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

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Problems solved by technology

[0012] The technical problem to be solved by the present invention is that the related substances of the existi

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

Example Embodiment

[0020] Example 1: Preparation of edaravone

[0021] Add 30g of edaravone to 120ml of ethyl acetate-ethanol=3:2 solution, heat to reflux to dissolve all, decolorize the activated carbon for 5min, filter while hot, cool the filtrate to room temperature, filter, and use a small amount of cold ethyl acetate- Ethanol=3:2 solution washing, 40° C. air drying for 5 hours, 120 mesh sieving to obtain 21.8 g of white crystalline product, yield: 72.7%.

[0022] The powder X-diffraction pattern was measured under the following experimental conditions (attached figure 1 ):

[0023] Testing unit: Modern Analysis Center of Nanjing University

[0024] Instrument: X’TRA powder diffractometer from Swiss ARL Company

[0025] Test conditions: target type: Cu; tube pressure: 40kv; tube flow: 40mA; starting angle: 3; ending angle: 40; scanning speed: 10; number of repetitions: 1; step length: 0.02; slit: 2 / 4 / 0.5 / 0.2.

[0026] The following table shows the powder X-diffraction spectrum data of edaravone pre...

Example Embodiment

[0029] Example 2: Preparation of edaravone

[0030] Add 10g of edaravone to 50ml of ethyl acetate-ethanol=3:2 solution, heat to reflux to dissolve all, decolorize the activated carbon for 3min, filter while hot, cool the filtrate to room temperature, filter, and use a small amount of cold ethyl acetate- Ethanol=3:2 solution washing, 40° C. air drying for 5 hours, 120 mesh sieving to obtain 6.73 g of white crystalline product, yield: 67.3%. The powder X-ray diffraction pattern is the same as in Example 1.

Example Embodiment

[0031] Example 3: Preparation of edaravone

[0032] Add 15g of edaravone to 60ml of ethyl acetate-ethanol=3:2 solution, heat to reflux to dissolve all, decolorize the activated carbon for 6min, filter while hot, cool the filtrate to room temperature, filter, and use a small amount of cold ethyl acetate- Ethanol=3:2 solution washing, 40° C. air drying for 5 hours, 120 mesh sieving to obtain 10.6 g of white crystalline product, yield: 70.7%. The powder X-ray diffraction pattern is the same as in 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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