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Preparation method of dexibuprofen amino acid salt and application

A technology of amino acid salt and Dexibuprofen, which is applied in the field of preparation of Dexibuprofen amino acid salt, can solve the problems that patients cannot receive treatment, increase gastrointestinal bleeding, kidney damage, etc. Increase and reduce the stimulating effect

Inactive Publication Date: 2007-03-07
陈亦林
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

When taking Dexibuprofen orally to treat chronic diseases (rheumatism and rheumatoid arthritis, etc.), long-term frequent and high-dose medication will increase gastrointestinal bleeding and cause certain damage to the kidneys, resulting in reduced efficacy in the body, and some patients cannot accept it. treat

Method used

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  • Preparation method of dexibuprofen amino acid salt and application
  • Preparation method of dexibuprofen amino acid salt and application
  • Preparation method of dexibuprofen amino acid salt and application

Examples

Experimental program
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Effect test

Embodiment 1

[0022] Compounds of the present invention are:

[0023]

[0024] Chemical name: +2-(4-isobutylphenyl) propionate arginine salt.

[0025] The preparation method is as follows: 100 g of dexibuprofen is placed in a reaction bottle. Add 300ml of ethanol, stir to dissolve, control the temperature between 40-78°C, gradually add 80g of essence, stir to dissolve, keep warm for 30 minutes, after cooling down to room temperature, slowly pour the reaction solution into the prepared acetone solution , a white precipitate precipitated out, stirred for another 10 minutes, put it in the refrigerator for 12 hours, filtered it with suction, washed the crystals with acetone, drained them, put the crystals in an oven at 60°C, and dried them to constant weight to obtain white crystals.

Embodiment 2

[0027] Compounds of the present invention are:

[0028]

[0029] Chemical name: +2-(4-isobutylphenyl) propionate lysine salt.

[0030] The preparation method is as follows: 100 g of dexibuprofen is placed in a reaction bottle. Add 400ml of ethanol, stir to dissolve, control the temperature between 40-78°C, gradually add 150g of lysyl acid, stir to dissolve, keep it warm for 30 minutes, after cooling down to room temperature, slowly pour the reaction solution into the prepared acetone In the solution, a white precipitate precipitated out, stirred for another 10 minutes, put it in the refrigerator for 12 hours, filtered it with suction, washed the crystal with acetone, drained it, put the crystal in an oven at 60°C, and dried it to constant weight to obtain a white crystal.

Embodiment 3

[0032] Compounds of the present invention are:

[0033]

[0034] Chemical name: +2-(4-isobutylphenyl)propionic acid histidine salt.

[0035] Its preparation method is:

[0036] Dexibuprofen 100g is placed in the reaction bottle. Add 300ml of ethanol, stir to dissolve, control the temperature between 40-78°C, gradually add 100g of histidine acid, stir to dissolve, keep it warm for 30 minutes, after cooling down to room temperature, slowly pour the reaction solution into the prepared acetone In the solution, a white precipitate precipitated out, stirred for another 10 minutes, put it in the refrigerator for 12 hours, filtered it with suction, washed the crystal with acetone, drained it, put the crystal in an oven at 60°C, and dried it to constant weight to obtain a white crystal.

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PUM

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Abstract

The invention discloses a nalorphine amino compound and preparing method with structural formula as (I), wherein the amino can be Arg, Lys or His; the molecular rate of nalorphine and amino is 1:1-1: 5 or 5:1-1:1.

Description

technical field [0001] The invention relates to a preparation method and application of dexibuprofen amino acid salt. Background technique [0002] Dexibuprofen is the dextrorotatory form of ibuprofen, and its chemical name is +2-(4-isobutylphenyl)propionic acid. It has analgesic, anti-inflammatory and antipyretic effects. Clinically, it is mainly used for arthritis, mild and moderate pain, gout and dysmenorrhea. Since the structure of Dexibuprofen is ibuprofen, it is insoluble in water, so it is unfavorable to be prepared into various dosage forms for clinical needs. Moreover, the molecule of Dexibuprofen contains acidic groups, and its aqueous solution is acidic, which is easy to produce irritation to the gastrointestinal tract. Taking Dexibuprofen is prone to produce various side effects such as gastrointestinal toxicity. When taking Dexibuprofen orally to treat chronic diseases (rheumatism and rheumatoid arthritis, etc.), long-term frequent high-dose medication will ...

Claims

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Application Information

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IPC IPC(8): C07C227/18A61K31/198A61P29/00A61P19/02A61P19/06A61P15/00
Inventor 陈亦林
Owner 陈亦林
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