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Application of senkyunolide I to medicaments for prevention and treatment of cerebral apoplexy and relevant treatment during convalescence

A technique for yangchuanxiong lactone and cerebral apoplexy, which is applied in the field of new medical use of yangchuanxiong lactone I, and can solve problems such as reducing aggregation

Inactive Publication Date: 2011-08-10
SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are still few reports on its pharmacological effects at present, and it is only found that it can reduce the deformable damage of ConA-induced erythrocytes and reduce its aggregation (Shi Zhen Guoyi Guoyao, 2003, 14 (12): 738-739.); Calcium influx in cardiomyocytes and human neuroblastoma (Clin Exp Pharmacology Physion, 1999, 26: 845-846.)
There are no reports or patents on its activity in anti-cerebral ischemia and protection of traumatic brain tissue

Method used

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  • Application of senkyunolide I to medicaments for prevention and treatment of cerebral apoplexy and relevant treatment during convalescence
  • Application of senkyunolide I to medicaments for prevention and treatment of cerebral apoplexy and relevant treatment during convalescence
  • Application of senkyunolide I to medicaments for prevention and treatment of cerebral apoplexy and relevant treatment during convalescence

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0021] Embodiment 1, alcohol extraction method prepares chuanxiong lactone I

[0022] Chuanxiong decoction pieces 1kg, after removing impurities, crushed into powder, 70% ethanol 10L 90 ℃ reflux extraction twice, each time 2 hours, combined extracts, recovered about 8L of solvent to obtain 2L of extract A (equivalent to crude drug 0.5g·ml -1 ). Extract A solution 5000r·min -1 Centrifuge for 15 min, and take the supernatant (the floating oil in the upper layer is discarded). 240g of HPD-100 macroporous resin (equivalent to 80g of dry resin) was wet-packed, the extract A solution was loaded, and the adsorption flow rate was about 0.7L h -1 . After the sample was loaded, it was washed with 3.5 L of distilled water until it was nearly colorless, and then 1.4 L was eluted with 50% 7 alcohol, the alcohol eluate was collected, and the solvent was recovered to obtain extract B. Dissolve extract B in 500ml of distilled water to obtain an aqueous solution of extract B, extract with ...

Embodiment 2

[0023] Embodiment 2. The preparation of Liguscaractone I tablet

[0024] Ingredients Amount per Tablet

[0025] Ligustilide I 100mg

[0026] Microcrystalline Cellulose 37.45mg

[0027] Micronized silica gel 10.5mg

[0028] Stearic acid 17.5mg

[0029] Lactose 10.5mg

[0030] Magnesium Stearate 1.05mg

[0031] According to the prescription quantity, add Ligusticolide I (prepared according to the method of Example 1) into microcrystalline cellulose, micropowder silica gel, stearic acid, lactose and mix evenly to make granules, add magnesium stearate, mix evenly, and press into tablets , That is, (each tablet contains chuanxionglide I 0.1g). The recommended oral dosage for adults is 1-4 tablets / time, 2-3 times a day.

Embodiment 3

[0032] Embodiment 3. The preparation of Yangchuanxiong lactone I capsule

[0033] Ingredients Amount Per Capsule

[0034] Ligustilide I 100mg

[0035] Microcrystalline Cellulose 37.45mg

[0036] Micronized silica gel 10.5mg

[0037] Stearic acid 17.5mg

[0038] Lactose 10.5mg

[0039] Add microcrystalline cellulose, micropowder silica gel, stearic acid, lactose to Ligusticolactone I (prepared by the method of Example 1) according to the prescription amount, and mix evenly, after making granules, fill into No. 0 hard capsule shell, beat Light that is the system (each capsule containing chuanxiong lactone I 0.1g). The recommended oral dosage for adults is 1-4 capsules / time, 2-3 times a day.

[0040] The present invention will be further illustrated by the test example and the pharmacological activity test and results of Ligustilide I below.

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Abstract

The invention discloses new medicinal application of senkyunolide I shown in a structural formula (I). In the application, the influence of the senkyunolide I on the cerebral blood flow change of rats in a reperfusion model of local cerebral ischemia caused by middle cerebral artery occlusion (MCAO) of the rats and a kalium chloratum (KCL) induced rat cortical spreading depression model is studied by adopting an animal model, and pharmacological results prove that the senkyunolide I can improve the cerebral blood flow of the rats after MCAO molding obviously and can restore and exceed the original cerebral blood flow formed before modeling quickly after reperfusion so as to play a certain role in cerebral protection. In addition, the senkyunolide I can resist the condition that cerebral blood flow descends due to KCL-induced rat local cerebral vasoconstriction, so the senkyunolide I can be used for preparing medicaments for the prevention and treatment of cerebral apoplexy and relevant treatment during convalescence.

Description

technical field [0001] The invention relates to the technical fields of traditional Chinese medicine chemistry and medicine, in particular to a new medical application of senkyunolide I extracted and prepared from Ligusticumchuanxiong Hort. Background technique [0002] Chuanxiong (Ligusticum chuanxiong Hort.) is a plant of the genus Ligusticum in the family Umbelliferae, and its medicinal part is the rhizome. Chuanxiong is a traditional Chinese medicine in my country. It has the effects of promoting blood circulation and promoting qi, dispelling wind and relieving pain. It was listed as a top grade in the Eastern Han Dynasty "Shen Nong's Materia Medica", and it is a commonly used traditional Chinese medicine for treating depression and migraine. [0003] Phthalides are a class of compounds present in Rhizoma Chuanxiong, which have been shown to be active in cardiovascular, blood and smooth muscle. Among them, butylphthalide, which has been studied more, has many activities...

Claims

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Application Information

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IPC IPC(8): A61K31/365A61P9/10
Inventor 梁爽冯怡徐德生阮克锋王硕
Owner SHANGHAI ZHANGJIANG ENG RES CENT OF MODERN PREPARATION TECH OF TRADITIONAL CHINESE MEDICINE
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