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Edaravone crystal form and preparation method thereof

A technology of edaravone and its crystal form, which is applied in the field of edaravone crystal form and its preparation, can solve the problem that the related substances are not high enough, and achieve the effect of reducing the related substances and having good water solubility

Inactive Publication Date: 2011-05-18
NANJING CHANGAO PHARMA SCI & TECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The technical problem to be solved by the present invention is that the related substances of the existing Edaravone raw materials are not high enough, and a new crystal form of Edaravone is provided at the same time

Method used

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  • Edaravone crystal form and preparation method thereof
  • Edaravone crystal form and preparation method thereof
  • Edaravone crystal form and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Embodiment 1: the preparation of Edaravone

[0021] Add 30 g of Edaravone to 120 ml of ethyl acetate-ethanol=3:2 solution, heat to reflux to dissolve it completely, decolorize activated carbon for 5 minutes, filter while it is hot, cool the filtrate to room temperature, filter, and use a small amount of cold ethyl acetate- Wash with ethanol=3:2 solution, air-dry at 40°C for 5 hours, and sieve through a 120-mesh sieve to obtain 21.8 g of white crystalline product, yield: 72.7%.

[0022] Measure under the following experimental conditions to obtain the powder X-diffraction spectrum (attached figure 1 ):

[0023] Test Unit: Modern Analysis Center of Nanjing University

[0024] Instrument: X’TRA powder diffractometer of ARL company in Switzerland

[0025] Test conditions: Target type: Cu; Tube pressure: 40kv; Tube current: 40mA; Start angle: 3; End angle: 40; Scan speed: 10; Repeat times: 1; Step size: 0.02; Slit: 2 / 4 / 0.5 / 0.2.

[0026] The following table is the powde...

Embodiment 2

[0029] Embodiment 2: the preparation of Edaravone

[0030] Add 10 g of Edaravone to 50 ml of ethyl acetate-ethanol=3:2 solution, heat to reflux to dissolve it completely, decolorize with activated carbon for 3 minutes, filter while it is hot, cool the filtrate to room temperature, filter, and use a small amount of cold ethyl acetate- Washed with ethanol=3:2 solution, air-dried at 40°C for 5 hours, and sieved through a 120-mesh sieve to obtain 6.73g of white crystalline product, yield: 67.3%. The powder X-diffraction pattern is the same as that of Example 1.

Embodiment 3

[0031] Embodiment 3: the preparation of Edaravone

[0032] Add 15g of Edaravone to 60ml of ethyl acetate-ethanol=3:2 solution, heat to reflux to dissolve it completely, decolorize with activated carbon for 6min, filter while it is hot, cool the filtrate to room temperature, filter, and use a small amount of cold ethyl acetate- Washed with ethanol=3:2 solution, air-dried at 40°C for 5 hours, and sieved through a 120-mesh sieve to obtain 10.6 g of a white crystalline product with a yield of 70.7%. The powder X-diffraction pattern is the same as that of Example 1.

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Abstract

The invention relates to an Edaravone crystal form and a preparation method thereof. The Edaravone crystal form is characterized by X-ray diffractogram of powder. The crystal form can obviously improve the water solubility of Edaravone, thereby being more beneficial to preparation of injections. Besides, related substances are further decreased, and the safety of the preparation is improved.

Description

technical field [0001] The invention relates to a specific crystal form of Edaravone and a preparation method thereof; the crystal form can obviously improve the water solubility of Edaravone, is more conducive to the preparation of injections, and further reduces related substances. The chemical structural formula of Edaravone is shown in the following formula: [0002] Background technique [0003] Edaravone is a brain protectant (free radical scavenger), which is currently on the market in Japan. Clinical studies suggest that N-acetylaspartic acid (NAA) is a specific marker of surviving nerve cells, and its content decreases sharply in the early stage of cerebral infarction. The administration of edaravone to patients in the acute stage of cerebral infarction can inhibit the reduction of local cerebral blood flow around the infarction, and make the NAA content in the brain significantly higher than that of the glycerol control group on the 28th day after the onset. P...

Claims

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Application Information

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IPC IPC(8): C07D231/26
Inventor 储刚黄海燕李战叶海姜立勋李纬
Owner NANJING CHANGAO PHARMA SCI & TECH CO LTD
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