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Edaravone lyophilized preparation and preparation technique thereof

A freeze-dried preparation and preparation process technology, applied in the field of pharmaceutical preparations, can solve the problems of low drug concentration, difficulty in actual production, difficulty in determining whether the improvement of solubility can meet the requirements of actual use, etc., and achieve the effect of simple preparation process

Active Publication Date: 2008-10-22
JIANGSU SIMCERE PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The first patent is about the combination of Edaravone and alkaline substances. It uses alkaline substances in the prescription to increase the pH value of the solution, so that the solubility of Edaravone in water is improved, and then water is used as the freeze-drying medium. Freeze-drying, but the addition of alkaline medium will greatly aggravate the instability of Edaravone, and it is difficult to determine whether the improvement of solubility can meet the requirements of actual use
The latter two patents are to dissolve Edaravone in water or ethanol / water for freeze-drying. Since Edaravone is difficult to dissolve in water, the actual drug concentration in the aqueous solution is low; while the freezing point of ethanol is minus 144 degrees, common It is difficult for the freeze dryer to freeze and capture the ethanol gas extracted during sublimation drying, which leads to difficulties in actual production

Method used

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  • Edaravone lyophilized preparation and preparation technique thereof
  • Edaravone lyophilized preparation and preparation technique thereof
  • Edaravone lyophilized preparation and preparation technique thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] prescription:

[0029] Edaravone 10g

[0030] Mannitol 200g

[0031] tert-butanol 750ml

[0032] Add water for injection to 5000ml

[0033] Preparation: Take the prescribed amount of Edaravone, add 750ml of tert-butanol (if the room temperature is low, tert-butanol is a solid, it can be heated at 35°C to dissolve and then used), stir to dissolve, add water for injection to 5000ml, and stir evenly , add the prescribed amount of mannitol, stir to dissolve, and obtain the drug-containing solution. Add 0.1% activated carbon and stir at 40°C for 30 minutes, filter to decarbonize, then filter through a 0.22um microporous membrane, pack in vials, and freeze-dry according to the freeze-drying process.

Embodiment 2

[0035] prescription:

[0036] Edaravone 75g

[0037] Lactose 125g

[0038] tert-butanol 2250ml

[0039] Add water for injection to 5000ml

[0040] Preparation: Take the prescribed amount of Edaravone, add 2250ml of tert-butanol (if the room temperature is low, tert-butanol is solid, it can be heated at 35°C to dissolve and then used), stir to dissolve. Get the lactose of the prescribed amount, add water for injection to 5000ml, stir to dissolve, mix with tert-butanol solution evenly, and obtain the drug-containing solution. Add 0.1% activated carbon and stir at 40°C for 30 minutes, filter to decarbonize, then filter through a 0.22um microporous membrane, pack in vials, and freeze-dry according to the freeze-drying process.

Embodiment 3

[0042] prescription:

[0043] Edaravone 10g

[0044] Mannitol 200g

[0045] Sucrose 200g

[0046] tert-butanol 1750ml

[0047] Add water for injection to 5000ml

[0048]Preparation: Take the prescribed amount of Edaravone, add 1750ml of tert-butanol (if the room temperature is low, tert-butanol is a solid, it can be heated at 35°C to dissolve and then taken), stir to dissolve, add water for injection to 5000ml, stir evenly , add the prescribed amount of mannitol and sucrose, stir to dissolve, and obtain the drug-containing solution. Add 0.1% activated carbon and stir at 40°C for 30 minutes, filter to remove carbon, then filter through a 0.22um microporous membrane, pack in vials, and freeze-dry according to the freeze-drying process.

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PUM

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Abstract

The invention relates to a stable edaravone freeze-dried preparation, a preparation process and a using method. The preparation is composed of edaravone and a freeze-dried stabilizer. The preparation process is that the edaravone and the freeze-dried stabilizer are dissolved in a mixed solvent system with tertiary butyl alcohol / water, and the freeze-drying process is carried out for freeze-drying. The preparation has stable quality and the preparation process is applicable to the industrial production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations. The invention relates to a stable edaravone freeze-dried preparation and a preparation process thereof. Background technique [0002] Edaravone (edaravone) is the first oxygen free radical scavenger for the treatment of cerebral infarction developed by Japan's Mitsubishi Pharmaceutical Company and first launched in the world in 2001. Nanjing Xiansheng Dongyuan Pharmaceutical Co., Ltd. In December, it was the first company in China to be approved for production and launch. The chemical name of Edaravone is: 3-methyl-1-phenyl-2-pyrazolin-5-one, and the English chemical name is: 3-methyl-1-phenyl-2-pyrazolin-5-one. The chemical structural formula is as follows: [0003] [0004] Pharmacological studies have shown that intravenous administration of edaravone to rats after ischemia / ischemia-reperfusion can prevent the progression of cerebral edema and cerebral infarction, rel...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/4152A61P9/10
Inventor 和健李晓强黄圣娟江征刘春晖张浩波许向阳张斐
Owner JIANGSU SIMCERE PHARMA
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