Application of butylbenzene phthalein homolog in preparation of medicine for treating cerebral ischemia disease

A technology of butylphthalide and cerebral ischemia, applied in blood diseases, nervous system diseases, cardiovascular system diseases, etc., can solve problems such as unclear pharmacodynamic effects, and achieve the effect of improving neurological symptoms

Active Publication Date: 2005-11-02
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The ratio of prototype drug to metabolite in urine is about 9:91, and the ratio of metabolite to prototype drug in brain tissue is about 56:44. However, the metabolite in brain only has MI and no MII. Currently, the ratio of these two metabolites is The pharmacodynamic effect is not yet clear. Judging from the structures of the above two compounds, they both belong to butylphthalide homologues

Method used

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  • Application of butylbenzene phthalein homolog in preparation of medicine for treating cerebral ischemia disease
  • Application of butylbenzene phthalein homolog in preparation of medicine for treating cerebral ischemia disease

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Embodiment 1, MI and MII are on the influence of neurological symptoms caused by traumatic brain injury in rats

[0032] Experimental animals: male Wistar rats

[0033] Experimental method: use a conical metal object weighing 220g to drop freely from a height of 30cm, and hit the rat's left coronal suture posterior nuchal bone, causing traumatic brain injury in the rat. After 5 minutes, oral administration: MI and MII (20, 40, 80mg / kg), 24 hours later, scoring and evaluating behavioral changes.

[0034] Experimental results: rats with neurological symptoms caused by traumatic brain injury accompanied by cerebral ischemia, after oral administration, compared with the solvent control group, the MI group can significantly improve the neurological symptoms in a dose-dependent manner. Compared with the control group, P<0.05, indicating that the two metabolites MI and MII of butylphthalide can improve the neurological symptoms caused by cerebral ischemia caused by traumatic ...

Embodiment 2

[0035] Embodiment 2, the impact of MI and MII on memory impairment caused by focal cerebral ischemia

[0036] Experimental instrument: shuttle box, others are the same as in Example 1

[0037] Experimental animal is the same as embodiment 1

[0038] experimental method:

[0039] (1) Carry out learning and memory acquisition training to rats:

[0040] (2) Cerebral artery ligation: According to the Tamura method, rats were subjected to cerebral artery ligation. After 24 hours, the experiment of measuring the learning and memory of the rats was repeated, and the method was the same as (1).

[0041] (3) Grouping and administration: divided into 9 groups, normal group, sham operation group, ischemia control group, MI and MII (15, 30, 60 mg / kg) groups. Oral administration was performed 15 minutes after the operation, and the changes in the latent period of the active and passive avoidance reactions of the drug on the rats were observed 24 hours later.

[0042] Experimental resul...

Embodiment 3

[0043] The effect of embodiment 3, MI and MII on rat cerebral artery ligation cerebral edema

[0044] Experimental animal is the same as embodiment 1

[0045] Experimental method: The right middle cerebral artery was ligated to the rats to cause cerebral edema. After 15 minutes, MI and MII (20, 40, 80 mg / kg) were administered orally, and they were killed in 24 hours. Ww. After baking at 100°C for 24 hours, the dry weight was measured, and the water weight of the brain tissue was calculated by the dry-wet method. The tissue was nitrated for 4 hours, the pH value was adjusted with HCI, and the ion-selective electrode was connected to the oxygen tissue analyzer to measure the Na in the brain tissue + 、K + concentration.

[0046] Experimental results: MI group reduced brain water volume and Na + content, the increase of K+ content is very significant, and there is a dose-effect relationship; the MII middle and high dose group has a more obvious effect, compared with the blank...

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Abstract

The present invention relates to the application of butyl benzene phthalein homolog in preparing medicine for preventing and treating cerebral ischemic disease, resisting platelet aggregation and thrombus and preventing and treating dementia. The butyl benzene phthalein homolog is 3-(3'-hydroxy) butyl benzene phthalein or 3-hydroxy-3-butyl benzene phthalein.

Description

technical field [0001] The invention relates to the application of butylphthalide homologues in the preparation of drugs for preventing and treating cerebral ischemia, anti-platelet aggregation and anti-thrombosis, and treating and preventing dementia. Background technique [0002] Butylphthalide, also known as apigenin, was originally found in celery seeds. Its pharmacodynamic characteristics cover many aspects of effects: 1. It can improve the energy metabolism of ischemic brain; 3. Improve brain edema caused by local cerebral ischemia; 4. Significantly improve local cerebral blood flow and pia mater microcirculation in ischemic area; 5. Can significantly improve cerebral edema caused by local cerebral ischemia memory impairment. And less toxic side effects. In Chinese patent 93117148.2, the application of apigenin A in the preparation of drugs for preventing and treating diseases caused by cerebral ischemia in mammals or humans is disclosed. In ad...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/34A61K31/365A61P7/02A61P9/10A61P25/28
CPCA61K31/34A61P7/02A61P9/10A61P25/28
Inventor 刘振涛张宏武申东民冯小龙王荣端孙经国
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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