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Flavonoid compound and application thereof in preparation of pharmaceutical preparation

A flavonoid compound and a technology for preparing drugs are applied in the direction of drug combinations, antipyretics, anti-inflammatory agents, etc., and can solve the problems of poor water solubility of baicalin, which is not conducive to drug absorption, utilization, and preparation of pharmaceutical preparations, etc. Good sex and strong pharmacological activity

Inactive Publication Date: 2012-03-28
车庆明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Furthermore, the water solubility of baicalin is poor, which is not conducive to the absorption and utilization of medicine, and is also not conducive to the preparation of pharmaceutical preparations.

Method used

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  • Flavonoid compound and application thereof in preparation of pharmaceutical preparation
  • Flavonoid compound and application thereof in preparation of pharmaceutical preparation
  • Flavonoid compound and application thereof in preparation of pharmaceutical preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0203] One kilogram of baicalin was dissolved in 20 liters of fuming sulfuric acid, stirred at 80°C for 8 hours, neutralized with saturated sodium hydroxide, concentrated under reduced pressure, extracted with 20 liters of ethanol, and obtained a yellow powder product ( 0.9 kg).

[0204] The chemical structure identification data of the yellow powder product:

[0205]

[0206] 5,6,7-Trihydroxy, 8,3′-disulfonic acid flavone

[0207] Molecular weight: MW=430, molecular formula is C 15 h 10 o 11 S 2

[0208] Mass Spectrum: ESI-MS (negative ion mode): m / z 451[M-2H+Na]-, 429[M-H]-; Secondary Mass Spectrum: 429[M-H]-, 349[M-SO3H]-, 319, 181 .

[0209] NMR data: 1H-NMR (400MHz) and 13C-NMR (100MHz) data (DMSO-d6)

[0210]

[0211]

[0212]

[0213] Hydrocarbon long-range correlations (HMBC correlations) of compounds of the present invention

[0214] It is identified by the above spectroscopic method that the yellow powder product is 5,6,7-trihydroxy, 8,3'-disulfo...

Embodiment 2

[0216] 5,6,7-Trihydroxy, 8,3′-disulfoflavone injection:

[0217] Take 5000mg of 5,6,7-trihydroxyl, 8,3′-disulfonic acid flavone, dissolve it in 500ml of water to make an aqueous solution, adjust the pH to 5.5-6.5, heat to dissolve, mix well, and divide into 100mg / 10ml / branch of injection, sterilized by steam circulation for 30 minutes.

[0218] Usage and dosage: intramuscular injection or intravenous injection, 100-1000mg per day.

Embodiment 3

[0220] 5,6,7-trihydroxy, 8,3'-disulfonic acid flavone oral solution:

[0221] Dissolve 50,000mg of 5,6,7-trihydroxyl,8,3′-disulfonic acid flavone in 2,000ml of water to make a 2.5% aqueous solution, adjust the pH to 5.5-6.5, heat to dissolve, mix well, and fill in 10ml In the medicine bottle, seal and sterilize.

[0222] Method of administration: take orally, take 250-1500 mg of 5,6,7-trihydroxyl, 8,3′-disulfonic acid flavone daily.

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Abstract

The invention discloses a flavonoid compound and application thereof in preparation of a pharmaceutical preparation. The chemical name of the flavonoid compound is 5,6,7-trihydroxy,8,3'-disulfonyl flavone. The compound can be derived from baicalin by a chemical method. The compound disclosed by the invention has good effects of clearing heat, resisting viruses and resisting inflammation. The compound is prepared into a preparation for clearing heat, resisting virus and resisting inflammation, therefore a new pharmacy option is provided for resisting respiratory tract infection.

Description

technical field [0001] The present invention relates to a novel compound and its application, in particular to a flavonoid compound and its application in the preparation of pharmaceutical preparations. Background technique [0002] Flavonoids are a class of compounds that exist in nature and have the structure of 2-phenylchromanone. There is a ketone carbonyl group in their molecules, and the oxygen atom at the first position is basic and can form a salt with a strong acid. Baicalin is a flavonoid compound extracted from the traditional Chinese medicine Scutellaria baicalensis. It has antipyretic, antiviral, anti-inflammatory, antibacterial, diuretic, anti-allergic and antispasmodic effects, but its clinical efficacy is poor. Therefore, the pure baicalin raw material is rarely used as an antipyretic or antiviral or anti-infective drug at present. For example, baicalin capsules are used for adjuvant treatment of acute and chronic hepatitis and persistent hepatitis; and whe...

Claims

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Application Information

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IPC IPC(8): C07D311/30A61K31/352A61P29/00A61P31/04A61P31/12
Inventor 车庆明
Owner 车庆明
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