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Apramycin liposome and preparation method thereof

A technique of apramycin lipid and apramycin, which is applied in the field of apramycin liposome and its preparation, can solve the problems of large particle size, small action force, easy agglomeration and the like of the liposome, and achieves a small particle size. , avoid oxidation, overcome the effect of easy agglomeration

Active Publication Date: 2014-02-12
HENAN SOAR VETERINARY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the problem at this stage is that due to CO 2 The polarity of water is very different, and the force between the two molecules is very small, directly in the supercritical CO 2 It is very difficult to disperse the liposome membrane material in water in the medium, and the obtained liposome has a large particle size and is easy to agglomerate

Method used

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  • Apramycin liposome and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Weighed 3.75 g of phosphatidylcholine, purchased from Shanghai Boao Bioengineering Company, analytically pure, lot number BA20121206; cholesterol 1.25 g, provided by Shanghai Bioengineering Company, analytically pure, lot number BA20121125; apramycin 0.25 g, Zhengzhou Furuikang Chemical Products Co., Ltd., batch number 120115; dissolve the weighed phosphatidylcholine, cholesterol and apramycin in 13mL of absolute ethanol, mix well to obtain a mixed solution, and place the resulting mixed solution in CO 2 Fluid reactor, capped.

[0032] Poloxamer 188 was dissolved in PBS phosphate buffer solution with pH 7.2 to prepare 100 mL of a stabilizer solution with a mass concentration of Poloxamer 188 of 5%, and the prepared stabilizer solution was placed in CO 2 Fluid collector, capped.

[0033] open CO 2 Cylinder, CO 2 After the gas is cooled into a liquid by a refrigerator, it is pressurized by a high-pressure metering pump and enters the CO 2 Fluid Reactor, CO 2The te...

Embodiment 2

[0045] Weigh 6 g of phosphatidylcholine, purchased from Shanghai Boao Bioengineering Company, analytically pure, batch number BA20121206; 0.2 g of apramycin, Zhengzhou Furuikang Chemical Products Co., Ltd., batch number 120115; Alkali and apramycin were dissolved in 15mL ethanol (aqueous solution with a mass fraction of 20%), mixed evenly to obtain a mixed solution, and the resulting mixed solution was placed in CO 2 Fluid reactor, capped.

[0046] Poloxamer 188 and Tween 80 were dissolved in PBS phosphate buffer solution of pH 7.2 to prepare 100 mL of a stabilizer solution. The mass concentrations of Poloxamer 188 and Tween 80 in the stabilizer solution were both 5%. The prepared stabilizer solution was placed in CO 2 Fluid collector, capped.

[0047] Open CO 2 Cylinder, CO 2 After the gas is cooled into a liquid by a refrigerator, it is pressurized by a high-pressure metering pump and enters the CO 2 Fluid Reactor, CO 2 The temperature of the fluid reactor is controll...

Embodiment 3

[0050] Weigh 6 g of phosphatidylcholine, purchased from Shanghai Boao Bioengineering Company, analytically pure, batch number BA20121206; 0.6 g of apramycin, Zhengzhou Furuikang Chemical Products Co., Ltd., batch number 120115; Alkali and apramycin were dissolved in 20mL ethanol (90% aqueous solution), mixed evenly to obtain a mixed solution, and the resulting mixed solution was placed in CO 2 Fluid reactor, capped.

[0051] Dissolve poloxamer 188 and alkyl diphenyl ether sulfonate (DAS) in PBS phosphate buffer at pH 7.2 to prepare 100 mL of stabilizer solution. In the stabilizer solution, poloxamer 188, alkyl diphenyl ether sulfonate The mass concentration of phenyl ether sulfonate (DAS) was 5%, and the prepared stabilizer solution was placed in CO 2 Fluid collector, capped.

[0052] Open CO 2 Cylinder, CO 2 After the gas is cooled into a liquid by a refrigerator, it is pressurized by a high-pressure metering pump and enters the CO 2 Fluid Reactor, CO 2 The temperature...

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Abstract

The invention discloses an apramycin liposome. The apramycin liposome is a composition with a spherical or ellipsoidal double-film structure, and is formed by encapsulating apramycin with a liposome film. A preparation method comprises the following steps: 1) dissolving the apramycin and the liposome film with ethanol to obtain a mixed solution, and dissolving the mixed solution into supercritical CO2 to obtain a supercritical solution, wherein the mass ratio of the apramycin to the liposome film is (1 : 1) to (1 : 30); the liposome film is phosphatidylcholine, or a mixture of phosphatidylcholine and cholesterol; 2) dissolving a stabilizer into an aqueous medium to obtain a stabilizer solution; 3) spraying the supercritical solution to the stabilizer solution at an expansion pressure of 15-30MPa and a pre-expansion temperature of 323-343K, dispersing and precipitating to obtain an apramycin liposome suspension.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to an apramycin liposome and a preparation method thereof. Background technique [0002] Apramycin is a fat-soluble substance, which has poor dissolution in the body and low bioavailability, resulting in short administration time and small area, which affects the administration effect. Therefore, it is very necessary to make it into a new dosage form with good water solubility, fast absorption, liver targeting effect, long-acting and controlled release. Liposome is an ultrafine particle drug carrier preparation prepared by encapsulating drugs in lipid bilayers with phospholipids, cholesterol, etc. as membrane materials. Liposomes have the function of targeting and moving. When entering the body, they are preferentially taken up by tissues rich in reticuloendothelial cells, such as liver, spleen, and bone marrow. According to the characteristics of liver organ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7036A61K47/34A61K47/26A61K47/20A61J3/00
Inventor 孙江宏管倩杨震豪
Owner HENAN SOAR VETERINARY PHARMA
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