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Edaravone sodium chloride injection liquid and preparation method thereof

A technology of edaravone sodium chloride and injection, which is applied in the direction of active ingredients of alkali/alkaline earth metal chlorides, pharmaceutical formulas, medical preparations of non-active ingredients, etc., and can solve the problem of uneven stability and influence on drug use Safety, long-term medication and other issues to achieve the effect of avoiding the generation of harmful impurities, improving the safety and compliance of medication, and reducing the generation of impurities

Active Publication Date: 2019-08-06
JINAN KANGHE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, there are common problems in the production, storage and use of Edaravone: ① Since the main ring of Edaravone is a five-membered ring ketone, the carbonyl group is adjacent to N, the structure is unstable, and oxidation is easy to occur, and high temperature can accelerate Oxidation, easy to produce polymer impurities, causing harm to the human body; ②Edaravone is very slightly soluble or insoluble in water, and its solubility is poor; ③The current clinical application of Edaravone injection is 20ml: 30mg small water injection, and Added cysteine ​​hydrochloride and sodium bisulfite as antioxidants in the prescription, cysteine ​​hydrochloride is prone to degradation during storage, resulting in insoluble cystine, resulting in small white spots in the solution, affecting the efficacy of the drug Safety; ④ Edaravone requires long-term medication in clinical use (medication within 24 hours after onset, and a course of treatment is within 14 days). Diluted, inconvenient to use
It needs to be diluted with sodium chloride injection to make a small water injection, and it needs to be used for a long time in clinical use (medication within 24 hours after the onset of the disease, and a course of treatment is within 14 days), which is inconvenient to use. Moreover, the small water injection components of Edaravone injection are different, and the stability within the validity period is uneven.

Method used

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  • Edaravone sodium chloride injection liquid and preparation method thereof
  • Edaravone sodium chloride injection liquid and preparation method thereof
  • Edaravone sodium chloride injection liquid and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041]

[0042] Preparation:

[0043] (1) Weigh 20% of the prescribed amount of water for injection, keep it warm at 20-30°C, fill the liquid with nitrogen for 15 minutes, add the prescribed amount of propylene glycol, stir to dissolve vitamin C, add edaravone and stir to dissolve, add sodium chloride and stir Dissolve, add 70% water for injection, add sodium carbonate to adjust the pH to 3.5;

[0044] (2) Constant volume, fine filtration through 0.22 μm filter membrane;

[0045] (3) Divide the obtained medicinal solution into 100ml / bottles, fill with nitrogen, stopper, cover, and sterilize with damp heat at 126°C for 6 minutes to obtain the finished product.

Embodiment 2

[0047]

[0048] Preparation:

[0049] (1) Weigh 20% of the prescribed amount of water for injection, keep it warm at 20-30°C, fill the liquid with nitrogen for 15 minutes, add the prescribed amount of glycerin, stir to dissolve vitamin C, add edaravone and stir to dissolve, add sodium chloride and stir Dissolve, add 70% water for injection, add sodium bicarbonate to adjust the pH to 5.0;

[0050] (2) Constant volume, fine filtration through 0.22 μm filter membrane;

[0051] (3) Divide the obtained medicinal solution into 100ml / bottles, fill with nitrogen, stopper, cover, and sterilize with damp heat at 126°C for 8 minutes to obtain the finished product.

Embodiment 3

[0053]

[0054]

[0055] Preparation:

[0056] (1) Weigh 20% of the prescribed amount of water for injection, keep it warm at 20-30°C, fill the liquid with nitrogen for 15 minutes, add the prescribed amount of propylene glycol, glycerin, vitamin C and stir to dissolve, add edaravone and stir to dissolve, add chloride Stir and dissolve the sodium, add 70% water for injection, add sodium bicarbonate and sodium carbonate to adjust the pH to 4.5;

[0057] (2) Constant volume, fine filtration through 0.22 μm filter membrane;

[0058] (3) Divide the obtained medicinal solution into 100ml / bottles, fill with nitrogen, stopper, cover, and sterilize with damp heat at 126°C for 6 minutes to obtain the finished product.

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Abstract

The invention relates to an edaravone sodium chloride injection liquid and a preparation method thereof. 100 ml of the injection liquid comprises 20-40 mg of edaravone, 0.6-1.0 g of sodium chloride, 100-150 mg of propylene glycol, 2.5-3.5 g of vitamin C, and 0.3-1.0 g of sodium hydrogen carbonate, wherein the pH is adjusted to 3.5-5.0. The preparation process of the injection liquid comprises thesteps: liquid preparation, filtration, filling, capping, sterilization and lamp inspection; liquid preparation adopts a two-step preparation method, and the preparation process adopts low temperaturepreparation. The adopted method is simple to operate and low in cost, and the prepared edaravone sodium chloride injection liquid has good drug stability and fewer side effects, can effectively reducethe generation of impurities, has high patient compliance with medication and safety, can be used for improving neurological symptoms, daily living activities and function disorder caused by acute cerebral infarction, and can effectively prevent and treat brain injury.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to an edaravone sodium chloride injection and a preparation method thereof. Background technique [0002] Edaravone, Chinese chemical name: 3-methyl-1-phenyl-2-pyrazolin-5-one, English name: 3-methyl-1-phenyl-2-pyrazolin-5 -one with a CAS registry number of 89-25-8. [0003] [0004] This product is white or off-white crystalline powder, odorless and tasteless, with a melting point of 127.5-128.5°C. Edaravone is a brain protectant (free radical scavenger), which can prevent the peroxidative damage of brain cells (vascular endothelial cells, nerve cells) by eliminating free radicals and inhibiting lipid peroxidation. It is used to improve neurological symptoms, activities of daily living and dysfunction caused by acute cerebral infarction. By inhibiting cerebral edema, cerebral infarction, neurological symptoms, inhibiting delayed neuronal cell death and other neuropr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K33/14A61K9/08A61K47/10A61K47/22A61K47/02A61P25/00A61P9/10A61K31/4152
CPCA61K9/0019A61K9/08A61K31/4152A61K33/14A61K47/02A61K47/10A61K47/22A61P9/10A61P25/00A61K2300/00
Inventor 王丽伟李鹏张颖李娟娟王磊磊孙丽梦杨静静
Owner JINAN KANGHE MEDICAL TECH
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