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Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage

An elastase and inhibitor technology is applied in the application field of elastase inhibitors in the preparation of cerebral hemorrhage protection drugs, and achieves the effects of high modeling success rate, good repeatability and easy positioning

Inactive Publication Date: 2006-08-09
CHONGQING PHARMA RES INST +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is no literature report on the use of elastase inhibitors, especially neutrophil elastase inhibitors, in the treatment and prevention of brain tissue and brain cell damage caused by cerebral hemorrhage

Method used

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  • Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage
  • Use of elastic protease inhibitor for preparing medicine for protecting cerebral hemorrhage

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Example 1 Sivelestat sodium protects against cerebral hemorrhage in rats

[0038] Materials and methods

[0039] Experimental Materials:

[0040] Experimental animals:

[0041] Wistar rats, half male and half female, weighing 180-250 g, were provided by the Experimental Animal Center of Chongqing Medical University. 12h fasting before operation, free drinking water.

[0042] Main reagents and medicines:

[0043] Collagenase Type VII Sigma, USA

[0044] Chloral Hydrate Suzhou Zhengxing Chemical Factory

[0045] Sivelestat Sodium Chongqing Pharmaceutical Industry Research Institute Co., Ltd.

[0046] Nimodipine (Nirissu) Shandong Taian Pharmaceutical Factory

[0047] Main instruments:

[0048] Stereotaxic Instrument Northwest Optical Instrument Factory

[0049] Micro Syringe Shanghai Baoxi Glass Instrument Factory

[0050] Constant temperature drying oven Chongqing Experimental Instrument Factory

[0051] Electronic Analytical Balance Sartorius, Germany

[005...

Embodiment 2

[0091] Embodiment 2 sivelestat sodium freeze-dried powder injection

[0092] Sivelestat Sodium 100g

[0093] Mannitol 300g

[0094] Polyvinylpyrrolidone 100g

[0095] Appropriate amount of sodium carbonate

[0096] Dilute to 51 with water for injection

[0097] Makes 1000 bottles

[0098] Preparation Process:

[0099] Prepare sodium carbonate into a 4% solution for later use; mix sivelestat sodium, mannitol, and polyvinylpyrrolidone, add a certain amount of water for injection, stir well until dissolved, adjust the pH to 6.5-8.5 with sodium carbonate solution, and then Dilute to volume with water for injection, after primary filtration and sterilizing filtration, pack into 5ml / bottle, freeze-dry to obtain.

Embodiment 3

[0100] Embodiment 3 sivelestat sodium injection

[0101] Sivelestat Sodium 100g

[0102] HP-β-cyclodextrin 100g

[0103] EDTA-CaNa 1g

[0104] Sodium metabisulfite 1g

[0105] Sodium Phosphate Appropriate amount

[0106] Dilute to 5L with water for injection

[0107] Makes 1000 bottles

[0108] Preparation Process

[0109] Sodium phosphate is formulated into a 4% solution for later use; after mixing sivelestat sodium, HP-β-cyclodextrin, EDTA-CaNa, and sodium metabisulfite, add a certain amount of water for injection, stir fully to dissolve it, and then use Sodium phosphate solution is used to adjust the pH to 6.5-8.5, and water for injection is used to make up the volume, and after primary filtration and sterilizing filtration, it is obtained by subpackaging.

[0110] Instructions:

[0111] For patients with cerebral hemorrhage, the lyophilized powder injection is diluted with normal saline and infused at 0.2-0.5 mg / kg / hour, which can ...

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PUM

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Abstract

The present invention relates to a new medicine application of elastic proteinase inhibitor, in the concrete, it relates to an application of neutral granulocyte elastic proteinase inhibitor sevilesta in preparation of medicine for preventing or / and curing cerebral hemorrhage. It can be freeze-dried powder injection and injection liquor.

Description

technical field [0001] The present invention relates to a new medical application of an elastase (neutrophil elastase, NE) inhibitor, and more specifically relates to the application of the neutrophil elastase inhibitor sivelestat in the preparation of a drug for preventing or / and treating cerebral hemorrhage. Background technique [0002] Intracerebral hemorrhage (ICH) refers to non-traumatic intraparenchymal hemorrhage. After cerebral hemorrhage, in addition to the space-occupying damage of the hematoma itself, there are blood circulation disorders in the surrounding brain tissue, a decrease in the flow rate of local cerebral hemorrhage, metabolic disorders, Inflammatory reactions, etc., which lead to damage of surrounding cells and brain edema, resulting in neurological deficits. [0003] Stroke is a common clinical emergency, mostly in middle-aged and elderly patients. With the aging of the population, the incidence of this disease is also increasing. Hemorrhagic stroke ...

Claims

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Application Information

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IPC IPC(8): A61K31/222A61K45/00A61P9/10
Inventor 邓杰叶文润董志曾凡新刘全罗杰
Owner CHONGQING PHARMA RES INST
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