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Edaravone pharmaceutical composition

A technology of composition and medicine, applied in the field of medicine, can solve the problems of difficulty in preparation, unsatisfactory performance (unsatisfactory release rate of stability), etc.

Active Publication Date: 2020-09-22
BEIJING TIANTAN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] However, sublingual pharmaceutical compositions containing edaravone are not readily available
The inventors have found through experiments that a variety of commonly used excipients are not suitable for preparing qualified sublingual preparations, or the performance (stability, release rate, etc.) of the prepared sublingual preparations is not satisfactory

Method used

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  • Edaravone pharmaceutical composition
  • Edaravone pharmaceutical composition
  • Edaravone pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037]

[0038]

[0039]Preparation method: Mix Edaravone, lactose, hypromellose, croscarmellose sodium and magnesium stearate evenly according to the formula ratio, and press into tablets.

Embodiment 2

[0041] Material name Dosage / tablet (mg) effect Edaravone 30 active ingredient starch 41.2 filler hypromellose 4 Adhesive Croscarmellose Sodium 4 disintegrant Magnesium stearate 0.8 lubricant

[0042] Preparation method: Mix Edaravone, starch, hypromellose, croscarmellose sodium and magnesium stearate evenly according to the formula ratio, and press into tablets.

Embodiment 3

[0044] Material name Dosage / tablet (mg) effect Edaravone 30 active ingredient microcrystalline cellulose 41.2 filler hypromellose 4 Adhesive Croscarmellose Sodium 4 disintegrant Magnesium stearate 0.8 lubricant

[0045] Preparation method: Mix Edaravone, microcrystalline cellulose, hypromellose, croscarmellose sodium and magnesium stearate evenly according to the formula ratio, and press into tablets.

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PUM

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Abstract

The invention discloses an edaravone pharmaceutical composition and its use as a sublingual preparation, wherein the pharmaceutical composition comprises edaravone or its salt and mannitol. The sublingual administration preparation can avoid the liver first-pass effect, and the sample has the advantages of good stability, easy transportation, and convenient use.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a sublingual pharmaceutical composition of edaravone and its application. Background technique [0002] Edaravone (chemical name: 3-methyl-1-phenyl-2-pyrazolin-5-one) is a listed neuroprotective agent (Yakugaku Zasshi.2004,124(3):99-111 ). Studies have shown that Edaravone has antioxidant activity, can significantly improve the neurological deficit symptoms of cerebral ischemia-reperfusion animals, reduce the infarct size, reduce the degree of brain damage, reduce cerebral edema, and inhibit lipid peroxidation in damaged brain tissue . [0003] [0004] Edaravone [0005] (molecular formula C 10 h 10 N 2 O, molecular weight 174.20) [0006] Cerebrovascular disease, especially ischemic cerebrovascular disease is an acute disease that needs to be relieved quickly, so injection is the first choice for first aid. However, intramuscular injection or intravenous injection can...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K9/20A61K47/10A61K47/38A61K31/4152A61P9/10A61P25/02A61P21/00
CPCA61P9/10A61K9/0056A61K9/2018A61K31/4152A61K9/006A61P25/00A61K47/26A61P21/00A61K9/2009A61K9/2013A61K9/2027A61K9/2054A61K9/2031A61K9/2059
Inventor 王伊龙王拥军赵性泉张安元
Owner BEIJING TIANTAN HOSPITAL AFFILIATED TO CAPITAL MEDICAL UNIV