Paclitaxel liposome and preparation method thereof

A liposome and paclitaxel technology, applied in the field of paclitaxel liposome and its preparation, can solve the problems of poor water solubility

Active Publication Date: 2020-11-20
SHANGHAI GINSOME PHARMATECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But all do not have patent or document openly to report about the long circulation liposome that takes ginsenoside as membrane material
[0008] And the lipophilic section of ginsenoside Rg3 and Rh2 only contains a double bond, water solubility is poor, soluble in methanol, ethanol, insoluble in ether, chloroform (see International Journal of Pharmaceutical Research, June 2017, the 6th phase of volume 44 " Research progress on dosage forms of ginsenoside Rg3")

Method used

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  • Paclitaxel liposome and preparation method thereof
  • Paclitaxel liposome and preparation method thereof
  • Paclitaxel liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0140] The preparation of embodiment 1 common Rg3 liposome

[0141] Add 1g of egg yolk lecithin, 0.1g of cholesterol, and 0.1g of ginsenoside 20(S)-Rg3 (without micronization treatment) into 20mL of absolute ethanol, and stir at room temperature to form a clear solution. In a constant temperature water bath at ℃, remove the organic solvent by rotary evaporation, and form a film, add 20mL of 5% trehalose aqueous solution (the stated percentage refers to the percentage of the quality of trehalose in the total mass of trehalose aqueous solution), and sonicate until the liposome particles 0.1-0.3 micron, pass through a microporous membrane of 0.22 micron to obtain an aqueous solution containing ginsenoside Rg3 liposome, and then put the solution in a vial. Put the above aqueous solution into a freeze dryer to freeze dry for 72 hours, pass through a protective gas (argon or nitrogen), seal it, and obtain the common ginsenoside Rg3 liposome. After testing, the D10 of the liposome w...

Embodiment 2

[0142] The preparation of embodiment 2Rg3 blank liposome

[0143] Add 1g of egg yolk lecithin and 0.1g of superfine powdered ginsenoside 20(S)-Rg3 into 200mL of chloroform, stir at room temperature to form a clear solution, and remove the organic solvent by rotary evaporation in a constant temperature water bath at 40-50°C. To form a film, add 20mL of 5% trehalose aqueous solution (the percentage refers to the percentage of the quality of trehalose in the total mass of trehalose aqueous solution), sonicate until the liposome particles are at 0.1-0.3 microns, and pass through a 0.22 micron microporous membrane , to obtain an aqueous solution of blank liposomes containing ginsenoside Rg3, and then the solution is divided into vials. Put the above aqueous solution into a freeze dryer to freeze dry for 72 hours, pass through a protective gas (argon or nitrogen), seal it, and obtain the ginsenoside Rg3 blank liposome. After testing, the D10 of the liposome was 66nm, the D50 was 90...

Embodiment 3

[0144] The preparation of embodiment 3Rg5 blank liposome

[0145] By the same method as in Example 2, Rg3 was replaced by Rg5 to prepare Rg5 blank liposomes. After testing, the D10 of the liposome was 70nm, the D50 was 96nm, and the D90 was 111nm.

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Abstract

The invention discloses a paclitaxel liposome and a preparation method thereof. The invention provides a liposome loaded with an active substance. The liposome comprises a blank liposome with ginsenoside as a membrane material shown in formula I and the active substance, wherein the active substance is paclitaxel; and the blank liposome has a membrane which contains a lipid substance and ginsenoside as shown in formula I. The paclitaxel liposome provided by the invention has the characteristics of good film-forming property, encapsulation efficiency, targeting property, long cycle, stability,safety and uniformity, and the preparation process is simple.

Description

[0001] This application is a divisional application of the invention patent application CN111228219A (the application date is 2018.11.29, the application number is 2018114472434, and the invention name is a blank liposome with ginsenoside Rg3 or its analogue as the membrane material, its preparation method and application) . technical field [0002] The invention relates to a paclitaxel liposome and a preparation method thereof. Background technique [0003] Liposome is a targeted drug carrier, which belongs to a new dosage form of targeted drug delivery system. It can embed drug powder or solution in microparticles with a diameter of nanometers. This kind of microparticles is similar to the bilayer microvesicles of the biological membrane structure. The distribution of the drug in the body makes the drug mainly accumulate in the target tissue, thereby improving the therapeutic index of the drug, reducing the therapeutic dose of the drug and reducing the toxicity of the dru...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/28A61P35/00
CPCA61K47/28A61K31/337A61P35/00A61K9/1271A61K9/1277A61K9/127A61K31/4745A61K33/243A61K31/704A61K45/06C07B63/04C07J17/005
Inventor 王建新洪超朱颖夏加璇王丹陈颖江詹华杏
Owner SHANGHAI GINSOME PHARMATECH CO LTD
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