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Bilobalide injection and preparation method thereof

A technology for ginkgolide and injection, which is applied in the directions of pharmaceutical formulations, antidote, cardiovascular system diseases, etc., can solve the problems of low solubility of ginkgolide, high extraction process cost, low content of effective substances, etc., so as to solve the problem of water solubility. problems, eliminate cross-contamination, and simplify the effect of operation

Inactive Publication Date: 2005-11-23
江苏吴中苏药医药开发有限责任公司 +1
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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

[0036] 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

[0038] 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

[0040] 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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Abstract

The invention relates to a bilobalide injection and preparation process, wherein the preparation process comprises charging hydroxypropyl-beta-cyclodextrin into water for injection, stirring to dissolve, charging bilobalide, stirring and heating to dissolve, charging chelating agent, stirring and dissolving, charging activated charcoal and straining, charging water for injection for constant volume, refining and split charging, hot-pressed sterilization.

Description

[0001] This application is a divisional application. The filing date of the original application is June 30, 2004, the application number is 200410041120.2, and the name of the invention is "Ginkgolide Extraction Technology and Ginkgolide Injection and Its Preparation Method". technical field [0002] 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 [0003] 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 th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365
Inventor 曹庆先楼凤昌丁峰周勤阎政冯志英
Owner 江苏吴中苏药医药开发有限责任公司
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