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Preparation method of ibuprofen arginine salt

A kind of technology of arginine salt and arginine, which is applied in the field of preparation of ibuprofen arginine salt, can solve the problems that ibuprofen arginine salt cannot be reproduced, so as to improve melting point, save washing operation, The effect of simplifying the process

Inactive Publication Date: 2010-09-01
SHANDONG XINHUA PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Chinese Journal of Pharmaceutical Industry 2002: 33 (2): 58, the patent of application number 200410014369.4 and the preparation process of ibuprofen arginine salt in journal literature have not completely solved the above problems and cannot be reproduced

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Weigh 17.4g of arginine, add 152ml of absolute ethanol, raise the temperature to above 70°C and stir for 2 hours, add 20.6g of ibuprofen, and the reaction solution becomes transparent instantly. Continue to stir for 20 minutes and the reaction solution becomes cloudy, then keep warm and stir for 1 hour to crystallize, let stand overnight at room temperature, then suction filter and dry to obtain 36.9 g of ibuprofen arginine with a melting point of 167° C. and a yield of 97.11%.

Embodiment 2

[0021] Weigh 17.4g of arginine, add 152ml of absolute ethanol, heat up to 60°C and stir for 0.5h, add 20.6g of ibuprofen, and the reaction solution becomes transparent instantly. Continue to stir for about 30 minutes, and the reaction solution becomes cloudy, then keep warm and stir to crystallize for 0.5 hours, let it stand at room temperature for 8 hours, then suction filter and dry to obtain 36.7g of ibuprofen arginine with a melting point of 166°C and a yield of 96.58%.

Embodiment 3

[0023] Weigh 17.4g of arginine, add 152ml of 95% (ml / ml) ethanol, heat up to 80°C and stir for 4h, add 20.6g of ibuprofen, and the reaction solution becomes transparent instantly. Continue to stir for about 10 minutes, and the reaction solution becomes cloudy, then keep warm and stir to crystallize for 4 hours, let stand at room temperature for 24 hours, then filter with suction, and dry to obtain 36.8g of ibuprofen arginine with a melting point of 167°C and a yield of 96.84%.

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Abstract

The invention relates to a preparation method of ibuprofen arginine salt, belonging to the technical field of pharmaceutical chemistry. The preparation method of the ibuprofen arginine salt comprises the following steps of: firstly adding arginine and ethanol for heating and stirring; and then adding ibuprofen to obtain the ibuprofen arginine salt through crystallization, temperature reduction, standing, filtering and drying. The invention can well solve the dissolution problem in the reaction process and the crystallization problem after reaction, and has the advantages of simple process, easy implementation, reliable quality and high yield.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry and relates to a preparation method of ibuprofen arginine salt. Background technique [0002] Ibuprofen is a phenylpropionic acid non-steroidal anti-inflammatory analgesic, which has strong antipyretic, analgesic, anti-inflammatory and anti-rheumatic effects. It has exact curative effect, small adverse reactions, light gastrointestinal side effects and high safety , widely used clinically. [0003] Ibuprofen is almost insoluble in water and is suitable for the preparation of solid preparations. After ibuprofen and arginine are salted, the water solubility is greatly enhanced, and can be used to prepare liquid preparations, which is beneficial to speed up absorption, improve bioavailability, and expand the scope of medication. [0004] Ibuprofen is easily soluble in common organic solvents but insoluble in water; arginine and its product ibuprofen arginine salt are easily soluble in water but i...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C279/14C07C277/08C07C57/30C07C51/41
Inventor 翟吉胜王云峰
Owner SHANDONG XINHUA PHARMA CO LTD
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