Application of nafamostat mesilate in preparing drugs for preventing and curing ischemic cerebral apoplexy

A technology of nafamostat mesylate and ischemic stroke, applied in the field of medicine

Inactive Publication Date: 2013-01-16
JIANGSU DURUI PHARMACEUTICAL CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, there is no report on whether nafamostat mesylate can be used for the treatment of stroke

Method used

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  • Application of nafamostat mesilate in preparing drugs for preventing and curing ischemic cerebral apoplexy
  • Application of nafamostat mesilate in preparing drugs for preventing and curing ischemic cerebral apoplexy
  • Application of nafamostat mesilate in preparing drugs for preventing and curing ischemic cerebral apoplexy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Study on the therapeutic effect of nafamostat mesylate on brain injury caused by permanent cerebral ischemia in rats

[0019] 1. Experimental method

[0020] 1) Animal grouping

[0021] A total of 66 clean-grade male SD rats (certificate number: SCXK (Zhejiang) 2008-0033), weighing 250-280g. Sham operation group: 6; pMCAO model group: 12; positive drug group: 12; low-dose nafamostat mesilate group: 12; middle-dose nafamostat mesilate group: 12; Nafamostat sulfonate high-dose group: 12 rats.

[0022] 2) Establishment of permanent cerebral ischemia model (pMCAO) in rats

[0023] With reference to the method of Longa et al., the rat pMCAO model was prepared by the internal carotid artery suture method: the rat was anesthetized with 3% chloral hydrate (300 mg / kg, ip), fixed in supine position, routinely disinfected, and the neck was cut in the middle The skin was bluntly dissected from all layers to expose the right common carotid artery (CCA). After the separation to ...

Embodiment 2

[0050] Study on the therapeutic effect of nafamostat mesylate on brain injury induced by cerebral ischemia-reperfusion in rats

[0051] 1. Experimental method

[0052] 1) Animal grouping

[0053] A total of 80 clean-grade male SD rats (certificate number: ), weighing 250-280g. Sham operation group: 6; tMCAO model group: 15; positive drug group: 12; low-dose nafamostat mesilate group: 17; middle-dose nafamostat mesilate group: 15; Nafamostat sulfonate high dose group: 15 rats.

[0054] 2) Establishment of rat cerebral ischemia-reperfusion model (tMCAO)

[0055] Referring to the method of Longa et al., the rat tMCAO model was prepared by the internal carotid artery suture method: the rat was anesthetized with 3% chloral hydrate (300mg / kg, ip), fixed in supine position, routinely disinfected, and the neck was cut in the middle The skin was bluntly dissected in all layers, exposing the right CCA. After the ICA and the ECA bifurcation of the external carotid artery were separa...

Embodiment 3

[0072] Preventive effect of nafamostat mesylate on brain injury induced by permanent cerebral ischemia in rats

[0073] 1. Experimental method

[0074] 1) Animal grouping

[0075] A total of 66 clean-grade male SD rats (certificate number: ), weighing 250-280g. Sham operation group: 6; pMCAO model group: 10; positive drug group: 10; test drug low dose group: 11; test drug medium dose group: 12; test drug high dose group: 11 .

[0076] 2) Establishment of experimental rat permanent cerebral ischemia model (pMCAO)

[0077] With reference to the method of Longa et al., the rat pMCAO model was prepared by the internal carotid artery suture method: the rat was anesthetized with 3% chloral hydrate (300 mg / kg, ip), fixed in supine position, routinely disinfected, and the neck was cut in the middle The skin was bluntly dissected from all layers to expose the right common carotid artery (CCA). After the separation to the bifurcation of the internal carotid artery ICA and the exter...

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Abstract

The invention relates to the technical field of drugs and aims to provide a new use of nafamostat mesilate in preparing drugs for preventing and curing ischemic cerebral apoplexy. Preoperative preventative administration or postoperative therapeutic administration is performed on a classical permanent cerebral ischemia model (permanent middle cerebral artery occlusion-pMCAO) and a classical cerebral ischemia reperfusion model (transient middle cerebral artery occlusion-tMCAO) by the invention, respectively, and the results show that the nafamostat mesilate is remarkable in effect of resisting the ischemic cerebral apoplexy. At a dosage point appointed by experiments, the nafamostat mesilate can be used for obviously improving animal behavior dysfunctions caused by ischemia and lowering the cerebral infarction rate of permanent cerebral ischemia and cerebral ischemia reperfusion rats. Prompted by research results, the nafamostat mesilate can be used for preventing and curing the ischemic cerebral apoplexy.

Description

Technical field: [0001] The invention relates to the technical field of medicine, in particular to the new application of nafamostat mesylate for preventing and treating ischemic cerebral apoplexy. Background technique: [0002] According to statistics in recent years, there are about 1.3 to 1.5 million new cases of cerebral apoplexy in my country every year, and about 1 million deaths, which is 4 to 5 times higher than that in European and American countries. At present, the incidence of stroke in my country is increasing at an annual rate of nearly 9%. Stroke has the characteristics of high morbidity, high mortality and high disability rate, which brings a heavy burden to individuals, families and society. Ischemic stroke accounts for 70% of the total number of stroke patients. It refers to the disorder of cerebral blood flow and ischemic necrosis of brain tissue caused by various reasons, resulting in corresponding neurological deficit symptoms. Clinically common stroke...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/245A61P9/10
Inventor 廖红王静李晨辉陈涛王艺瑾安鲁凡
Owner JIANGSU DURUI PHARMACEUTICAL CO LTD
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