Cardiovascular/cerebral and ophthalmological medicines, and preparation and use thereof

A cardio-cerebrovascular and ophthalmology technology, applied in the field of cardio-cerebrovascular and ophthalmic drugs and their preparation, to achieve the effect of easy storage and transportation, and good fluidity

Active Publication Date: 2010-12-29
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, there is no published literature that only reports puerarin [8-β-D-glucopyranose-4′, 7-dihydroxyisoflavone, molecular formula: C 21 h 20 o 9 , Molecular weight: 416.37,

Method used

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  • Cardiovascular/cerebral and ophthalmological medicines, and preparation and use thereof
  • Cardiovascular/cerebral and ophthalmological medicines, and preparation and use thereof
  • Cardiovascular/cerebral and ophthalmological medicines, and preparation and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of Puerarin Monohydrate In a reaction vessel, 80 g of dried Pueraria root powder was extracted 3 times with 400 ml of ethanol 80% aqueous solution, and the extracts were combined, coarsely filtered, and then filtered with a 0.22 μm microporous membrane, and the filtrate was concentrated , to obtain Pueraria root extract, add water, adjust PH=3-5 with dilute hydrochloric acid, then adjust PH between 6-7 with sodium bicarbonate solution, filter, then use n-butanol and isohexanone as solvents to extract, and the extract is evaporated Dry to obtain a solid, use water, methanol, formic acid, and acetonitrile as crystallization solvents, recrystallize three times, filter, wash with water, and dry the solid at about 80°C for 4 hours to obtain 1.8g of off-white crystalline powder; melting point: 208.4~212.5°C decomposition (uncorrected), UV spectrum: λ CH3OH max 250nm, [a] D 21 +18.14°C (c=1, methanol), ESI-MS: m / z: 417[M+1] + ;Infrared Spectrum: v KB...

Embodiment 2

[0049] Example 2 Preparation of Puerarin Crystal Hydrate Add 30 g of puerarin extract or total flavonoids of puerarin, add water, heat to about 50-70°C, filter through a 0.15-0.24 μm ceramic membrane, pass the filtrate through a neutral alumina chromatography column, and elute , D101 macroporous resin adsorption, washing with water, TLC monitoring, and then eluting with 30-75% ethanol aqueous solution until the elution is complete, filtering, concentrating under reduced pressure, standing still, using water, acetone, ethanol, acetonitrile as crystals Solvent, recrystallized twice, left to stand, filtered, washed with water, and dried the obtained solid; dried at about 80°C for 4-6 hours to obtain 6.6 grams of off-white solid, melting point: 227.8-231.8°C (uncorrected), UV spectrum: lambda CH3OH max 250nm; [a] D 21 +18.14°C (c=1, methanol), ESI-MS: m / z: 417[M+1] + ;Infrared Spectrum: v KBr max cm -1 3380, 1626, 1586, 1516, 1446; Karl Fischer's method measures moisture t...

Embodiment 3

[0050] Example 3 Preparation of Puerarin Monohydrate 90g of dried kudzu root powder of about 40 mesh, add 400ml of water, ultrasonically and reflux extraction 3 times, combine the extracts, coarse filter, and then filter through a 0.22 μm microporous membrane or ceramic membrane, The filtrate is then between 25-65°C, under 0.15-2MPa (the pressure can be dynamically adjusted, or the pressure difference can be increased as the test progresses), and an ultrafiltration membrane (polysulfone hollow fiber membrane module with a molecular weight cut-off of 4000-50000) is used , fiber pore diameter 0.011μm, internal diameter is 1.1mm) filtration, the filtrate is filtered through the nanofiltration membrane with a molecular weight cut-off of more than 200, concentrated, dissolved with 90% methanol aqueous solution, add acetic acid and acetonitrile as the crystallization solvent, place, crystallize, pump Filter and wash with water; as above, recrystallize 3 times with methanol, water, ac...

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PUM

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Abstract

The invention relates to cardiovascular/cerebral and ophthalmological medicines-puerarin crystalline hydrate for the treatment of high blood pressure, coronary heart disease, cerebral infarction, cerebral thrombosis and sequela thereof, cerebral circulation improvement, vertebral-basilar insufficiency vertigo, post-deep venous thrombosis syndrome, diabetes, diabetes complication, diabetic nephropathy, diabetic peripheral neuropathy, diabetic retinopathy, retinal artery ostruction, retinal vein obstruction, sudden hearing loss, glaucoma and other diseases, and further relates to preparation and use thereof; the derivative has excellent storage stability and is suitable for the use of preparing the medicines for the prevention and the treatment of cardiovascular/cerebral diseases and ophthalmological diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides cardiovascular and cerebrovascular and ophthalmic medicines and their preparation and application. Background technique [0002] At present, there is no published literature that only reports puerarin [8-β-D-glucopyranose-4′, 7-dihydroxyisoflavone, molecular formula: C 21 h 20 o 9 , Molecular weight: 416.37, CAS: 3681-99-0], so far, there is no published literature at home and abroad to report puerarin crystalline hydrate [C 21 h 20 o 9 · n H 2 O, n=0.8~1.3] and its preparation method and application. Contents of the invention [0003] What the present invention relates to is reported to be used for hypertension, coronary heart disease, pulmonary heart disease, heart failure, angina pectoris, myocardial infarction, cardiogenic shock, arrhythmia, myocarditis, ischemic encephalopathy, cerebral infarction, cerebral thrombosis and its sequelae, Improve cerebral cir...

Claims

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Application Information

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IPC IPC(8): A61K31/352A61P9/00A61P27/02A61P7/02A61P3/10A61P13/12A61P3/06C07D407/04
Inventor 刘力
Owner 刘力
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