A kind of fluticasone furoate liposome suspension and preparation method thereof

A technology of fluticasone furoate and fluticasone furoate, which is applied in the directions of liposome delivery, pharmaceutical formulation, liquid delivery, etc., can solve problems such as limitations, and achieve the effects of high encapsulation rate, favorable drug absorption, and simple operation.

Active Publication Date: 2021-06-29
SHANGHAI ANOVENT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, in clinical practice, nebulizers are widely used in the inhalation administration of water-soluble drugs, however, the application of inhalation administration of water-insoluble drugs is limited.

Method used

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  • A kind of fluticasone furoate liposome suspension and preparation method thereof
  • A kind of fluticasone furoate liposome suspension and preparation method thereof
  • A kind of fluticasone furoate liposome suspension and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Preparation of 10ml liposomes

[0032] Total initial volume = 100ml,

[0033] Ethanol content 30%, lipid composition: DPPC / cholesterol (molar ratio is 1: 1),

[0034] Initial lipid = 0.3 mg / ml, initial fluticasone furoate = 0.01 mg / ml,

[0035] Volume of final product = 10ml,

[0036] Step (1) mix and inject:

[0037] Dissolve 19.6mg of DPPC and 10.4mg of cholesterol directly in 30ml of ethanol in a water bath at 50°C, and then add 1mg of fluticasone furoate to completely dissolve it. Slowly inject the above-mentioned ethanol solution into 50ml of physiological saline under stirring state, and after mixing for 20 minutes, dilute to 100ml with physiological saline to obtain an initial volume of 100ml.

[0038] Step (2) diafiltration concentration step:

[0039] Hook the mixing container onto the peristaltic pump and diafilter cartridge. Diafilter cartridges are concave membrane fibers with a molecular weight cut off of 500,000 Daltons. The product was pumped from ...

Embodiment 2

[0041] Preparation of 10ml liposomes

[0042] Total initial volume = 100ml, ethanol content 30%,

[0043] Lipid composition: DPPC / ergosterol (molar ratio is 1:1), initial lipid=0.2mg / ml,

[0044] Initial fluticasone furoate = 0.01 mg / ml, final product volume = 10 ml,

[0045] Step (1) mix and inject:

[0046] Dissolve 19.6mg of DPPC and 10.4mg of ergosterol directly in 30ml of ethanol in a water bath at 50°C, and then add 1mg of fluticasone furoate to completely dissolve it. Slowly inject the above-mentioned ethanol solution into 50ml of physiological saline under stirring state, and after mixing for 20 minutes, dilute to 100ml with physiological saline to obtain an initial volume of 100ml.

[0047] Step (2) diafiltration concentration step:

[0048] Hook the mixing container onto the peristaltic pump and diafilter cartridge. Diafilter cartridges are concave membrane fibers with a molecular weight cut off of 500,000 Daltons. The product was pumped from the reaction vesse...

Embodiment 3

[0050] Fluticasone furoate liposomes with high encapsulation efficiency

[0051] According to the following steps, 5 parts of liposome suspensions with different drug and lipid ratios and high encapsulation efficiency were prepared, and the encapsulation efficiency of 5 parts of samples was all above 80%, and the encapsulation efficiency of sample 5 The rate is above 90%, and the average particle size is between 130nm and 160nm.

[0052]Sample #1: Weigh 6.5mg of DPPC and 3.5mg of cholesterol in a beaker, add 30ml of ethanol in a water bath at 50°C to dissolve completely, then add 1mg of FF to dissolve completely. While stirring, slowly drop the above solution into 50ml of normal saline with a syringe, mix for 20 minutes, and then dilute to 100ml with normal saline. The product was passed through a hollow fiber membrane at room temperature to remove ethanol and free fluticasone furoate and concentrated to 10 ml.

[0053] Sample #2: Weigh 9.8mg of DPPC and 5.2mg of cholesterol...

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Abstract

The invention provides a fluticasone furoate liposome and a preparation method thereof. The fluticasone furoate liposome comprises phospholipids, sterols and fluticasone furoate, wherein the amount of fluticasone furoate is 0.01% to 1%, and the amount of phospholipids is 0.065% %~0.196%, the amount of sterol is 0.035%~0.104%, the preparation method of the fluticasone furoate liposome comprises: (1) mixing and injecting (2) diafiltration concentration steps, the method of the present invention is simple to operate, and the process is stable , suitable for mass production.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to fluticasone furoate liposome suspension and a preparation method thereof. Background technique [0002] Certain sustained-release technologies suitable for inhaled administration use liposomes and lipoplexes to provide prolonged drug therapy to the lungs and systemically through sustained release and targeting capabilities and enhanced drug absorption at the site of disease. The invention comprises a method for treating lung diseases with liposome fluticasone furoate inhalation suspension. [0003] For drugs that are easily destroyed in the gastrointestinal tract or cannot be taken orally, inhalation is a better way of administration than injection. The bioavailability of the hormone drug system is low, and administration through the inhalation route can overcome the shortcomings of oral administration or intravenous injection of hormone therapy, especially t...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/10A61K9/72A61K47/24A61K47/28A61K31/58A61P11/00
CPCA61K9/0078A61K9/10A61K9/127A61K31/58A61K47/24A61K47/28A61P11/00
Inventor 黄才古许英爱范晨梦
Owner SHANGHAI ANOVENT PHARMA CO LTD
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