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Cardiovascular disease treating medicament and preparation method and application thereof

A technology for treating drugs and cardiovascular and cerebrovascular, which is applied in the field of medicine to achieve the effects of good sliding property, good water solubility, and easy storage and transportation.

Active Publication Date: 2012-03-21
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, published literature only reports that scutellarin (C 21 h 18 o 12 .CAS No.: 27740-01-8, Molecular Weight: 462.37), so far, there is no published literature at home and abroad to report scutellarin crystal hydrate C 21 h 18 o 12 ·nH 2 O, n=1.7~2.2] and its preparation method and use

Method used

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  • Cardiovascular disease treating medicament and preparation method and application thereof
  • Cardiovascular disease treating medicament and preparation method and application thereof
  • Cardiovascular disease treating medicament and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Preparation of scutellarin 1.75 crystalline hydrate In an extraction tank, 2 kg of scutellaria scutellaria whole herb dry powder of about 40 mesh was refluxed and extracted 3 times with 200 ml of methanol, 12 L of ethanol, and 2 L of water as a mixed solvent. Filter and combine the extracts, then filter with a 0.45-1μm microporous membrane, then filter with an ultrafiltration membrane with a molecular weight cut-off of 10,000 to 30,000, concentrate the filtrate until almost alcohol-free, and then adjust the diluent with sodium bicarbonate solution The pH is about 7.2, filter, the filtrate is passed through D101 macroporous adsorption resin, washed with water, the eluate is collected, filtered, the filtrate is adjusted to pH = 2-3 with dilute phosphoric acid, and left to stand until the precipitate is fully separated, filtered, used for precipitation Wash with water until near-neutral, then wash with ethanol and chloroform, filter with suction, recrystallize the...

Embodiment 2

[0044] Example 2 Preparation of scutellarin dihydrate In an extraction tank, 4 kg of scutellaria scutellaria whole herb dry powder of about 40 mesh was refluxed for 3 times with 32 L of ethanol and 4 L of water as a mixed solvent, filtered, and the extracts were combined, and the filtrate Concentrate until there is almost no alcohol, dilute with water, adjust the pH of the diluted solution to about 7.5 with sodium carbonate solution, filter with a 0.2-1μm ceramic membrane, absorb the filtrate with D101 macroporous resin, wash with water, collect the eluate, filter, and filtrate Use acetic acid to adjust pH=2~3, let it stand still, wait for the precipitate to be fully analyzed, filter, wash the precipitate with water until nearly neutral, then wash with ethanol and chloroform, and filter with suction, dilute the obtained solid with water, add sodium carbonate solution under stirring to make It is dissolved, and the pH of the diluent is adjusted to about 7.5, and the ultrafiltrat...

Embodiment 3

[0045] Example 3 Preparation of scutellarin dihydrate In an extraction tank, 2 kg of scutellaria whole herb dry powder of about 40 meshes was fully wetted with 3 L of 80% ethanol, and ultrasonically extracted with 16 L of ethanol and 3 L of water as a mixed solvent. Once, the extracts were combined, coarsely filtered through a filter cloth, and then filtered with a 0.45 μm microporous membrane, using an ultrafiltration membrane with a molecular weight cut-off of 10,000 to 30,000 (polysulfone hollow fiber membrane module, fiber pore diameter of about 0.011 μm, inner diameter of about 1.1 mm) to filter, concentrate the filtrate under reduced pressure until almost alcohol-free, dilute with water, adjust the pH of the diluted solution to about 7.5 with sodium carbonate solution, filter, absorb with D101 macroporous resin, wash with water, collect the eluate, and filter , the filtrate was adjusted to pH=2~3 with acetic acid, left to stand until the precipitate was fully separated, f...

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Abstract

The invention relates to a medicament for treating or preventing coronary disease, angor pectoris, myocardial infarction, arrhythmia, ischemic brain disease, cerebral thrombosis, cerebral hemorrhage and sequelae thereof, vascular dementia and peripheral circulation disturbance disease, including various artery occlusions, vasculitis, and microcirculatory disturbance caused by diabetes mellitus, high blood pressure, hyperlipidemia and hyperviscosity as well as refractory neck syndrome, vertebrobasilar artery insufficiency and other ischemic diseases accompanying with microcirculatory disturbance, namely, a scutellarin derivative and preparation and application thereof. The derivative has high storing stability, and is suitable for preparing a medicament for treating or preventing heart cerebrovascular diseases.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, it provides a cardiovascular and cerebrovascular therapeutic drug—scutellarin derivatives and its preparation method and application. Background technique [0002] Scutellarin exists in the traditional Chinese medicine breviscapine. From a pharmacological point of view, scutellarin can improve microcirculation, increase cerebral blood flow, and improve the permeability of the blood-brain barrier; improve blood rheology, reduce whole blood viscosity, and resist Significant platelet aggregation, promote fibrinolytic activity, reduce fibrinogen, prevent thrombolysis; prevent intracellular calcium overload and extracellular excitatory amino acid accumulation, inhibit protein kinase C displacement activation or excessive activation, reduce brain edema, delay Ischemic brain cell death, increase nutritional myocardial blood flow, improve myocardial microcirculation, and have a certain ef...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61P9/00A61P9/10A61P9/06A61P7/02A61P9/12A61P3/06A61P43/00C07H17/07C07H1/08
Inventor 刘力
Owner 胡梨芳
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