A kind of preparation method and application of multivesicular liposome

A multivesicular liposome and lipid technology, which can be used in liposome delivery, pharmaceutical formulations, antibody medical components, etc., can solve problems such as the limitations of multivesicular liposome preparation

Active Publication Date: 2011-12-14
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] But people such as Kim in the prior art all rely on adopting L-lysine as emulsion stabilizer in the preparation technology of multivesicular liposome, make for the preparation of various different kinds of medicine multivesicular liposomes all be subject to limited to a certain extent

Method used

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  • A kind of preparation method and application of multivesicular liposome
  • A kind of preparation method and application of multivesicular liposome
  • A kind of preparation method and application of multivesicular liposome

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Raw material formula:

[0052]

[0053] Preparation of multivesicular liposomes:

[0054] (1) Dissolve the lipid with an organic solvent according to the above formula as the lipid phase; ultrasonically dissolve the active ingredient of the drug and the osmotic pressure regulator sucrose with an appropriate amount of hydrochloric acid solution (0.1mol / L), and set the volume to 5mL as the lipid phase. For the water phase, slowly add the inner water phase to the upper layer of the lipid phase; use a high-speed shear homogenizer to act on the resulting mixture at a speed of 10,000 rpm for 9 minutes to obtain W / O type colostrum;

[0055] (2) Add 20mL of the external aqueous phase containing 3.2g / 100mL osmotic pressure regulator glucose and 1g / 100mL auxiliary emulsifier polyvinylpyrrolidone to the upper layer of W / O colostrum, and act for 15 seconds at a speed of 4500rpm to prepare Obtain the double emulsion suspension of the water-in-oil-in-water type dichloromethane mi...

Embodiment 2

[0060] Raw material formula:

[0061]

[0062] Preparation of multivesicular liposomes:

[0063] (1) According to the above formula, the lipid is dissolved in an organic solvent as the lipid phase; the active ingredient of the drug and the osmotic pressure regulator sucrose are ultrasonically dissolved with an appropriate amount of citric acid solution (0.02mol / L), and the volume is adjusted to 5mL as the lipid phase. For the inner water phase, slowly add the inner water phase to the upper layer of the lipid phase; use a high-speed shear homogenizer to act on the resulting mixture at a speed of 10,000 rpm for 9 minutes to obtain W / O type colostrum;

[0064] (2) Add 20mL of the external water phase containing 6.0g / 100ml of osmotic pressure regulator glucose and 2.765g / 100ml of dextran to the upper layer of W / O colostrum, and act for 15 seconds at a speed of 4500rpm to obtain oil-in-water The double emulsion suspension of water-wrapped chloroform microspheres;

[0065] (3) ...

Embodiment 3

[0069] Raw material formula:

[0070]

[0071] Preparation of multivesicular liposomes:

[0072] (1) According to the above formula, dissolve the lipid with an organic solvent as the lipid phase; dissolve the active ingredient of the drug with an appropriate amount of phosphoric acid solution (0.2mol / L) ultrasonically, and set the volume to 5mL as the inner water phase, and the inner water The phase was slowly added to the upper layer of the lipid phase; the resulting mixture was acted on at a speed of 10,000 rpm for 9 minutes with a high-speed shear homogenizer to obtain W / O type colostrum;

[0073] (2) Add 60mL of the external aqueous phase containing 1.07g / 100mL osmotic pressure regulator glucose and 2.9mg / 100mL auxiliary emulsifier arginine to the upper layer of W / O colostrum, and act for 15 seconds at a speed of 4500rpm, The double emulsion suspension of water-in-oil-in-water type chloroform-ether microspheres was obtained;

[0074] (3) Inject the above-mentioned dou...

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Abstract

The invention relates to a multi-vesicular liposome, a blank multi-vesicular liposome and a preparation method and application thereof. The multi-vesicular liposome contains the following components in part by weight: 1 part of liposome, 0.01 to 20 parts of auxiliary emulsifier, 1 to 50 parts of osmotic pressure regulator and medicinal active ingredients; the medicament-to-lipid ratio of the multi-vesicular liposome is 1:(0.1-1):200; the lipid contains of a specific amount of neutral phospholipid, cholesterol and triglyceride; and the auxiliary emulsifier is selected from dextran, polyvinyl pyrrolidone, hydroxyethyl starch, gelatin, albumin, arginine and hydroxymethyl starch. The blank multi-vesicular liposome contains the following components in part by weight: 1 part of lipid, 0.01 to 20 parts of auxiliary emulsifier, 1 to 50 parts of osmotic pressure regulator and 0.1 to 50 parts of ion gradient regulator; the osmotic pressure of the in vivo water phase of the multi-vesicular liposome is equal to the osmotic pressure of human plasma; and the auxiliary emulsifier is as previously mentioned. The multi-vesicular liposome has high entrapment rate, and can achieve good sustained-release effect on in vivo and in vitro experiments.

Description

technical field [0001] The invention relates to a multivesicular liposome, a blank multivesicular liposome, a preparation method and application thereof. Background technique [0002] Kim et al. first discovered and studied multivesicular liposomes in 1983. They successfully prepared multivesicular liposomes by using phospholipids, cholesterol and neutral lipids as film-forming materials and using chloroform and ether as organic solvents by double emulsion method. Vesicular liposomes, and the microstructure of multivesicular liposomes was observed by light microscope and electron microscope. In the preparation process, the drug solution and the oil phase are firstly formed into water-in-oil (W / O) type colostrum under mechanical force, and then the colostrum is mixed with the external water phase to obtain double emulsion, and the organic matter is removed by drying with nitrogen gas. solvent to prepare multivesicular liposome suspensions. The average particle size of the m...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K45/00A61K38/00A61K38/14A61K39/00A61K31/7084A61K31/7088A61K47/26A61K47/32A61K47/36A61K47/42A61K47/16
Inventor 陆伟根陈亭亭徐成业杨耀杰虞丽芳
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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