Application of pinocembrin to preparation of anti-cerebral hemorrhage drugs

A drug and hemorrhagic technology, which is applied in the application field of pinoselin in the preparation of anti-intracerebral hemorrhage drugs, can solve problems such as no report on the application of pinoselin, achieve significant vascular protection effect, reduce vascular damage, reduce The effect of HT risk

Inactive Publication Date: 2016-11-30
INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But do not see the application report of pinocerine in the preparation anticerebral hemorrhage drug so far

Method used

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  • Application of pinocembrin to preparation of anti-cerebral hemorrhage drugs
  • Application of pinocembrin to preparation of anti-cerebral hemorrhage drugs
  • Application of pinocembrin to preparation of anti-cerebral hemorrhage drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030]Example 1. Pinocerin injection was prepared according to the following method. (1) pulverize the pinoscelin raw material, cross 100 mesh sieves, and set aside; (2) take by weighing the hydroxypropyl-beta-cyclodextrin of prescription quantity, add 700ml water for injection and stir to dissolve; (3) add 0.5% ( g / ml) gac for injection, kept boiling slightly for 30 minutes, and decarbonized by filtration; (4) took by weighing the pinocerine of prescription quantity, and added in the above-mentioned hydroxypropyl-beta-cyclodextrin aqueous solution at room temperature; (5) ) Slowly add 10% aqueous sodium hydroxide solution dropwise under stirring, adjust and keep the pH value of the solution between 8.4~8.5, stir for about 4 hours, until the pinocerine is completely dissolved; (6) add water for injection to 1000ml, Stir well; (7) add 0.05% (g / ml) activated carbon for injection, stir at room temperature for 30 minutes, and filter; (8) use 0.45 μm and 0.22 μm microporous membran...

Embodiment 2

[0031] Example 2. Pinocerin reduces the exudation of Evan's blue dye in brain tissue during tPA thrombolysis in a rat intravascular thrombosis model of acute stroke.

[0032] Experimental materials: Sprague Dawley (SD) rats were purchased from Weitong Lihua (Beijing Weitong Lihua Experimental Animal Technology Co., Ltd.). tPA was purchased from Boehringer-Ingelheim, Germany. Pinocerin injection (10 mg) was provided by Wu Song's research group at the Institute of Materia Medica, Chinese Academy of Medical Sciences. When injecting, add 1 mL of normal saline for injection (Shijiazhuang Pharmaceutical No. 4 Factory), and use it at a dose of 10 mg / kg. The injections were protected from light and stored in a -20°C refrigerator.

[0033] SD rats with a body weight ranging from 250 to 300 g were anesthetized by intraperitoneal injection of chloral hydrate (350 mg / kg). The hair around the bregma was shaved, and the skin on the top of the head was cut to expose the bregma. Select 2 ...

Embodiment 3

[0040] Example 3. Pinocerin reduces hemoglobin exudation in brain tissue during tPA thrombolysis in a rat intravascular thrombosis model of acute stroke.

[0041] Animal modeling and administration methods are the same as in Example 2. The homogenate of the perfused brain tissue was taken and added with a hemoglobin stabilizer, the absorbance was detected at 575 nm, and the hemoglobin content in the brain tissue was calculated by substituting it into the standard curve. see results figure 2 , after injection of tPA, the blood content in rat brain tissue homogenate showed a rising trend. After the injection of pinocerin, the content of hemoglobin in the homogenate of bilateral brain tissue decreased significantly regardless of whether thrombolytic therapy was performed. Tip pinocerin can significantly reduce the bleeding caused by tPA.

[0042] Table 2. The effect of pinocerin (10mg / kg) on ​​the amount of hemoglobin exudation in the brain tissue after delaying 6h of tPA thr...

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Abstract

The invention discloses application of pinocembrin to preparation of anti-cerebral hemorrhage drugs. Cerebral hemorrhage includes transformational hemorrhage caused by the incidence of cerebral embolism, thrombolytic drugs and other factors. Experimental study finds that pinocembrin can alleviate hematopedesis of cerebral infarction areas after incidence of cerebral embolism in rats, can effectively alleviate hemorrhagic transformation during use of thrombolytic drugs, and significantly reduce the rat death phenomenon caused by cerebral hemorrhage. Pinocembrin can be used for preparation of drugs treating cerebral hemorrhage and hemorrhage caused by hemorrhagic transformation and the adverse effects of thrombolytic agents, relieve secondary hemorrhage of ischemic areas and improve prognosis of patients.

Description

technical field [0001] The present invention relates to the new application of pinocerine compound in drug preparation, mainly relates to the application of pinocerine in the preparation of cerebral hemorrhage side effects caused by treating hemorrhagic stroke and thrombolytic drugs, especially relates to the application of pinocerin in the preparation of Hemorrhagic transformation after the onset of cerebral embolism and the application of drugs in cerebrovascular accidents caused by thrombolytic drugs. Background technique [0002] Cerebral embolism refers to the blockage of cerebral arteries due to various factors such as various emboli in the blood (such as wall thrombus in the heart, atherosclerotic plaque, etc.) , causing ischemic necrosis of the brain tissue in the arterial blood supply area, and then focal neurological deficits. [0003] One of the key measures in the clinical treatment of cerebral embolism is to relieve vascular embolism and restore the blood suppl...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P7/04
CPCA61K31/352
Inventor 杜冠华马寅仲宋俊科李莉牛子冉吴松吕扬
Owner INST OF MATERIA MEDICA AN INST OF THE CHINESE ACAD OF MEDICAL SCI
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