Composition of aescine derivative and salt thereof, preparation method and medical uses thereof

A technique for aescin and derivatives, applied in the field of medicine, can solve problems such as difficult adverse reactions, and achieve the effects of strong industrial production practicability, high yield and mild reaction conditions

Active Publication Date: 2012-12-05
南京星银药业集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The technical routes disclosed in these invention patents all improve the vascular irritation of aescin in the form of organic alkali-salt complexes, but the active and toxic substances in the composition have basically not changed, and it is difficult to fundamentally avoid the existing adverse reactions

Method used

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  • Composition of aescine derivative and salt thereof, preparation method and medical uses thereof
  • Composition of aescine derivative and salt thereof, preparation method and medical uses thereof
  • Composition of aescine derivative and salt thereof, preparation method and medical uses thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] (1) Preparation of aescin derivative composition (QYY):

[0040] Aescin extract (total aescin content 15%) 10g, add water to dilute to an extract: solution ratio of 1:100W:V, add 15g of β-glycosidase to dissolve, adjust the pH of the solution to 5.0, at 55℃ Enzymatic hydrolysis at constant temperature for 72 hours, filtration, the filtrate is adsorbed by 200ml macroporous adsorption resin, eluted with 2 column volumes of water, 1 column volume of 10% ethanol solution, and finally eluted with 75% ethanol for 2 column volumes , Collect 75% ethanol eluate, concentrate under reduced pressure until there is no alcohol smell, see white precipitation, filter to get the precipitate, then reconstitute with 70% ethanol, filter, and concentrate the filtrate until the solution begins to become turbid. Place it for crystals to precipitate. QYY crystals (white amorphous powder) are obtained by filtration.

[0041] (2) Preparation of arginine salt of QYY: 0.4g of QYY, 0.07g of arginine, a...

Embodiment 2

[0043] (1) Preparation of aescin derivative composition (QYY):

[0044] Aescin extract (total aescin content 70%) 2g, add 100ml of medicinal ethanol to dissolve, add water to dilute to an extract: medicinal solution ratio of 1:500W:V, add 30g β-glucosidase to dissolve, adjust the solution The pH value is 6.0, enzymatically digested at 40℃ for 24 hours, filtered, the filtrate is adsorbed by 100ml D101 macroporous adsorption resin, and eluted with 1 column volume of water, 2 column volumes of 15% ethanol solution, and finally 85% ethanol Elute 2 column volumes, collect the 85% ethanol eluate, concentrate under reduced pressure until there is no alcohol smell, and wait for a white precipitate to precipitate. The precipitate is filtered, reconstituted with ethanol, filtered, and the filtrate is concentrated until the solution begins to become turbid. Place it for crystal precipitation and filter to obtain pure QYY (white needle-like powder).

[0045] (2) Preparation of lysine salt of ...

Embodiment 3

[0048] Aescin extract (total aescin content 40%) 5g, dilute with water to extract: drug solution ratio of 1:800W:V, add 80g cellulase, 40g β-glucosidase to dissolve, adjust the pH value of the solution It is 4.5, enzymatically digested at 55℃ for 48 hours, filtered, and the filtrate is adsorbed by 500ml D101 macroporous adsorption resin, and eluted with 2 column volumes of water, 2 column volumes of 20% ethanol solution, and finally eluted with 70% ethanol 2 column volumes, collect the 70% ethanol eluate, concentrate under reduced pressure until there is no alcohol smell, and wait for a white precipitate to precipitate. The precipitate is filtered, reconstituted with methanol, filtered, the filtrate is concentrated until the solution becomes turbid, and the crystals are left to precipitate, filtered to obtain crystals, and then recrystallized with methanol-water to obtain pure QYY (white needle-like powder).

[0049] Preparation of monomer components:

[0050] 1g of pure QYY produ...

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PUM

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Abstract

The invention provides an aescine derivative composition and a salt thereof, and a preparation method and medicinal uses. According to the present invention, the composition belongs to a biological enzyme hydrolysis product of escin, and provides strong anti-inflammatory and anti-edema activities compared with the aescine, hemolysis safety is good, the preparation process has strong industrial production executability, and the composition can be used for developments of anti-inflammatory drugs and anti-edema drugs.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a new aescin derivative and its salt composition, its preparation method and medical use. Background technique [0002] Aescin is a mixture of triterpene saponins containing polyester bonds extracted from the traditional Chinese medicine Aesculus chinesis Bge and the dried and mature fruits of other plants in the Aesculus family. It has anti-inflammatory, anti-exudation, strengthening of vein tension, and neuroprotection. And so on. Its medicinal use originated in Germany and was later promoted in Japan, my country and other countries. At present, preparations including intravenous injections, tablets, and external use have been on the market. In my country, total aescinate is made into injections in the form of its sodium salt. The indications are cerebral edema, swelling caused by trauma or surgery, and venous reflux disorders. Clinical studies have confirmed that sod...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61P29/00A61P7/10C12P33/00C07J63/00C07H15/256
Inventor 韩英梅夏广萍赵娜夏王玉丽刘巍
Owner 南京星银药业集团有限公司
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