stopping heating, Stir for 10 minutes, then use residual temperature to carry out vacuum drying for 20 minutes to get final product, the vacuum degree is -0.10MPa, the weight ratio of the ibuprofen and arginine is 1:1, and the water consumption is the total weight of the ibuprofen and arginine 5%.

Embodiment 2

[0020] A preparation process for ibuprofen arginine salt: including the following steps: first heating water to above 120°C, adding ibuprofen and heating for 90 minutes until melting, adding arginine at a stirring rate of 100rpm, and stopping heating , stirred for 20min, and then vacuum-dried for 60min using residual temperature to get final product. The vacuum degree is -0.05MPa. The weight ratio of ibuprofen and arginine is 1:1.2, and the water consumption is ibuprofen and arginine total weight 15%.

Embodiment 3

[0022] A preparation process for ibuprofen arginine salt: including the following steps: first heating water to above 100°C, adding ibuprofen and heating for 60 minutes until melting, adding arginine at a stirring rate of 60rpm, and stopping heating , stirred for 15min, and then vacuum-dried for 40min using residual temperature to get final product, the vacuum degree is -0.08MPa, the weight ratio of said ibuprofen and arginine is 1:1.1, and the water consumption is the total amount of ibuprofen and arginine. 10% by weight.

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Abstract

The invention provides a salifying preparation process of ibuprofen arginine. A mode of firstly adding water is adopted, high temperature heating is performed to adjust the feeding sequence and the interval time of adding the ibuprofen and the arginine, the specific heating temperature and heating time are set, and vacuum drying is performed after mixing and stirring. The problems encountered by material transfer can be reduced while it is guaranteed that qualified and uniform samples are obtained; meanwhile, residual temperature vacuum drying is performed in situ, the drying time is shorter and the safety is also guaranteed.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to a preparation process for arginine ibuprofen salt formation. Background technique [0002] Ibuprofen (Ibuprofen, 1) is one of the non-steroidal anti-inflammatory drugs (NSAID). The drug inhibits cyclooxygenase and reduces the synthesis of prostaglandins to produce analgesic and anti-inflammatory effects, and has an antipyretic effect through the hypothalamic thermoregulatory center. It is widely used for its anti-inflammatory, antipyretic and analgesic effects, less adverse reactions, and easy absorption after oral administration, especially in the treatment or adjuvant treatment of various pediatric diseases. At present, there are many dosage forms of ibuprofen on the market at home and abroad, including ordinary tablets, sustained-release tablets, capsules, suspensions, suppositories, creams, gels, etc., which are widely used clinically. [0003] Ibuprofen arginine salt, al...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C279/14C07C277/08C07C57/30C07C51/41
CPCC07C51/412C07C277/08C07C279/14C07C57/30
Inventor 夏中宁曹俊张丽杰
Owner 北京鑫开元医药科技有限公司
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