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Application of Myricetin Crystal Compounds in Nervous Inhibitor Drugs

A technology of crystal compounds and compounds, applied in drug combinations, nervous system diseases, cosmetic preparations, etc., can solve problems such as undiscovered

Inactive Publication Date: 2015-12-02
WEST CHINA HOSPITAL SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, so far, other more efficient and precise targets and mechanisms of myricetin have not been found. After long-term research by the inventors, it has been found that myricetin has a certain inhibitory effect on neural activity.

Method used

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  • Application of Myricetin Crystal Compounds in Nervous Inhibitor Drugs
  • Application of Myricetin Crystal Compounds in Nervous Inhibitor Drugs

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Example 1: Preparation of myricetin crystal compound

[0013] Take 100g of a commercially available oxymycin compound, put the weighed compound into an agate grinding body in a fume hood, grind it thoroughly to make it evenly mixed, and then put the sample into a platinum crucible. In order to make the post-reaction go smoothly, put it into a box furnace for pre-calcination and grinding at 80°C. Finally, keep the temperature at 80° C. for 2 hours, and after slowly cooling to room temperature in stages, massive crystals are obtained at the bottom of the crucible.

[0014] Dissolve the blocky crystals obtained above in anhydrous acetone, stir at room temperature for several minutes until the solid is completely dissolved, then add 5% aqueous sodium hydroxide solution dropwise, the reaction solution changes from light yellow clear liquid to wine red clear liquid, and the reaction is complete , Rotary evaporation to remove acetone, add hot water to the raffinate until the...

Embodiment 2

[0015] Example 2: Inhibitory effect of myricetin and its crystals on neural activity

[0016] In Table 1, the in vitro potency [inhibiting the binding of [35S]-tert-butylbicyclic glucothioate (TBPS)] of the compound and its crystal was compared, and the rotating rod TD50 (half of the test animals could not rotate The dose when the rod remains on the rod for 1 minute) and the length of time before all test animals are able to pass the rotarod test (duration of action). These methods for measuring the in vitro and in vivo activity of the compounds of the invention are fully disclosed in US Patent No. 5,232,917. The TBPS assay yields the in vitro potency of the compound, while the rotarod assay evaluates the sedative / hypnotic activity of the compound. Since the duration of action of the compounds is dose dependent and will be prolonged at higher doses, the duration of action was measured at the lowest dose at which all animals failed the rotarod test. For compounds with a dur...

Embodiment 3

[0019] Example 3: Granule preparation

[0020] formula:

[0021] Myricetin crystal compound 2000g

[0022] Sucrose 5000g

[0023] Dextrin 400g

[0024] Appropriate amount of ethanol

[0025] Granulate according to common granulation method, pack into 1000 bags (about 7.4g per bag), each bag contains myricetin 2000mg.

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Abstract

The invention relates to an application of a myricetin crystal compound to a medicament of a nerve inhibitor, and in particular relates to the application of the myricetin crystal compound in the field of narcotics.

Description

technical field [0001] The invention relates to the application of myricetin in nerve inhibitor drugs, specifically the application of myricetin in the field of anesthetics. Background technique [0002] Myricetin (Myricetin), as shown in (I), is a natural compound of flavonols, yellow needle-like crystals, melting point is 324.0-325.5 °C, soluble in methanol, ethanol, acetone or ethyl acetate, slightly soluble in water, hardly Soluble in chloroform and petroleum ether, easy to oxidize and turn green in the air. [0003] [0004] (I) [0005] At present, myricetin has been extensively studied in pharmacology. Flavonoid natural products have become a hot spot in the research and development of natural medicines and human health products in recent years. With multiple functions, scientists began to study the use of myricetin in medicine, food, health care products and cosmetics. Foreign health products and American health products FYI have used myricetin as an additive t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/352A61K8/49A61P25/00A61P23/00
Inventor 吕小兰
Owner WEST CHINA HOSPITAL SICHUAN UNIV