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Synthesis and application of ibuprofen lysine

A technology of lysine and synthesis process, which is applied in the field of lysinoprofen synthesis and its application, can solve the problems of poor water solubility of ibuprofen, limited preparation types and clinical applications, etc., and achieves strong tolerance and expanded preparation types. and clinical application, the effect of improving bioavailability

Inactive Publication Date: 2011-09-14
SHAANXI HONGFU YIYUE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, ibuprofen has poor water solubility, which limits its preparation type and clinical application

Method used

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  • Synthesis and application of ibuprofen lysine

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Experimental program
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Effect test

Embodiment 1

[0018] Embodiment 1: Under normal temperature and normal pressure, carry out the synthetic technique of first decolorization rear reaction:

[0019] Dissolve 16.4kg (0.1kmol) of L-type and DL-lysine monohydrate (generally, it should reach more than 98% according to the dry product) in 16.4kg, 49.2kg, 82kg, 114.8kg, and 164kg of water respectively to obtain five groups Solution A1, A2, A3, A4, A5; 20.6kg (0.1kmol) ibuprofen (generally should reach more than 98% by dry product) is dissolved in 20.6kg, 61.8kg, 103kg, 144.2kg, 206kg ethanol respectively (95% industrial ethanol is enough), get five groups of solutions B1, B2, B3, B4, B5. The molar feeding ratios are respectively 1.0:1; 1.1:1; 1.2:1; 1.3:1; 1.5:1. Add 1kg (according to the total weight of the solution to calculate the amount of activated carbon added) activated carbon to decolorize the above-mentioned five groups of solutions A and five groups of solutions B respectively, and filter. Then mix the two corresponding...

Embodiment 2

[0020] Embodiment 2: Under normal temperature and pressure, carry out the synthetic technique of decolorization after first reaction:

[0021] Dissolve 16.4kg (0.1kmol) DL-lysine monohydrate in 16.4kg, 49.2kg, 82kg, 114.8kg, 164kg water to obtain solutions A1, A2, A3, A4, A5; Ibuprofen was dissolved in 20.6kg, 61.8kg, 103kg, 144.2kg, and 206kg of ethanol to obtain solutions B1, B2, B3, B4, and B5. Mix solution A and solution B, react at 25°C for 2 hours, add 2kg of activated carbon for decolorization, filter, cool, add 75kg of ethanol, cool to -10°C for 10 hours to crystallize. Centrifuge, wash with ethanol, spin dry, and dry below 50°C to obtain 23.9kg of lysinoprofen, which is a white crystalline powder.

[0022] It should be noted:

[0023] 1. In the above two embodiments, not only DL-lysine monohydrate, but also D-lysine, L-lysine and their monohydrates can be used.

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Abstract

The invention relates to synthesis and application of a medicament ibuprofen lysine. currently, the medicinal popularity of the ibuprofen lysine reaches above 95% in large cities, however, the water solubility of the ibuprofen lysine is poor, so that the preparation types and clinic application of the ibuprofen lysine are limited. The invention aims at the synthesis and application of the ibuprofen lysine, namely, preparation of high-purity compound solid bulk pharmaceutical chemical and applications of the pharmaceutical chemical as water-soluble non-steride antipyretic, analgesia and anti-inflammatory agent formulations. The synthesis method comprises the following steps: dissolving lysine in purified water so as to obtain a solution A; dissolving ibuprofen in ethanol so as to obtain a solution B; respectively adding activated carbon for decoloration and filtration, mixing, and putting the mixture in a kettle to react for 0.1-12 hours at the temperature of 0-80 DEG C; then cooling to room temperature, replenishing the ethanol, freezing and crystallizing at the temperature of minus 30 DEG C-0 DEG C; and centrifuging, washing with the ethanol, centrifugally drying, and baking, so as to obtain the white or white-like crystal ibuprofen lysine. The ibuprofen lysine has the effects that antipyretic and analgesia speed is faster than that of the ibuprofen, biological utilization degree is higher than that of the ibuprofen, toxic effect is low, and stability is good.

Description

1. Technical field [0001] The present invention relates to a kind of synthesis of medicine lysinoprofen and its application, i.e. lysinoprofen (lysine ibuprofen, Ibuprofen Lysinate) is the lysine (Lysinate) salt of ibuprofen (Ibuprofen), is a A water-soluble non-steroidal antipyretic, analgesic, and anti-inflammatory drug. 2. Background technology [0002] Ibuprofen has analgesic, anti-inflammatory and antipyretic effects. Its mechanism of action reduces the synthesis of prostaglandins through the inhibition of cyclooxygenase, thereby reducing tissue congestion and swelling caused by prostaglandins, and reducing the sensitivity of peripheral nerve pain. It acts as an antipyretic via the hypothalamic thermoregulatory center. Ibuprofen has remarkable curative effect and few adverse reactions, and it is widely used in the world rapidly after listing, and the market continues to expand. In the late 1980s, many countries in Europe and the United States turned it into an over-t...

Claims

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Application Information

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IPC IPC(8): C07C57/30C07C51/41C07C229/26C07C227/18A61K31/198A61K31/192A61P29/00
Inventor 王培良王凌波姚李潮张克军
Owner SHAANXI HONGFU YIYUE PHARMA
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