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Quercetin long-acting liposome powder for injection and its preparing method

A technology of liposome powder and quercetin, which is applied in the direction of liposome delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problems of purification, quercetin pharmacological effects, chemical Modify the separation and other issues to achieve the effects of improving absorption and stability, prolonging blood circulation time, and improving pharmacokinetics

Inactive Publication Date: 2008-02-27
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the method of chemical modification affects the pharmacological effects of quercetin, and chemical modification has problems such as separation and purification.
Therefore, there is currently no suitable and economical way to use quercetin as a drug in clinical and industrial production.

Method used

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  • Quercetin long-acting liposome powder for injection and its preparing method
  • Quercetin long-acting liposome powder for injection and its preparing method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0076] Dissolve 60mg of lecithin, 6mg of cholesterol, 12mg of polyethylene glycol-phosphatidylethanolamine, the molecular weight of polyethylene glycol in polyethylene glycol-phosphatidylethanolamine is 2000, and 20mg of quercetin are dissolved in chloroform and methanol In 100ml of organic solvent, including 75ml of chloroform and 25ml of methanol, stir in a closed bottle until lecithin, cholesterol, polyethylene glycol-phosphatidylethanolamine and quercetin are completely dissolved, and place the completely dissolved solution in 250ml Connect the flask to a rotary evaporator, immerse the flask in a constant temperature water bath at 40°C, vacuum the rotary evaporation to remove the organic solvent, and form a uniform film on the wall of the flask, then put it into a vacuum drying oven, Dry at room temperature for 2 hours, add 100ml of sterilized water, ultrasonically disperse with an ultrasonic breaker, the power of the ultrasonic instrument is 200W, and the ultrasonic time i...

Embodiment 2

[0078] 0.50g lecithin, 0.10g cholesterol, 0.09g polyethylene glycol-phosphatidylethanolamine, the molecular weight of polyethylene glycol in polyethylene glycol-phosphatidylethanolamine is 3000, and 0.30g quercetin is dissolved in trichloro In 1L organic solvent of methane and methanol, the volume ratio of chloroform and methanol is v:v=1:1, stir in a closed bottle until lecithin, cholesterol, polyethylene glycol-phosphatidylethanolamine and quercetin Completely dissolve, put the completely dissolved solution in a 2.5L eggplant-shaped flask, connect the eggplant-shaped flask to a rotary evaporator, and immerse the flask in a constant temperature water bath at 30°C, vacuumize the rotary evaporation to remove the organic solvent, and form a circle on the wall of the flask Layer a uniform lipid film, then put it into a vacuum drying oven, dry it at room temperature for 2 hours, add 1L of sterilized water, and ultrasonically disperse it with an ultrasonic breaker, the ultrasonic po...

Embodiment 3

[0080] Dissolve 45mg of lecithin, 8mg of cholesterol, 8mg of polyethylene glycol-phosphatidylethanolamine, the molecular weight of polyethylene glycol in polyethylene glycol-phosphatidylethanolamine is 2000, and 35mg of quercetin are dissolved in chloroform and methanol 200ml In the organic solvent, the volume ratio of chloroform and methanol is v:v=4:1, and the volume is measured in milliliters or liters. Stir in a closed bottle until lecithin, cholesterol, polyethylene glycol-phosphatidylethanolamine Dissolve completely with quercetin, place the dissolved solution in a 500ml eggplant-shaped flask, connect the eggplant-shaped flask to a rotary evaporator, and immerse the flask in a constant temperature water bath at 35°C, and vacuum the rotary evaporation to remove the organic solvent. Form a uniform film on the surface, then put it into a vacuum drying oven, dry it at room temperature for 2 hours, add 200ml of sterilized water, and carry out ultrasonic dispersion with an ultr...

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Abstract

The present invention relates to a quercetin long-acting liposome powder injection and its preparation method. Said powder injection is formed from quercetin, polyethylene glycol-ethanolamine phosphoglycerides, lecithin, cholesterol and excipient. Said invention also provides the concrete steps of its preparation method.

Description

1. Technical field [0001] The invention relates to a quercetin long-acting liposome powder injection and a preparation method thereof, more specifically, relates to a liposome surface modified by polyethylene glycol-phosphatidylethanolamine (PEG-PE). Long-acting liposome, a quercetin long-acting liposome powder injection in which bioactive quercetin is encapsulated in long-acting liposomes and a preparation method thereof. 2. Background technology [0002] Quercetin (3,3,4,5,7-phentahydroxyflavone) and its derivatives are the most widely distributed flavonoids in the plant kingdom, widely present in edible vegetables and fruits such as mountain dregs, apples, onions, tea leaves, honey, grapes, etc. etc. (Frankel et al., 1993; Hertog et al., 1993, 1996) and various Chinese herbal medicines such as cypress leaves, galangal, coltsfoot, Sanqi, ginkgo, etc. (Formica JV et al., 1995). Quercetin also has the same basic structure as other flavonoids, which is composed of three ring...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K47/34A61K9/14A61K31/352A61P35/00A61P29/00A61P39/06A61P9/10A61K47/24
Inventor 魏于全范琳玉陈俐娟
Owner SICHUAN UNIV
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