Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

A kind of edaravone sodium chloride injection 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: 2021-07-16
JINAN KANGHE MEDICAL TECH
View PDF20 Cites 0 Cited by
  • 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A kind of edaravone sodium chloride injection and preparation method thereof
  • A kind of edaravone sodium chloride injection and preparation method thereof
  • A kind of edaravone sodium chloride injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039]

[0040] Preparation:

[0041] (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;

[0042] (2) Constant volume, fine filtration through 0.22 μm filter membrane;

[0043] (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

[0045]

[0046] Preparation:

[0047] (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;

[0048] (2) Constant volume, fine filtration through 0.22 μm filter membrane;

[0049] (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

[0051]

[0052]

[0053] Preparation:

[0054] (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;

[0055] (2) Constant volume, fine filtration through 0.22 μm filter membrane;

[0056] (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.

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
melting pointaaaaaaaaaa
Login to View More

Abstract

The invention relates to an edaravone sodium chloride injection and a preparation method thereof. 100ml of the injection includes: edaravone 20-40mg, sodium chloride 0.6-1.0g, propylene glycol 100-150mg, vitamin C 2.5-3.5g, sodium bicarbonate 0.3-1.0g, pH adjusted to 3.5-5.0. The preparation process of the injection comprises: dosing, filtering, filling, capping, sterilizing, and lamp inspection; the dosing adopts a two-step preparation method, and the preparation process adopts low-temperature preparation. The method is simple to operate and low in cost, and the prepared Edaravone Sodium Chloride Injection has good drug stability, less side effects, effectively reduces the production of impurities, and has high drug compliance and safety for patients. It is used to improve acute cerebral palsy Neurological symptoms, activities of daily living and dysfunction caused by infarction 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

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K47/10A61K47/22A61K47/02A61P25/00A61P9/10A61K31/4152
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
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com