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Preparation method of ibuprofen arginine salt

A technology of arginine salt and arginine, applied in the field of pharmaceutical synthesis, can solve the problems of high preparation cost, large amount of solvent and high toxicity, and achieve the effects of improving production safety, avoiding environmental pollution problems and reducing harm

Active Publication Date: 2012-08-01
HEFEI JINKE BIOPHARML TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In order to overcome a series of shortcomings such as many steps in the preparation method of the existing ibuprofen arginine salt, large amount of solvent, high toxicity and high preparation cost, the purpose of the present invention is to provide a preparation method of the ibuprofen arginine salt

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] (1) Feed amount

[0043] Reactant

Feeding amount

moles

ibuprofen

4kg

19.417mol

arginine

3.36kg

19.28mol

purified water

7.36kg

[0044] (2) Operation process

[0045] Mechanically stir, add 4kg of ibuprofen and 3.36kg of solid arginine to a 20L reaction bottle, then add 7.36kg of purified water, stir at room temperature (about 25°C) until clear and transparent, after about 2h, use a 0.22μm microporous filter membrane Filter and use the filtrate for later use.

Embodiment 2

[0047] (1) Feed amount

[0048] Reactant

Feeding amount

moles

ibuprofen

4kg

19.417mol

arginine

3.36kg

19.28mol

purified water

5.6kg

[0049] (2) Operation process

[0050] Stir mechanically, add 5.6kg of purified water to a 20L reaction bottle, then add 4kg of ibuprofen and 3.36kg of solid arginine, stir at room temperature until clear and transparent, after about 4 hours, filter with a 0.22μm microporous membrane, and use the filtrate for later use.

Embodiment 3

[0052] (1) Feed amount

[0053] Reactant

Feeding amount

moles

ibuprofen

4kg

19.417mol

arginine

3.36kg

19.28mol

[0054] purified water

25.8kg

[0055] (2) Operation process

[0056] Stir mechanically, add 3.36kg of solid arginine and 4kg of ibuprofen to a 50L reaction bottle, then add 25.8kg of purified water, stir at 40°C until clear and transparent, after about 3 hours, filter with a 0.22μm microporous membrane filter, and use the filtrate for later use .

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PUM

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Abstract

The invention relates to a preparation method of ibuprofen arginine salt. The method comprises the following steps of: reacting ibuprofen with arginine in water; and after reacting, drying a reaction liquid. In the preparation method provided by the invention, an arginine solid and an ibuprofen solid are directly added into a reaction kettle, and purified water is added for reacting, so that the use of an organic solvent is avoided, the problem of environmental pollution is solved, and the production cost is reduced. After the reaction, drying is performed directly, and the organic solvent is not contacted, so that the production cost is reduced, the problem of environmental pollution is avoided, the yield is increased, and the production safety is enhanced. The method has the advantages of mild reaction conditions, implementation at the room temperature, reduction in energy consumption, energy saving, reduction in cost and environmental friendliness.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a method for preparing ibuprofen arginine salt using water as a solvent in a "one-step method". 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. [000...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C57/30C07C51/41C07C279/14C07C277/08
Inventor 石静波耿燕王雯
Owner HEFEI JINKE BIOPHARML TECH
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