Amino acid salt of (S)-ibuprofen and medicinal composition thereof

A technology of amino acid salt and composition, which is applied in the field of amino acid salt of ibuprofen and its pharmaceutical composition, which can solve the problem of poor water solubility of ibuprofen, poor oral bioavailability, and discomfort of patients. Sensation and other issues

Inactive Publication Date: 2008-09-17
FUKANGREN BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The water solubility of ibuprofen is not very good, so most of the ibuprofen currently used is its oral preparation, and the oral bioavailability is not very satisfactory. Can cause discomfort to patients

Method used

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  • Amino acid salt of (S)-ibuprofen and medicinal composition thereof
  • Amino acid salt of (S)-ibuprofen and medicinal composition thereof
  • Amino acid salt of (S)-ibuprofen and medicinal composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Embodiment 1L-lysine Dexibuprofen

[0013] Dissolve 25g of ibuprofen in 250ml of ethanol, add dropwise 35.4g of 50% (m / m) L-lysine aqueous solution-180ml of ethanol at room temperature, react at room temperature for 1h after dropping, keep at 0°C for 2h, filter, Washed with a small amount of ethanol and dried in vacuo to obtain 39.4 g of product with a yield of 92.3%. Elemental analysis (C19H32N2O4, %): Calculated: C 64.77, H 9.09, N 7.95; Found: C 64.86, H 9.01, N 7.76.

Embodiment 2

[0014] Example 2 L-Arginine Dexibuprofen

[0015] Dissolve 25g of ibuprofen in 250ml of ethanol, add 42.3g of 50% (m / m) L-arginine aqueous solution-200ml of ethanol dropwise at room temperature, react at room temperature for 1h after dropping, keep at 0°C for 2h, filter, Washed with a small amount of ethanol and dried in vacuo to obtain 41.8 g of product with a yield of 90.5%. Elemental analysis (C19H32N4O4, %): Calculated: C 60.00, H 8.42, N 14.74; Found: C 60.22, H 8.52, N 14.56.

Embodiment 3

[0016] The preparation of embodiment 3 L-lysine Dexibuprofen tablet

[0017] prescription:

[0018]

[0019] Preparation:

[0020] Pass L-Lysine Dexibuprofen and Microcrystalline Cellulose through 80 mesh sieve respectively, mix evenly, and set aside; another appropriate amount of 50% ethanol solution is taken as a soft material for binder, granulated with 24 mesh sieve, 50°C Dry, sieve into 20-mesh sieve, add micropowder silica gel and CMS-Na, mix evenly, and press a suitable die to form a tablet.

[0021] If the above-mentioned tablet is coated, a coated tablet can be obtained, which can be a film-coated tablet, an enteric-coated tablet, and the like.

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PUM

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Abstract

The invention provides a preparation and synthesis method of basic amino acid medicine salt of a dextral optical isomer in ibuprofen that is the existing anti-inflammation antipyretic and analgesic, and a medicinal combination thereof. After being mixed with necessary auxiliary material, the medicine salt can be prepared into oral solid preparations such as oral liquid, granules, tablets, dispersible tablets, capsules, coated tablets, sustained release tablets, collocystis, etc. through necessary pharmaceutics operations, and can also be prepared into the preparations for intravenous injection such as hydro-acupuncture, freeze-dried powders, aseptic powders, high volume transfusions, etc.

Description

technical field [0001] The invention relates to an amino acid salt of Dexibuprofen and a medicinal composition thereof, belonging to the technical fields of chemical industry and pharmacy. Background technique [0002] Ibuprofen is an anti-inflammatory, antipyretic and pain-relieving drug. It is one of the most commonly used NSAID drugs in clinical practice. It is widely used by doctors to treat rheumatism or rheumatoid diseases, as well as joint and muscle pain, headache, dysmenorrhea and other pains. . Ibuprofen is the product of long-term research in the 1950s and 1960s in the development of a "super aspirin" for rheumatoid arthritis. Ibuprofen was hailed as a "super aspirin", meaning that it was as effective as other drugs at the time, but safer. Ibuprofen is a nonselective cyclooxygenase (COX) inhibitor, and recent evidence suggests that its anti-inflammatory properties are achieved by modulating leukocyte activity, reducing cytokine production, inhibiting free radica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C57/30A61K31/192A61P29/00C07C279/14C07C229/26C07D233/64
Inventor 姚勇敢
Owner FUKANGREN BIO PHARMA
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