Ginkgolide B sodium chloride injection and preparation method thereof

A technology of sodium chloride injection and ginkgolide, which is applied in the directions of blood diseases, pharmaceutical formulations, extracellular fluid diseases, etc., can solve the problems of short biological half-life, generally low yield, cumbersome methods, etc., and achieves good stability, Avoid phagocytosis and reduce the effect of toxic side effects

Inactive Publication Date: 2016-03-30
广东艾希德药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, ginkgolide B is an active ingredient of ginkgo for treating cardiovascular and cerebrovascular diseases, but its water solubility is poor and its biological half-life is short.
[0003] At present, the methods for the preparation and purification of ginkgolide B generally use organic solvent multistage extraction combined with silica gel adsorption chromatography, activated carbon adsorption chromatography and lead acetate precipitation method, etc., but the general yield is low and the method is cumbersome.

Method used

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  • Ginkgolide B sodium chloride injection and preparation method thereof
  • Ginkgolide B sodium chloride injection and preparation method thereof

Examples

Experimental program
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Effect test

preparation example Construction

[0055] A preparation method of ginkgolide B sodium chloride injection, the preparation method comprises the following steps:

[0056] 1) Extract Ginkgolide B:

[0057] a. Select fresh and dried ginkgo green leaves, dry them, remove impurities, crush them, extract with cycloalcohol, concentrate the extract under reduced pressure, and recover cycloalcohol; add water to the concentrated solution, precipitate for 20-25h, centrifuge, and take the supernatant for adsorption The column was first washed with water, then eluted with ethanol, and the eluate was collected and concentrated to obtain a concentrated extract;

[0058] b. Import the above-mentioned concentrated extract into the extraction tower, add ethyl acetate evenly from the bottom of the tower for countercurrent solvent extraction, collect different tower bodies separately; recover the extracted ethyl acetate extract to obtain a thick paste, concentrate to 20-25 degrees Baume, dried and pulverized to obtain crude ginkgo...

Embodiment 1

[0067] A kind of ginkgolide B sodium chloride injection, prepared by the following method:

[0068] 1) Extraction of Ginkgolide B:

[0069] a: Dry fresh and dried ginkgo green leaves at 70°C, remove impurities, pulverize, pass through a 60-mesh sieve, and extract twice with 60% cycloalcohol; each time for 1 hour, combine the extracts, concentrate under reduced pressure, and recover ethanol; Add 2 times the amount (volume) of water to the concentrated solution, precipitate for 24 hours, centrifuge, take the supernatant and put it on the HP-20 adsorption column, wash it with water first, then elute with 80% ethanol, collect the eluate, and concentrate;

[0070] b: The concentrated extract is introduced into the extraction tower, and ethyl acetate is evenly added from the bottom of the tower for countercurrent solvent extraction. The amount of ethyl acetate is 1.5 times the volume of the liquid, and the number of cycles is 4 times. Different tower bodies, Collect separately; rec...

Embodiment 2

[0077] A kind of ginkgolide B sodium chloride injection, prepared by the following method:

[0078] 1) Extraction of Ginkgolide B:

[0079] a: Dry the fresh and dried ginkgo green leaves at 65°C, remove impurities, pulverize, pass through a 55-mesh sieve, and extract twice with 60% cycloalcohol; each time for 1 hour, combine the extracts, concentrate under reduced pressure, and recover ethanol; Add 2 times the volume of water to the concentrated solution, precipitate for 20 hours, centrifuge, take the supernatant and put it on the HP-20 adsorption column, wash it with water first, then elute with 80% ethanol, collect the eluate, and concentrate;

[0080] b: The concentrated extract is introduced into the extraction tower, and ethyl acetate is evenly added from the bottom of the tower for countercurrent solvent extraction. The amount of ethyl acetate is twice the volume of the liquid, and the number of cycles is 5 times. Different tower bodies, Collect separately; recover the ...

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Abstract

The invention discloses a ginkgolide B sodium chloride injection and a preparation method thereof. The ginkgolide B sodium chloride injection is the injection which is formed by mixing ginkgolide B lipid nanoparticles with a 5% sodium chloride solution and has the mass concentration of 0.02%. The ginkgolide B lipid nanoparticles are prepared from, by weight, 0.4-0.5% of ginkgolide B, 0.3-0.5% of glycerin monostearate, 0.2-0.3% of intravenous injection soyabean lecithin, 0.5-1% of ethyl acetate, 0.3-0.5% of polyoxyethylene 100-stearate, 0.2-0.3% of glycerinum and the balance deionized water. The ginkgolide B sodium chloride injection is stable and reliable in performance, has the slow release effect, is few in toxic and side effect, and solves the problems that existing ginkgolide B is poor in water solubility and short in biological half life period.

Description

technical field [0001] The invention relates to the technical field of medical injections, in particular to a ginkgolide B sodium chloride injection and a preparation method thereof. Background technique [0002] Ginkgo biloba is the leaves of Ginkgo biloba, a plant of the genus Ginkgo, which mainly contains flavonoid glycosides and unique terpenes: flavonoid glycosides are mainly kaempferol and quercetin glucoside and rhamnoside; terpenes are mainly ginkgolides and Bilobalide. Ginkgolide is the fat-soluble active ingredient in Ginkgo biloba. It is a highly specific platelet activating factor (PAF) receptor antagonist. It has pharmacological effects such as increased permeability, and has been widely used clinically to treat diseases such as cardiovascular and cerebrovascular diseases. Among them, ginkgolide B is an active ingredient of ginkgo for treating cardiovascular and cerebrovascular diseases, but its water solubility is poor and its biological half-life is short. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K9/51A61K31/365A61K47/34A61P9/10A61P7/02A61K47/14A61K47/24
CPCA61K31/365A61K9/0019A61K9/08A61K9/5123A61K9/5146A61K2236/333A61K2236/39A61K2236/53A61K2236/55
Inventor 罗锦达罗清
Owner 广东艾希德药业有限公司
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