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Method for preparing ibuprofen arginine salt

A technology of arginine salt and arginine, which is applied in the field of drug synthesis, can solve the problems of many steps, large amount of solvent used, and high cost, and achieve the effect of mild conditions, shortened amount of solvent used, and low cost

Active Publication Date: 2012-08-01
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) Feeding 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 arginine solid, then add 11kg of 95% ethanol, heat and stir to 65℃, keep warm and stir for about 20min, stop heating after the solution is clear. Stir at room temperature until the solution is white and turbid, stop stirring at room temperature and let stand for 24 hours to crystallize, filter with suction, wash the filter cake twice with absolute ethanol, and place it at 60~70℃ for 8 hours and dry with air to obtain ibuprofen. Acid, as white crystalline powder, yield 6.80 kg, yield 92.39%, purity 99.7%.

Embodiment 2

[0039] (1) Feeding 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 arginine solid, then add 8.1kg of 95% ethanol, heat and stir to 65℃, keep warm and stir for about 60min, stop heating after the solution is clear When stirring at room temperature until the solution is white and turbid, stop stirring at room temperature and let stand for 24 hours to crystallize, filter with suction, wash the filter cake twice with absolute ethanol, and place it at 60~70℃ for air drying for 8 hours to obtain ibuprofen Arginine, white crystalline powder, yield 6.94kg, yield 94.12%, purity 99.6%

Embodiment 3

[0045] (1) Feeding 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 arginine solid, then add 11kg of 95% ethanol, heat and stir to 65℃, keep warm and stir for about 20min, stop heating after the solution is clear. Stir at room temperature until the solution is white and turbid, stop stirring at room temperature and let stand for 24 hours to crystallize, filter with suction, wash the filter cake twice with absolute ethanol, and place it at 60~70℃ for 8 hours and dry with air to obtain ibuprofen. Acid, white crystalline powder, yield 6.78kg, yield 92.11%. 99.7% purity

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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 by adopting a "one-step method". Background technique [0002] Ibuprofen (Ibuprofen, 1) is one of non-steroidal anti-inflammatory and analgesic drugs (NSAID). The drug inhibits cyclooxygenase and reduces the synthesis of prostaglandins, and produces analgesic and anti-inflammatory effects. It has an antipyretic effect through the hypothalamic body temperature regulation center. It is widely used because of its anti-inflammatory, antipyretic and analgesic effects, few adverse reactions, and easy absorption by oral administration, especially in the treatment or adjuvant treatment of various pediatric diseases. There are many ibuprofen dosage forms currently on the market at home and abroad, including ordinary tablets, sustained-release tablets, capsules, suspensions, suppositories, creams, gels, etc., which have a wide range of clinical appli...

Claims

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Application Information

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