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Stabilized liposome

A liposome, stable technology, applied in the field of liposomes that can be administered orally, can solve problems such as poor stability and poor targeting function, and achieve the effect of improving appearance

Inactive Publication Date: 2007-02-21
天津未名生物医药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For those drugs with a long gastric emptying time, if the gastric emptying time is not significantly shortened after being prepared into liposomes, the stability and targeting function of this preparation will be very poor

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0069] The preparation method of the liposome of the present invention will be described below.

[0070] The liposome preparation method adopted in the present invention can be prepared by conventional methods, for example, referring to Lu Bin, "New Drug Formulation and New Technology" People's Medical Publishing House, April 1998: 107-164 pages, can adopt injection method or phospholipid Liposomes were prepared by directly dispersing with a suitable concentration of phosphate buffer system.

[0071] When the injection method is used, the lipid and fat-soluble substances are dissolved in an organic solvent to form a transparent and uniform solution, and then injected at a constant speed into the water phase (buffer solution containing water-soluble drugs) at a constant temperature above the boiling point of the organic solvent. Stir to evaporate the organic solvent, then emulsify or sonicate to obtain liposomes. Injection method commonly used solvents are ether, ethanol and s...

Embodiment 1

[0108] Embodiment 1: Preparation 1 of liposome

[0109] Weigh 4.75 g of disodium hydrogen phosphate 12 hydrate, 0.52 g of sodium dihydrogen phosphate dihydrate, 3.00 g of sorbitol, 1.50 g of β-cyclodextrin, and 1.04 g of PEG-2000, and dissolve them in 180 ml of water.

[0110] Weigh 14.09 grams of phospholipids and 1.61 grams of vitamin E, and dissolve them in 30 ml of absolute ethanol. A homogeneous and transparent ethanol solution of phospholipids is formed.

[0111] Place the aqueous solution in a three-necked flask, heat it in a water bath at 60°C, and stir at the same time to balance the internal and external temperatures. After the temperature is balanced, the phospholipid-ethanol solution is continuously and slowly added to the aqueous solution through a constant flow pump. Preparation of liposomes.

[0112] Air and part of ethanol in the system were removed by rotary evaporation. Afterwards, add pure water to adjust the volume of the system to 200mL.

[0113] Afte...

Embodiment 2

[0114] Embodiment 2: Preparation 2 of liposome

[0115] Weigh 8.91 g of disodium hydrogen phosphate 12 hydrate, 1.06 g of sodium dihydrogen phosphate dihydrate, 6.04 g of sorbitol, 3.02 g of β-cyclodextrin, and 2.03 g of PVP, and dissolve them in 400 ml of water.

[0116] Weigh 35.12 grams of phospholipids and 3.05 grams of vitamin E, and dissolve them in 72 ml of absolute ethanol. A homogeneous and transparent ethanol solution of phospholipids is formed.

[0117] Place the aqueous solution in a three-necked flask, heat it in a water bath at 60°C, and stir at the same time to balance the internal and external temperatures. After the temperature is balanced, the phospholipid-ethanol solution is continuously and slowly added to the aqueous solution through a constant flow pump. Preparation of liposomes.

[0118] The air and part of ethanol in the system were removed by rotary evaporation, and then supplemented with pure water to adjust the volume of the system to 400mL.

[0...

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PUM

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Abstract

A stabilized liposome resisting against both acidic and alkaline environments and suitable for oral taking features that the polyhydroxy substances are used to stabilized the membrane of liposome.

Description

technical field [0001] The present invention relates to a stabilized liposome, more specifically, to a liposome that is stable to an acidic environment and an alkaline environment, and further relates to a liposome that can withstand gastric juice or more acidic conditions and can also be stable in the intestinal tract Orally administrable liposomes. The present invention specifically uses polyol-stabilized liposomes. The liposomes have acid resistance and can be stabilized in an artificial gastric juice environment for more than 2 hours, preferably more than 5 hours, and at the same time stable for more than 24 hours in a weakly alkaline environment. Oral administration facilitates the administration route of liposomes. Background technique [0002] Liposome pharmaceutical preparations are preparations based on amphoteric substances such as phospholipids, and encapsulate active pharmaceutical substances in the middle of a thin film formed by a lipid bilayer or in a hollow ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127
Inventor 张磊石正国李得月梁凤玲
Owner 天津未名生物医药有限公司
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