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Method for preparing ibuprofen arginine salt

An arginine salt and arginine technology, applied in the field of pharmaceutical synthesis, can solve the problems of many steps, large solvent consumption, high cost and the like, and achieve the effects of mild conditions, shortened solvent consumption and low cost

Active Publication Date: 2014-11-19
HEFEI KEDA BIO TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] 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 used, and high cost, the purpose of the present invention is to provide a kind of preparation method of the ibuprofen arginine salt

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] (1) Feed amount

[0033] Reactant

Feeding amount

moles

[0034] ibuprofen

4kg

19.417mol

arginine

3.36kg

19.28mol

95% ethanol

13.5L (11.0kg)

[0035] Reactant: ethanol (weight ratio) = 1: 1.5

[0036] (2) Operation process

[0037]Mechanical stirring, reflux condenser, 20L reaction flask, add 4kg of ibuprofen and 3.36kg of solid arginine, then add 11kg of 95% ethanol, heat and stir to 65°C, keep stirring for about 20min, stop heating after the solution is clarified, Stir at room temperature until the solution is white and turbid, stop stirring and stand at room temperature for crystallization for 24 hours, filter with suction, wash the filter cake twice with absolute ethanol, and place it at 60-70°C for 8 hours to obtain ibuprofen essence Acid, in the form of white crystalline powder, with a yield of 6.80kg, a yield of 92.39%, and a purity of 99.7%.

Embodiment 2

[0039] (1) Feed amount

[0040] Reactant

Feeding amount

moles

ibuprofen

4kg

19.417mol

arginine

3.36kg

19.28mol

95% ethanol

10L (8.1kg)

[0041] Reactant: ethanol (weight ratio) = 1: 1.1

[0042] (2) Operation process

[0043] Mechanical stirring, reflux condenser, 20L reaction flask, add 4kg of ibuprofen and 3.36kg of solid arginine, then add 8.1kg of 95% ethanol, heat and stir to 65°C, keep stirring for about 60min, stop heating after the solution is clarified , stir at room temperature until the solution is white and turbid, stop stirring at room temperature and stand for crystallization for 24 hours, filter with suction, wash the filter cake twice with absolute ethanol, and place it at 60-70°C for 8 hours to obtain ibuprofen Arginine, white crystalline powder, output 6.94kg, yield 94.12%, purity 99.6%

Embodiment 3

[0045] (1) Feed amount

[0046] Reactant

Feeding amount

moles

ibuprofen

4kg

19.417mol

arginine

3.36kg

19.28mol

95% ethanol

13.6L (11kg)

[0047] Reactant: ethanol (weight ratio) = 1: 1.49

[0048] (2) Operation process

[0049] Mechanical stirring, reflux condenser, 20L reaction flask, add 4kg of ibuprofen and 3.36kg of solid arginine, then add 11kg of 95% ethanol, heat and stir to 65°C, keep stirring for about 20min, stop heating after the solution is clarified, Stir at room temperature until the solution is white and turbid, stop stirring and stand at room temperature for crystallization for 24 hours, filter with suction, wash the filter cake twice with absolute ethanol, and place it at 60-70°C for 8 hours to obtain ibuprofen essence Acid, in the form of white crystalline powder, with a yield of 6.78kg and a yield of 92.11%. 99.7% purity

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PUM

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Abstract

The invention relates to a method for preparing ibuprofen arginine salt, which includes: reacting ibuprofen and arginine in C1-C4 fatty alcohol, cooling until crystals are precipitated after the reaction is completed, and collecting and drying the crystals to obtain the ibuprofen arginine salt. The solid raw material and the liquid raw material are directly reacted by a one-step method, complex steps and process of dissolving and charging respectively are avoided, a synthesis process step and reaction equipment are omitted, solvent usage is greatly reduced, and conditions are mild by using a cooling crystallization method. In a word, the method for preparing ibuprofen arginine salt has the advantages of short operating steps, simple process, easiness in implementation, low cost, reliability in quality, high yield and the like, and is more applicable to massive industrial production.

Description

technical field [0001] The invention relates to the field of drug synthesis, in particular to a method for preparing ibuprofen arginine salt using 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. [0003] Because ibuprofen i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C57/30C07C51/41C07C279/14C07C277/08
Inventor 程千流王宗贵王刚
Owner HEFEI KEDA BIO TECH CO LTD