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Stable edaravone trihydrate and pharmaceutical compositions thereof

A technology of hydrate and edaravone, which is applied in the field of medicine, can solve the problems such as difficult dissolution of edaravone, and achieve the effect of simple method, high yield and good stability

Inactive Publication Date: 2014-01-01
TIANJIN SONGRUI MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The first object of the present invention is to provide a stable Edaravone trihydrate, which can overcome the deficiencies of the prior art and effectively solve the problems such as Edaravone being difficult to dissolve in water

Method used

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  • Stable edaravone trihydrate and pharmaceutical compositions thereof
  • Stable edaravone trihydrate and pharmaceutical compositions thereof
  • Stable edaravone trihydrate and pharmaceutical compositions thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] 1) Put 5.0g of crude Edaravone into a one-mouth bottle, add 80ml of pure ethanol aqueous solution (ethanol: pure water = 1:3), and stir to dissolve at 45°C;

[0054] 2) Then adjust the Edaravone solution to pH = 4.0 with hydrochloric acid at room temperature, add 600ml of ether and acetone mixture (ether: acetone = 1:2.5), stir and crystallize at 20°C for 3 hours;

[0055] 3) The precipitated Edaravone crystals were collected by filtration, washed with 100ml of the above ether and acetone mixture and dried in an oven at 30°C to obtain 4.5g of Edaravone trihydrate with a yield of 90% and a purity of 99.7%. .

Embodiment 2

[0057] 1) Put 5.0 g of crude Edaravone into a one-mouth bottle, add 100 ml of pure ethanol aqueous solution (ethanol: pure water = 1:3), and stir to dissolve at 48°C;

[0058] 2) Then adjust the Edaravone solution to pH = 4.2 with hydrochloric acid at room temperature, add 500ml of isopropyl ether and acetone mixture (isopropyl ether: acetone = 1:3), stir and crystallize at 30°C for 5 hours;

[0059] 3) The precipitated Edaravone crystals were collected by filtration, washed with 100ml of the above isopropyl ether and acetone mixture and dried in an oven at 30°C to obtain 4.55g of Edaravone trihydrate, with a yield of 91%, a purity of 99.6%.

Embodiment 3

[0061] Preparation of edaravone trihydrate pharmaceutical composition prepared 1000, made up of the following proportioning weight:

[0062]

[0063] Including the following steps:

[0064] 1) Preparation: receive the Edaravone trihydrate and auxiliary materials, and set aside;

[0065] 2) Take 70% of the prescribed amount of water for injection, at a temperature of 60°C, add the prescribed amount of calcium sodium edetate, acetylcysteine, and sodium chloride, stir until dissolved, and then add the prescribed amount of edax to the solution Lavone, stir until completely dissolved;

[0066] 3) Add 0.1% medicinal charcoal of the volume of the liquid medicine to item 2), stir well, and let stand for 30 minutes;

[0067] 4) Filter 3) with a plate-and-frame filter, add water for injection to the full amount, mix well, and measure the initial pH value. According to the initial pH value, use 4% sodium hydroxide solution and 10% phosphoric acid solution to adjust the pH range to 3...

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Abstract

The invention belongs to the technical field of medicine, and provides stable edaravone trihydrate, edaravone trihydrate pharmaceutical compositions for injection, a method for preparing the edaravone trihydrate and a method for preparing the edaravone trihydrate pharmaceutical compositions. Crude edaravone trihydrate is stirred and dissolved in an ethyl alcohol-pure water solution, the pH value is adjusted through hydrochloric acid to range from 3 to 5, and then liquor formed by mixing ethers and ketone according to the volume ratio of 1:(1-4) is added to the solution, and stirring and crystallization are carried out; filtering, collecting, washing and vacuum drying are carried out to obtain the edaravone trihydrate which is high in yield and purity and stable in quality. The edaravone trihydrate pharmaceutical compositions, for injection, prepared according to the preparation formulation and the preparation technology are stable in quality and can be easily employed in an industrialized mode.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a stable edaravone trihydrate and a pharmaceutical composition thereof. Background technique [0002] Edaravone [0003] Chemical name: 3-Methyl-1-phenyl-2-pyrazolin-5-one (3-Methyl-1-phenyl-2-pyrazolin-5-one); [0004] Molecular formula: C 10 h 10 N 20 ; [0005] Molecular weight: 174.20; [0006] Structural formula: [0007] Since the main ring of Edaravone is a five-membered ring ketone, the carbonyl group is adjacent to N, and the N at position 2 is connected to an unsaturated bond, which is easy to oxidize, so the molecular structure is very unstable, and it will be oxidized to There is no active substance, and it is easy to produce high molecular impurities, which will cause harm to the human body. In addition, because there are no hydrophilic groups such as hydroxyl and carboxyl in the structure, and methyl and phenyl are insoluble in water, the long-term dissolution pro...

Claims

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Application Information

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IPC IPC(8): C07D231/26A61K31/4152A61K9/08A61P39/06
CPCC07D231/26
Inventor 张昊
Owner TIANJIN SONGRUI MEDICAL TECH
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