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Composition taking high-purity ginkgolide B as active ingredient and preparation method thereof

A technology of ginkgolide and composition, which is applied in the field of composition and preparation thereof with high-purity ginkgolide B as the active ingredient, and can solve the problem of low purity and cannot be used for the preparation of ginkgolide B injection, ginkgolide B The purity is not high enough, the ginkgolide B monomer is difficult, etc., to achieve good effectiveness, safety and quality controllability, improve bioavailability, and improve the effect of drug safety

Active Publication Date: 2013-06-12
GUANGZHOU BOJI MEDICINE SERVICES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] At present, the medicinal ginkgolide B is mainly extracted from Ginkgo biloba, but because the content of Ginkgolide B in Ginkgo biloba is extremely low, and Ginkgolide B and Ginkgolide K, ginkgolic acid and bilobalide co-exist , the structures of ginkgolide B and ginkgolide K are very similar, and the polarity difference is very small. It is difficult to extract high-purity ginkgolide B monomer from ginkgo leaves, especially the combination of ginkgolide B and ginkgolide The separation of K is more difficult
The purity of the ginkgolide B extracted in the above-mentioned patents and the prior art is not high enough, and the solubility of the ginkgolide B is poor, so it can only be used as a raw material for oral administration and cannot be used as a raw material for injections, and the bioavailability of oral administration The drug effect of ginkgolide B is relatively low, and the efficacy of ginkgolide B cannot be fully exerted. The use of injections can greatly improve its bioavailability, and the clinically applicable population-patients with ischemic encephalopathy, including patients with acute ischemic stroke and cerebral infarction, have a treatment time window Narrow, and need to take effect quickly, generally oral preparations have a slower onset of action than injections, but after administration of injections, the onset of action is rapid. In addition, patients with ischemic encephalopathy may have difficulty swallowing oral drugs, but injections do not. difficulty swallowing
But the injection has very high requirements on the purity of ginkgolide B, and the ginkgolide B crude drug in the prior art cannot be used for the injection of preparing ginkgolide B because of low purity

Method used

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  • Composition taking high-purity ginkgolide B as active ingredient and preparation method thereof
  • Composition taking high-purity ginkgolide B as active ingredient and preparation method thereof
  • Composition taking high-purity ginkgolide B as active ingredient and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] Preparation of Ginkgolide B Extract:

[0058] Add 40g of diatomite to 750ml of ethyl acetate under stirring conditions, then add 50g of ginkgo biloba extract, heat and reflux at 60°C for 3.5 hours, filter, concentrate, and concentrate the filtrate to a liquid-solid ratio of 5ml: 1g; Add about 1 / 10 of the volume of distilled water to the concentrated solution to remove impurities, separate the ethyl acetate layer, and pass the ethyl acetate layer through an acidic alumina column. The diameter-to-height ratio of the acidic alumina column is 1:4, and the alumina is 200 mesh. The weight ratio of sample loading to alumina is 1:7, elute with saturated ethyl acetate at a rate of 1 / 4BV / h, and collect the eluate; the eluate is concentrated under reduced pressure until there is no ethyl acetate smell, Add an appropriate amount of ethanol to dissolve it, add water until the alcohol content is 60%, let it stand still, precipitate the crude crystals, filter, take the crude crystals,...

Embodiment 2

[0060] Preparation of Ginkgolide B Extract:

[0061] Add 40g of diatomaceous earth to 1000ml of ethyl acetate under stirring conditions, then add 50g of ginkgo biloba extract, heat and reflux at 73°C for 2 hours, filter, concentrate, and concentrate the filtrate until the liquid-solid ratio is 4ml: 1g; Add about 1 / 9 volume of distilled water to the solution to remove impurities, separate the ethyl acetate layer, and pass the ethyl acetate layer through an acidic alumina column. The diameter-to-height ratio of the acidic alumina column is 1:4, and the alumina is 200 mesh. The weight ratio of sample volume to alumina is 1:7, elute with water-saturated ethyl acetate, the elution rate is 1 / 4BV / h, collect the eluate; the eluate is concentrated under reduced pressure until there is no ethyl acetate smell, add Appropriate amount of ethanol to dissolve it, add water until the alcohol content is 60%, let it stand still, precipitate the crude crystals, filter, take the crude crystals, a...

Embodiment 3

[0063] Preparation of Ginkgolide B Extract:

[0064] Add 60g of diatomaceous earth to 850ml of ethyl acetate under stirring conditions, then add 50g of ginkgo biloba extract, heat and reflux at 70°C for 2.5 hours, filter, concentrate, and concentrate the filtrate until the liquid-solid ratio is 3ml:1g; Add about 1 / 11 volume of distilled water to the solution to remove impurities, separate the ethyl acetate layer, and pass the ethyl acetate layer through an acidic alumina column. The diameter-to-height ratio of the acidic alumina column is 1:10, and the alumina is 300 mesh. The weight ratio of the sample volume to alumina is 1:10, elute with saturated ethyl acetate with water, the elution rate is 1 / 2BV / h, collect the eluate; the eluate is concentrated under reduced pressure until there is no ethyl acetate smell, add Appropriate amount of ethanol to dissolve it, add water until the alcohol content is 70%, let it stand still, precipitate the crude crystals, filter, take the crude...

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Abstract

The invention relates to a composition taking high-purity ginkgolide B as an active ingredient. The composition is a ginkgolide B injection. The ginkgolide B injection comprises the following pharmaceutical active ingredients in parts by weight: 20 parts of ginkgolide B extract, 580-630 parts of polyethylene glycol-400, 770-830 parts of glycerol and 640-700 parts of ethanol, wherein the ginkgolide B extract is extracted from ginkgo leaves, and comprises ginkgolide B and ginkgolide K, the content of the ginkgolide B is more than 99%, and the content of the ginkgolide K is less than 0.6%. In a ginkgolide B composition provided by the invention, the ginkgolide B in the ginkgolide B extract as a raw medicine has a high purity, and the content of the ginkgolide K is extremely low, so that requirement of the injection on the raw medicine is met and the bioavailability of the raw medicine and the medication safety of patients are improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition with high-purity ginkgolide B as an active ingredient and a preparation method thereof. Background technique [0002] Ginkgolide B, English name Ginkgolide B; molecular formula: C 20 h 24 o 10 ; Molecular weight: 424.40; Structural formula is: [0003] [0004] Ginkgolide B is a highly active platelet activating factor (PAF) antagonist, which can competitively bind to the PAF receptor and inhibit the action of PAF; therefore, any diseases related to PAF, such as: thrombosis, cerebral Ginkgolide B has a certain curative effect on tissue damage, organ transplant rejection, acute inflammation, cardiac allergy, cellular endotoxin and shock caused by IgG. [0005] But so far, there are no preparations with a single component of ginkgolide B as a raw material on the market both at home and abroad. According to the chemical drug registration classifica...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/365A61K47/34A61P9/00A61P9/10A61P7/02A61P25/00A61P37/06A61P29/00A61P9/02
Inventor 李明华王广明宋良伟王军
Owner GUANGZHOU BOJI MEDICINE SERVICES
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