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Dextral ibuprofen arginine and preparation method thereof

An arginine salt, optical rotation technology, used in the research of analgesic drugs and their pharmacological activities, anti-inflammatory, antipyretic fields, can solve the problems of difficult to make stable, low water solubility, etc., to reduce irritation. Effect

Inactive Publication Date: 2011-09-14
吴家安 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] Aiming at the defects of low water solubility of dexibuprofen in the prior art and difficulty in making stable water-soluble preparations, the present invention provides a kind of dexibuprofen arginine salt

Method used

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  • Dextral ibuprofen arginine and preparation method thereof
  • Dextral ibuprofen arginine and preparation method thereof
  • Dextral ibuprofen arginine and preparation method thereof

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Embodiment Construction

[0016] The present invention will be further described according to specific embodiments below, but it does not mean to limit the protection scope of the present invention.

[0017] One, the synthesis and physicochemical property analysis of medicine of the present invention

[0018] Take 10g of arginine, add 20ml of water, heat to dissolve and transfer to the dropping funnel. Another 11.84g of ibuprofen was taken and dissolved in 50ml of 95% ethanol. The arginine solution was slowly added dropwise under stirring, and the addition was completed in about 30 minutes, and the solvent was evaporated after continuing to stir for 4 hours to obtain a fine product, which was recrystallized with 95% ethanol (1:3), and the yield was 90.7%.

[0019] This product is white powder, easily soluble in water. The pH of 20% aqueous solution is 6.5, the melting point is 170-172°C, and the optical rotation is right-handed. Ultraviolet spectrum and infrared spectrum analysis are under the same ...

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Abstract

The invention belongs to the technical field of pharmacy and in particular provides dextral ibuprofen arginine. The molecular formula of the dextral ibuprofen arginine is C19H32N4O4; the molecular weight is 380.48178[g / mol]; the structural formula is shown as (I); the dextral ibuprofen arginine is white powder and well soluble in water; the pH value of 20 percent aqueous solution is 6.5; the melting point is 170 to 172 DEG C; and the optical rotation is dextral. The dextral ibuprofen arginine has the characteristic of high solubility in water and can be prepared into various water-soluble preparations according to clinical requirements; the formula does not comprise cosolvents such as alcohol and the like; and the aqueous solution is neutral. The dextral ibuprofen arginine is absorbed by a human body easily, can relieve irritation on a gastrointestinal tract, and has antifebrile, antalgic and anti-inflammatory effects.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and specifically relates to antipyretic, anti-inflammatory and analgesic drugs and research on their pharmacological activities. Background technique [0002] Dexibuprofen is derived from ibuprofen, a non-steroidal antipyretic, anti-inflammatory, and analgesic drug. It is almost insoluble in water and has a low melting point. Therefore, when it is made into a preparation, its dosage form is limited, and the preparation process is difficult. Therefore, this paper reports the process of synthesizing Dexibuprofen into water-soluble Dexibuprofen arginine salt and studies the pharmacological effects. The results obtained are as follows: [0003] Experimental materials and instruments: [0004] Dexibuprofen batch number: 1009015M, Hubei Baike Hendy Pharmaceutical Co., Ltd.; L-arginine, batch number: 09121229, Shanghai Xiehe Amino Acid Co., Ltd.; 95% ethanol, batch number 20091212 Manufacturer: Tianj...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C57/30C07C51/41C07C279/14C07C277/08A61K31/198A61K31/192A61P29/00
Inventor 吴家安潘善庆
Owner 吴家安
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