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Edaravone injection and preparation method thereof

A technology of edaravone and injection, which is applied in the direction of pharmaceutical formulations, medical preparations containing no active ingredients, and medical preparations containing active ingredients. Water and other issues

Inactive Publication Date: 2011-01-05
NANJING SIMCERE DONGYUAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Methyl groups and benzene groups are insoluble in water. Adjusting the pH value can increase its solubility, but at the same time it will also increase its oxidation and cause instability
After 2005, China successively approved five enterprises to produce Edaravone injection, but they paid little attention to the anti-oxidation. Some (Patent Publication No. CN 1440749A) used sodium bisulfite as an antioxidant. It is difficult to solve the problem of easy oxidation and instability of this product, and the validity period of these enterprises is one and a half years

Method used

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  • Edaravone injection and preparation method thereof
  • Edaravone injection and preparation method thereof
  • Edaravone injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0082] Embodiment 1: specification: 5ml: 10mg

[0083] formula:

[0084]

[0085] Take a propylene glycol hot water bath and heat to 60-70°C, add Edaravone, and stir until completely dissolved. Separately weigh sodium metabisulfite (0.1%) and pour it into a beaker, add water for injection and stir until completely dissolved. Slowly add the pre-dissolved antioxidant-containing solution to the edaravone propylene glycol solution while stirring, and then slowly add water for injection to 1 / 4 of the total volume while stirring. Then add activated carbon for needles (0.1%), warm and stir for 15 minutes, let stand, filter with suction, and remove carbon. Add the remaining water for injection. Adjust the pH to 4.0 with 0.1mol / L hydrochloric acid, check the intermediate, and fine-filter it with a 0.22μm microporous membrane until it is clear, fill it with nitrogen, fill it in an ampoule, and sterilize it by autoclaving at 115°C for 30 minutes. After three years, all inspections...

Embodiment 2

[0086] Embodiment 2: specification: 5ml: 10mg

[0087] formula:

[0088]

[0089] Take a propylene glycol hot water bath and heat to 60-70°C, add Edaravone, and stir until completely dissolved. Separately weigh sodium metabisulfite (0.15%) and pour it into a beaker, add water for injection and stir until completely dissolved. Slowly add the pre-dissolved antioxidant-containing solution to the edaravone propylene glycol solution while stirring, and then slowly add water for injection to 1 / 4 of the total volume while stirring. Then add activated carbon for needles (0.1%), warm and stir for 15 minutes, let stand, filter with suction, and remove carbon. Add the remaining water for injection. Adjust the pH to 4.2 with 0.1 mol / L hydrochloric acid, check the intermediate, and fine-filter it with a 0.22 μm microporous membrane until it is clear, fill it with nitrogen, fill it in an ampoule, and sterilize it by autoclaving at 115°C for 30 minutes. After three years, all inspecti...

Embodiment 3

[0090] Embodiment 3: specification: 20ml: 30mg

[0091] formula:

[0092]

[0093]Take a propylene glycol hot water bath and heat to 60-70°C, add Edaravone, and stir until completely dissolved. Separately weigh sodium metabisulfite (0.1%) and pour it into a beaker, add water for injection and stir until completely dissolved. Slowly add the pre-dissolved antioxidant-containing solution to the edaravone propylene glycol solution while stirring, and then slowly add water for injection to 1 / 4 of the total volume while stirring. Then add activated carbon for needles (0.1%), warm and stir for 15 minutes, let stand, filter with suction, and remove carbon. Add the remaining water for injection. Adjust the pH to 3.9 with 0.1mol / L hydrochloric acid, check the intermediate, fine filter with a 0.22μm microporous membrane until it is clear, fill it with nitrogen, fill it in an ampoule, and sterilize it by autoclaving at 115°C for 30 minutes. After three years, all inspections meet t...

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Abstract

The invention discloses edaravone injection and a preparation method thereof. The injection contains edaravone serving as an active material, sodium pyrosulfite serving as antioxygen and propylene glycol serving as cosolvent. In the invention, in an edaravone injection production process, the sodium pyrosulfite antioxygen is added and high-purity nitrogen is charged into an ampoule bottle before and after liquid medicine canning and sealing to ensure the residual oxygen in the air above the liquid medicine in the ampoule bottle is less than 3 percent, so the edaravone is kept in a low-oxygen environment all the time. In the invention, the stability of the edaravone injection is improved, the period of validity of the edaravone injection is prolonged, and the safety and effectiveness of the edaravone injection in clinical use are ensured.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a stable Edaravone injection preparation and a preparation process. Background technique [0002] Edaravone Injection (Edaravone Injection) is a cranial neuroprotective agent developed by Mitsubishi Tokyo Pharmaceutical Co., Ltd. for the treatment of patients with acute cerebral infarction. Nanjing Xiansheng Dongyuan Pharmaceutical Co., Ltd. was the first to develop and market in my country in December 2003. The product name is Bi , the drug is a new type of free radical scavenger and neuroprotective drug for the treatment of ischemic cerebrovascular diseases, and has clear clinical efficacy in the treatment of cardiovascular and cerebrovascular diseases, especially acute ischemic stroke. [0003] The chemical name of Edaravone is: 3-Methyl-1-phenyl-2-pyrazolin-5-one (3-Methyl-1-phenyl-2-pyrazolin-5-one), and its structural formula is: [0004] ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/4152A61K47/02A61K47/10A61P9/10A61P25/00A61P39/06
Inventor 罗兴洪任晋生周进东彭素琴陈为功
Owner NANJING SIMCERE DONGYUAN PHARM CO LTD
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