Compound for treating cardiocerebral vascular disease and its preparing method and its use in pharmaceutical field

A technology for cardiovascular and cerebrovascular diseases and compounds, which is applied in the field of compounds for treating cardiovascular and cerebrovascular diseases and their preparation and application in the pharmaceutical field, and can solve problems such as unsatisfactory results

Inactive Publication Date: 2006-01-04
车庆明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] In order to seek more ideal drugs of the same kind, people hav

Method used

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  • Compound for treating cardiocerebral vascular disease and its preparing method and its use in pharmaceutical field
  • Compound for treating cardiocerebral vascular disease and its preparing method and its use in pharmaceutical field
  • Compound for treating cardiocerebral vascular disease and its preparing method and its use in pharmaceutical field

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The preparation of compound trihydroxyethyl quercetin of the present invention:

[0055] One kilogram of troxerutin was dissolved in 30 liters of water, 0.3 kg of glucoside hydrolase was added, and stirred at 50°C for 4 days, filtered, the precipitate was washed with water and dried to obtain trihydroxyethyl quercetin (0.6 kg) .

[0056] Identification of Trihydroxyethylquercetin: Mass Spectrum FAB-MS: m / z 435 (M+1) + ; C NMR spectrum 13 CNMR (DMSO-d 6 ): 146.7(C-2), 136.7(C-3), 176.2(C-4), 160.4(C-5), 98.0(C-6), 164.6(C-7), 92.7C-8), 156.3 (C-9), 104.1 (C-10), 123.4 (C-1′), 113.2 (C-2′), 148.1 (C-3′), 150.4 (C-4′), 113.2 (C- 5'), 122.0 (C-6'), 70.9, 70.6, 70.4 (O-CH2X3), 59.7, 59.6, 59.4 (-CH2X3). .Proton NMR spectrum 1 H-NMR (DMSO-d 6 ): 12.41(s, 1H, OH-5), 9.65(s, 1H, OH-3), 7.82(d, 1H, J=8.41Hz, H-6'), 7.81(s, 1H, H-2 '), 7.16 (d, 1H, J=8.71Hz, H-5), 7.15 (s, 1H, H-8), 6.34 (s, 1H, H-6), 4.08 (m, 6H, O-CH2 -), 3.89 (m, 6H, -CH2-). Ultraviolet Spectrum (MeO...

Embodiment 2

[0058] Trihydroxyethyl quercetin liquid:

[0059] Dissolve 5000mg trihydroxyethyl quercetin in 1000ml water to make a 0.5% aqueous solution, heat to dissolve, mix evenly, put into 20ml medicine bottle, seal and sterilize. Dosage: Take orally, take trihydroxyethyl quercetin 100-300mg daily.

Embodiment 3

[0061] Trihydroxyethyl Quercetin Injection:

[0062] Take 2000 mg of trihydroxyethyl quercetin, dissolve it in 1000 ml of water to make an aqueous solution, heat to dissolve, mix evenly, dispense into injections with a concentration of 20 mg / 10 ml / cartridge, and steam for 30 minutes to sterilize.

[0063] Usage and dosage: intramuscular injection or intravenous injection, 50-100mg per day.

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Abstract

The compound for treating cardiac and cerebral vascular diseases is triethoxyl quercetin. The preparation process includes the following steps: A. hydrolyzing Troxerutin as material with beteroside hydrolase through stirring at 30-70 deg c for 3-5 days; and B. filtering, water washing the precipitate and drying. Triethoxyl quercetin has pharmacological activity obviously superior to Troxerutin. Different forms of medicine may be prepared with the compound as active component for preventing and treating cardiac and cerebral vascular diseases and cerebral apoplexy.

Description

technical field [0001] The present invention relates to a compound, its preparation method and its application in the field of pharmacy. Background technique [0002] Troxerutin is a drug commonly used clinically for the treatment of cardiovascular and cerebrovascular diseases. It is a synthetic product of rutin and ethylene oxide. Its chemical structure is as follows: [0003] [0004] Clinical application shows that troxerutin has the effects of increasing blood flow in brain and coronary vessels, reducing vascular resistance, anti-platelet and red blood cell aggregation, and reducing blood viscosity. Its clinical curative effect is better. [0005] In order to seek more ideal drugs of the same kind, people have been conducting research on similar compounds, but nothing has been achieved. Contents of the invention [0006] One of the objects of the present invention is to provide a compound A with better effect than troxerutin. [0007] The second object of the p...

Claims

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Application Information

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IPC IPC(8): C07D311/30C12P17/06A61K31/352A61P9/10
Inventor 车庆明
Owner 车庆明
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