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New medical salt of dexibuprofen

A technology for dexibuprofen and new drugs, which is applied in the direction of antipyretics, drug combinations, carboxylate preparation, etc., and can solve the problems of poor solubility and slow onset of dexibuprofen

Inactive Publication Date: 2013-03-27
FUKANGREN BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Dexibuprofen has poor solubility, so currently only oral solid preparations are used clinically, and the onset of action is slow

Method used

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  • New medical salt of dexibuprofen
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  • New medical salt of dexibuprofen

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Synthesis of Dexibuprofen Sodium (x=1,n=2)

[0017] Dissolve 20.6g of dexibuprofen in 41mL of tetrahydrofuran, stir at room temperature, slowly add 16.6mL of an aqueous solution of 16.6g of sodium isooctanoate dropwise, continue stirring for 6 hours after the dropwise addition, concentrate under reduced pressure and evaporate tetrahydrofuran to obtain a viscous liquid. Pour into 206mL of acetone, stir at room temperature for 1 hour, filter the precipitated solid, wash with acetone, and dry in vacuo to obtain 18.5 g of dexibuprofen sodium hydrate.

Embodiment 2

[0019] Synthesis of Dexibuprofen Arginine Salt (x=1,n=0)

[0020] 10.3g dexibuprofen was dissolved in 50mL ethanol, stirred at room temperature, 9.3g arginine was added in batches, continued to stir at room temperature for 4 hours, the white solid separated out was filtered, washed with ethanol, and vacuum-dried to obtain dexibuprofen arginine salt.

Embodiment 3

[0021] Embodiment 3 Dexibuprofen sodium tablet

[0022]

[0023] Process: Take 700ml of purified water, add the main drug and various auxiliary materials in turn, stir to dissolve completely, adjust the pH value to a suitable range with sodium citrate and citric acid, add purified water to the scale, stir to mix evenly, filter, Just pack it.

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Abstract

The invention discloses new medical salt of dexibuprofen. According to the salt, x can be 0, 0.5, 1, 1.5, 2, 2.5 and 3, n can be 1, 2, and 3, and M can be sodium, potassium, magnesium, zinc, arginine and lysine. The invention provides a preparation method of the salt, and also a medicine composite containing the salt. The composite contains a carrier which can be accepted by medicines; and the medicine composite can be produced in an appropriate and medical dosage form during the producing of medicaments.

Description

technical field [0001] The invention is a new medicinal salt of Dexibuprofen, which belongs to the technical field of medicine. Background technique [0002] Ibuprofen is an effective PG synthase inhibitor with antipyretic, analgesic and anti-inflammatory effects. For sprains, strains, low back pain, frozen shoulder, bursitis, tendon and tenosynovitis. Toothache and postoperative pain, rheumatoid arthritis, osteoarthritis, and other seronegative (nonrheumatoid) joint diseases. It is used to relieve moderate pain, such as joint pain, muscle pain, migraine, headache, toothache, dysmenorrhea, neuralgia, and can also be used to relieve fever caused by the common cold or influenza. For a long time, the sales of ibuprofen in my country's pharmaceutical market have been growing steadily. Together with paracetamol, aspirin and diclofenac, it has become the four pillar products in my country's antipyretic and analgesic drug market. [0003] Dexibuprofen is the active ingredient in...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C57/30C07C51/41C07C279/14C07C277/08A61K31/192A61P29/00
Inventor 不公告发明人
Owner FUKANGREN BIO PHARMA
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