Process for extracting ginkgolide, ginkgolide injection and process for preparing same

A technology of ginkgolide and extraction process, which is applied in the direction of blood diseases, medical formulas, and extracellular fluid diseases, etc. It can solve the problems of low solubility of ginkgolide, high cost of extraction process, and low content of effective substances, and achieve the solution of water solubility. problems, eliminate cross-contamination, and simplify operations

Active Publication Date: 2005-03-16
HEILONGJIANG ZBD PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the current extraction process of ginkgolides has high cost, low yield, and low content of effective substances, and because ginkgolides have low solubility in water, it is difficult to make high-concentration injections, which limits its effective application.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] The extraction process of ginkgolide: take 100g of ginkgo biloba and pulverize, add 4 times the amount of 70% acetone liquid warm immersion extraction, the temperature is 30 ℃, leaching for 5 hours, stirring once every 10 minutes, filtering to obtain filtrate I. Continue to add 4 times the amount of 70% acetone solution to the dregs for warm extraction at a temperature of 30° C., extract for 1 hour, and filter to obtain filtrate II. Continue adding 3 times the amount of medicinal residues to 70% acetone solution for warm extraction at a temperature of 30°C for 1 hour, and filter to obtain filtrate III, discarding medicinal residues. Combine three extracts, recover acetone to about 1 / 4 of the total volume, and place it. Filter the above-mentioned concentrated solution and use petroleum ether (30 ° C, the dosage is 2: 1) to remove impurities 4 times, the aqueous phase is extracted 3 times with ethyl acetate (the dosage is 2: 1); the ethyl acetate solution is 8% sodium ace...

Embodiment 2

[0037] The extraction process of ginkgolide: take 200g of ginkgo biloba and pulverize, add 7 times the amount of 50% acetone liquid warm immersion extraction, the temperature is 40 ℃, leaching for 6 hours, stirring once every 10 minutes, filtering to obtain filtrate I. Continue to add 5 times the amount of 50% acetone solution to warm the dregs for extraction at 40°C for 1 hour, and filter to obtain filtrate II. Continue to add 3 times the amount of 50% acetone solution to extract the dregs, temperature is 40°C, extract for 1 hour, filter to obtain filtrate III, and discard the dregs. Combine three extracts, recover acetone to about 1 / 4 of the total volume, and place it. Filter the above-mentioned concentrated solution and use petroleum ether (120 ° C, the dosage is 3: 1) to remove impurities 5 times, and the aqueous phase is extracted 4 times with ethyl acetate (the dosage is 3: 1); the ethyl acetate solution is 10% sodium acetate solution ( The dosage is 3:1) to wash, recov...

Embodiment 3

[0039] The extraction process of ginkgolide: take 200g of ginkgo biloba and pulverize, add 5 times the amount of 60% acetone liquid warm immersion extraction, the temperature is 50 ℃, leaching for 8 hours, stirring once every 10 minutes, filtering to obtain filtrate I. Continue to add 5 times the amount of 60% acetone solution to warm the dregs for extraction at a temperature of 50° C., extract for 2 hours, and filter to obtain filtrate II. Continue to add 4 times the amount of 60% acetone solution to warm the dregs for extraction at a temperature of 50°C for 2 hours, filter to obtain filtrate III, and discard the dregs. Combine three extracts, recover acetone to about 1 / 4 of the total volume, and place it. Filter the above concentrated solution and use cyclohexane (amount of 3:1) to remove impurities 3 times, and extract the aqueous phase with ethyl acetate (amount of 3:1) twice; ethyl acetate solution with 15% sodium acetate solution (amount of 3:1) washing, recovering ethy...

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PUM

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Abstract

The invention discloses a process for extracting ginkgolide, ginkgolide injection and process for preparing same, wherein the extracting process consists of disintegrating the ginkgo leaves, leaching by diluted acetone solution, recovering acetone, removing impurities, extracting and purifying with acetic ether, removing impurities with sodium acetate again, reclaiming acetic ether, recrystallizing in ethanol or methanol, filtering, low temperature drying, solubilizing the bilobalide with hydroxypropyl-beta-cyclodextrin to obtain the bilobalide injection.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and in particular relates to a ginkgolide extraction process, ginkgolide injection and a preparation method thereof. Background technique [0002] Finding potent PAF (platelet activating factor) antagonists has been one of the major directions of new drug research since the 1980s. PAF participates in many pathophysiological processes in the body, and has a wide range of functions and great activity. It has been found that PAF plays an important role in pathological processes such as thrombosis, asthma, organ transplant rejection, acute inflammation, cardiac allergy, and shock caused by endotoxin. In the study of PAF antagonists, ginkgolides screened from natural products are the most active and most evaluated natural products. Pharmacological and clinical studies also show that ginkgolides are the most advanced PAF antagonists. Among them, ginkgolide B has the strongest selec...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/365A61P7/02A61P29/00A61P37/06A61P37/08A61P39/06C07D493/22
Inventor 曹庆先楼凤昌丁峰周勤阎政冯志英
Owner HEILONGJIANG ZBD PHARMA
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