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Magnolol liposome and derivative preparation and preparation method thereof

A technology of magnolol lipid and lipid derivatives, applied in the field of medicine, can solve problems such as poor targeting, achieve the effects of uniform distribution, high encapsulation rate, and simple and easy preparation method

Inactive Publication Date: 2016-04-06
CHENGDU JINRUI FOUND BIOTECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ordinary liposomes are composed of phospholipids and cholesterol, but their targeting is poor. In order to improve the stability, targeting and intracellular introduction of liposomes, some functional groups can be used to modify the surface of liposomes, such as polyethylene glycol Alcohol chain-modified liposomes can prolong the time of drugs in blood circulation, so that liposomes can effectively reach the lesion site

Method used

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  • Magnolol liposome and derivative preparation and preparation method thereof
  • Magnolol liposome and derivative preparation and preparation method thereof
  • Magnolol liposome and derivative preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Embodiment 1 The embodiment of the present invention adopts thin film dispersion method and ethanol injection method to prepare liposome, investigates preparation method

[0046] 1, the specific implementation means of ethanol injection method is: accurately take magnolol, phosphatidylcholine, cholesterol, methoxy polyethylene glycol phosphatidylethanolamine by prescription quantity, stir and dissolve in the round bottom flask with dehydrated alcohol, Place in a water bath and heat at a constant temperature, and stir until the auxiliary materials are completely dissolved and evenly distributed. Another 5ml of ultrapure water was taken, heated, and the ethanol solution was vertically injected into the rapidly stirred ultrapure water. Continue to stir for 10 minutes after the injection is completed, remove absolute ethanol by rotary evaporation, and dilute to 5ml to obtain a 2mg / ml liposome solution.

[0047] 2, the specific implementation means of film dispersion method...

Embodiment 2

[0049] The screening test of embodiment two magnolol liposome formula of the present invention

[0050] .1 Preparation of liposomes

[0051] Through preliminary experiments, a method for preparing magnolol liposomes by ethanol injection was preliminarily established. The specific method is: accurately weigh magnolol, phosphatidylcholine, cholesterol, and mPEG with an analytical balance according to the prescription amount. 2000 -DSPE, stir and dissolve in a round bottom flask with 2ml of absolute ethanol, place in a water bath to keep heated at a constant temperature, and stir magnetically until the excipients are completely dissolved and evenly distributed. This process takes about 10-15 minutes. Another 5ml of ultrapure water was taken, heated, and the ethanol solution in which the excipients and drugs were dissolved was injected into the rapidly stirred ultrapure water. Continue to stir for 5 minutes after the injection is completed, remove absolute ethanol by rotary evap...

preparation example 1

[0083] Preparation and performance testing of liposome of the present invention in preparation example 1:

[0084] Prescription amount: magnolol, phospholipids, cholesterol and mPEG 2000 -The mass ratio of DSPE is: 10:30:4:1.5

[0085] Prepared by ethanol injection method: accurately weigh magnolol, phosphatidylcholine, cholesterol, mPEG with an analytical balance 2000 - DSPE, stir and dissolve in a round-bottomed flask with 2ml of absolute ethanol, place in a water bath to heat at a constant temperature, and stir magnetically until the excipients are completely dissolved and evenly distributed. This process takes about 10-15 minutes. Another 5ml of ultrapure water was taken, heated, and the ethanol solution in which the excipients and drugs had been dissolved was vertically injected into the rapidly stirred ultrapure water. Continue to stir for 5 minutes after the injection is completed, remove absolute ethanol by rotary evaporation with a rotary evaporator, and set the vol...

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Abstract

The invention belongs to the field of medicine, and particularly relates to magnolol liposome and a derivative preparation and a preparation method thereof. The liposome prepared by taking magnolol as an active ingredient is capable of improving storage stability of pharmaceutic preparations as well as allowing drugs in the liposome to release sustainably. The magnolol liposome comprises, by weight, 1 part of magnolol, 2.5-11 parts of phospholipid, 0.4-3 parts of cholesterol and 0.10-3 parts of hydrophilic lipid derivatives. The preparation method of the liposome is simple and easy to implement, and the liposome is controllable in quality and convenient for industrial production; the magnolol liposome is small in particle size, uniform in distribution and high in entrapment efficiency, storage stability of the pharmaceutic preparations can be improved, the drugs in the liposome are allowed to release sustainably, retention time of the drugs in blood circulation is prolonged, bioavailability of the drugs is heightened, and the high-efficiency long-acting treatment goal is met.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to a magnolol liposome and its derivative preparation and preparation method. Background technique [0002] Magnolia officinalis is the dry bark, root bark and branch bark of Magnoliaceae Magnolia plant in my country. It is used in traditional Chinese medicine to treat anxiety, cough, headache and allergic diseases. Due to its good neuroprotective effect, it is also used to treat mental diseases such as depression. Studies have shown that the hydroxylated biphenyl compound magnolol (magnolol) isolated from Magnolia officinalis has anti-inflammation, scavenging free radicals, reducing traumatic brain injury, and reducing acute lung injury. Studies have also shown that magnolol also has certain effects in anti-tumor, treatment of pulmonary edema, prevention of atherosclerosis, prevention of skin photoaging, inhibition of wrinkle formation, and anti-epilepsy. Although magnolol ha...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/05A61K47/24A61K47/28A61P29/00A61P39/06A61P25/00A61P11/00A61P35/00A61P7/10A61P9/10A61P17/16A61P25/08
CPCA61K9/127A61K31/05A61K47/24A61K47/28
Inventor 邱能沈贝莉莎安莲英刘俊达蔡帮军
Owner CHENGDU JINRUI FOUND BIOTECH CO LTD
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