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Pharmaceutical application of nafamostat

A technology of nalimus, which is applied in the direction of medical preparations containing active ingredients, drug combinations, pharmaceutical formulas, etc., can solve problems such as hindering the extension of regenerated axons and affecting functional recovery, so as to promote the recovery of motor function and promote survival , the effect of reducing apoptosis

Active Publication Date: 2015-06-17
冯世庆
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Glial scar hinders the extension of regenerated axons to the distal end, and ultimately seriously affects the long-term functional recovery

Method used

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  • Pharmaceutical application of nafamostat
  • Pharmaceutical application of nafamostat
  • Pharmaceutical application of nafamostat

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Example 1 Therapeutic Trial of Nafamostat on Spinal Cord Injury

[0030] Using 8-week-old female Wistar rats, the New York University (NYU) standard spinal cord injury impactor (Impactor Model II) was used to impact the spinal cord at the 10th segment of the rat thorax to construct an animal model of spinal cord injury. Eight hours after the injury, Nafamostat was given by intraperitoneal injection at a dose of 10 mg / kg, and methylprednisolone was given by tail vein injection at a dose of 30 mg / kg, once a day until 2 weeks after the injury; Saline served as a control. BBB score, TUNEL, NF-200 and GFAP staining were used to observe the functional recovery, apoptosis after injury, the number of neurons survived and the size of glial scar after treatment.

[0031] Figure 1-4 It shows the comparison of the therapeutic effect of the nafamostat treatment group, the methylprednisolone treatment group and the normal saline control group when the drug was administered 8 hou...

Embodiment 2

[0033] Example 2 Comparison of the therapeutic effects of namostat and methylprednisolone when administered at different times

[0034] In this example, the efficacy of nafamostat for the clinical treatment of spinal cord injury was determined by comparing the curative effects of nafamostat and methylprednisolone when administered at different times.

[0035] Eight-week-old female Wistar rats were divided into three groups (30 rats in each group), and the spinal cord was hit at the thoracic 10th segment of the rats with the New York University (NYU) standard spinal cord injury impactor (Impactor Model II). Immediately after the blow was selected ( 0 hour), 3 hours, 8 hours, and 24 hours, the three groups of animals were treated with normal saline, methylprednisolone, and nafamostat for 2 weeks, and the recovery of the rats was observed.

[0036] Figure 5-6 A comparison of the therapeutic effects of the nafamostat treatment group, the methylprednisolone treatment group and ...

Embodiment 3

[0038] Example 3 Nafamostat dosing trial

[0039] In order to determine the optimal dosage of Nafamostat, a gradient concentration of Nafamostat (1mg / kg, 3mg / kg, 10mg / kg, 30mg / kg and 100mg / kg) was designed to treat rats with spinal cord injury. Simple PBS injection group was used as control. Figure 7 The BBB scores of rats treated with different concentrations of nafamostat are shown, from Figure 7 It can be seen that with the increase of the administration concentration, the BBB score increases synchronously, and the BBB score is higher when 10mg / kg, 30mg / kg and 100mg / kg are used. Considering that 10mg / kg, 30mg / kg and 100mg / kg There was no statistically significant difference in the BBB scores of the three groups, and 10 mg / kg was used as the applied dose for animal experiments.

[0040] Based on the above research results, for patients with spinal cord injury, according to the usual 50:1 dose conversion relationship between animals (rats) and humans, 0.2 mg / kg is used ...

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Abstract

The invention provides application of nafamostat in preparation of a medicament for treating spinal cord injury. The nafamostat is applied to therapeutic intervention of the spinal cord injury, and experiments show that the nafamostat can reduce apoptosis of cells, promote survival of neurons, inhibit formation of glial scars and remarkably improve the BBB score of a treated animal. Compared with a methylprednisolone medicament applied clinically at present, the nafamostat has the advantages of wider administration window, more lasting treatment effect and better long-term effect.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to the use of namostat in preparing medicines for spinal cord injuries. Background technique [0002] Nafamostat (nafamostat) is a synthetic serine proteolytic enzyme inhibitor with anticoagulant, antiplasmin and antiplatelet aggregation effects. Trypsin-like serine proteases such as plasmin, fibrinase, and CL-r and CL-s of the classical pathway of the complement system have a strong selective inhibitory effect. Nafamostat can inhibit the production of inflammatory mediators IL-6, IL-8, TNF-α, IL-1β and NOS, and is currently mainly used clinically for the treatment of acute pancreatitis. The inhibitory effect of nafamostat on the inflammatory response of organs other than the pancreas remains to be further studied. [0003] The incidence of acute spinal cord injury (SCI) caused by various accidents has increased year by year in recent years, and has become a common clinical dis...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/235A61P25/00A61P19/00
Inventor 冯世庆周新福刘燊安鲁凡吴秋丽史宏宇
Owner 冯世庆
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