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High purity aescine B bulk drug, its preparation method and medical application

A technique for aescin and an API, applied in the field of medicine, can solve the problems of lack of production feasibility, high risk of environmental pollution, low preparation efficiency, etc., and achieves stable and controllable quality, no risk of environmental pollution, and simple processing technology. Effect

Inactive Publication Date: 2012-10-24
TIANJIN INSTITUTE OF PHARMA RESEARCH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the most commonly used method is to use preparative high-performance liquid chromatography to separate, but this method has low preparation efficiency, and uses acetonitrile and other reagents with high cost and high risk of environmental pollution, so it is not feasible for production

Method used

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  • High purity aescine B bulk drug, its preparation method and medical application
  • High purity aescine B bulk drug, its preparation method and medical application
  • High purity aescine B bulk drug, its preparation method and medical application

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Aescin total saponins crude product 1g, add distilled water 10ml to dissolve, pass through the chromatographic column equipped with 30g C-18 alkyl bonded phase silica gel (30-50μm), with methanol (30%): 5mM ammonium acetate solution (70%): The mobile phase was eluted with 0.1% acetic acid, and the fractions containing aescin B were collected. Concentrate the fractions under reduced pressure at 40°C, remove all the methanol, dilute with 1 times the volume of the concentrated liquid, and place it at 10°C. A white powder precipitate precipitates, and the precipitate is filtered, washed repeatedly with cold distilled water, and dried to obtain seven Phylloside B (purity 96%).

Embodiment 2

[0028] Aescin total saponin crude product 1g, add distilled water 10ml to dissolve, pass through the chromatographic column equipped with 60gC-18 alkyl bonded phase silica gel (30-50μm), with methanol (35%): 5mM ammonium acetate solution (65%): The mobile phase was eluted with 0.1% acetic acid, and the fractions containing aescin B were collected. Concentrate the fractions under reduced pressure at 45°C, remove all methanol, and place at 4°C to precipitate a white powdery precipitate, which is filtered, washed repeatedly with cold distilled water, and dried to obtain aescin B (purity 98%).

Embodiment 3

[0030] Aescin total saponins crude product 1g, add distilled water 20ml to dissolve, pass through the chromatographic column equipped with 80g C-18 alkyl bonded phase silica gel (30-50μm), with methanol (40%): 5mM ammonium acetate solution (60%): The mobile phase was eluted with 0.5% acetic acid, and the fractions containing aescin B were collected. Concentrate the fractions under reduced pressure at 50°C, remove all methanol, place at 10°C, a white powder precipitate precipitates, filter the precipitate, wash repeatedly with cold distilled water, and dry to obtain aescin B (purity 95%).

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Abstract

Belonging to the field of medicinal technologies, the invention particularly relates to a high purity aescine B bulk drug, its preparation method and application as anti-inflammatory exudation and edema bulk drugs. The bulk drug provided in the invention has the advantages of simple preparation process, environmental protection, controllable quality, stronger activity than existing aescine drugs, good safety, and good application prospects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a high-purity aescin B crude drug, a preparation method and medical application thereof. Background technique [0002] Aescin is a triterpene saponin mixture containing polyester bonds extracted from the traditional Chinese medicine Aesculus chinesis Bge and other dried and mature fruits of Aesculus. It has anti-inflammatory, anti-exudation, enhanced venous tone, neuroprotective properties 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 marketed. In my country, total aescin is made into injections in the form of its sodium salt, and its indications are cerebral edema, swelling caused by trauma or surgery, and venous reflux disorders. Clinical studies have confirmed that aescin sodium has a high therapeuti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J63/00C07H15/256C07H1/08A61K31/704A61P29/00A61P7/10
Inventor 韩英梅赵娜夏夏广萍王玉丽
Owner TIANJIN INSTITUTE OF PHARMA RESEARCH
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