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Formula and preparation method of salmeterol/fluticasone

A formulation and liposome technology, applied in the direction of pharmaceutical formulations, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as insufficient fluffy feeling, achieve smooth surface, enhance comfort and touch soft effect

Inactive Publication Date: 2020-04-28
长沙而道新能源科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Surprisingly, it was found that the resulting liposome-encapsulated complex, salmeterol and fluticasone propionate, had good uniformity after mixing the two components, and no component separation would occur; and the liposomes were soft to the touch, solving the problem of The problem of insufficient fluffiness caused by direct mixing of solid particles

Method used

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  • Formula and preparation method of salmeterol/fluticasone
  • Formula and preparation method of salmeterol/fluticasone
  • Formula and preparation method of salmeterol/fluticasone

Examples

Experimental program
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Effect test

Embodiment 1

[0034] A salmeterol-ticasone formula, comprising liposomes, and components encapsulated by liposomes, the components are composed of the following components in parts by mass:

[0035]

[0036] Wherein, the liposome is composed of myristyl phosphatidylcholine: dipalmitate phosphatidylglycerol: monoacyl phospholipid with a molar ratio of 1:1:1; the mass fraction of the liposome is 310 parts.

[0037] The mean particle size of salmeterol was milled to 10 microns and the mean particle size of fluticasone propionate was milled to 10 microns.

[0038] The preparation method of above-mentioned salmeterol-ticasone formula, comprises the steps:

[0039] S1. At 60°C, dissolve salmeterol, fluticasone propionate and acesulfame potassium in 500 parts by mass of ethanol according to the above-mentioned parts by mass, and stir to make solution A;

[0040] S2. At 60°C, dissolve liposomes in a mixed solution of 500 parts by mass of ethanol and water (1:1, v / v), heat to 60°C and stir to fo...

Embodiment 2

[0046] A salmeterol-ticasone formula, comprising liposomes, and components encapsulated by liposomes, the components are composed of the following components in parts by mass:

[0047]

[0048]Wherein, the liposome is composed of myristyl phosphatidylcholine: dipalmitate phosphatidylglycerol: monoacylphospholipid with a molar ratio of 5:3:1; the mass parts of liposome is 1950 parts.

[0049] The mean particle size of salmeterol was milled to 30 microns and the mean particle size of fluticasone propionate was milled to 30 microns.

[0050] The preparation method of above-mentioned salmeterol-ticasone formula, comprises the steps:

[0051] S1. At 60°C, dissolve salmeterol, fluticasone propionate and acesulfame potassium in 500 parts by mass of ethanol according to the above-mentioned parts by mass, and stir to make solution A;

[0052] S2. At 60°C, dissolve liposomes in a mixed solution of 2500 parts by mass of n-propanol and water (1:1, v / v), heat to 60°C and stir to form s...

Embodiment 3

[0058] A salmeterol-ticasone formula, comprising liposomes, and components encapsulated by liposomes, the components are composed of the following components in parts by mass:

[0059]

[0060] Wherein, the liposome is composed of myristyl phosphatidylcholine: dipalmitoylphosphatidylglycerol: monoacylphospholipid with a molar ratio of 4:2:1; the mass fraction of the liposome is 960 parts.

[0061] Salmeterol was milled to an average particle size of 20 microns, and fluticasone propionate was milled to an average particle size of 20 microns.

[0062] The preparation method of above-mentioned salmeterol-ticasone formula, comprises the steps:

[0063] S1. At 60°C, dissolve salmeterol, fluticasone propionate and acesulfame potassium in 500 parts by mass of ethanol according to the above-mentioned parts by mass, and stir to make solution A;

[0064] S2. At 60°C, dissolve liposomes in a mixed solution of 1500 parts by mass of n-butanol and water (1:1, v / v), heat to 60°C and stir...

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Abstract

The invention discloses a formula of salmeterol / fluticasone. The formula of the salmeterol / fluticasone comprises liposomes, as well as ingredients encapsulated in the liposomes. The ingredients encapsulated in the liposomes are as follows: 10-20 parts of salmeterol, 20-40 parts of fluticasone propionate, 1-5 parts of acesulfame, and 0.1-0.5 parts of an emulsifier; and parts by mass of the liposomes are 10-30 times of the sum of the parts by mass of the ingredients. In the complex prepared by encapsulating the ingredients with the liposomes, the two ingredients, namely the salmeterol and the fluticasone propionate, are mixed so as to achieve good uniformity, so that the phenomenon of component separation does not occur; and moreover, the liposomes are soft to touch, so that the problem of insufficient fluffy feeling due to direct mixing of solid particles is solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparation production, and in particular relates to a salmeterol-ticasone formula and a preparation method thereof. Background technique [0002] Salmeterol is a new type of selective long-acting β2-receptor agonist asthma drug. First launched in the UK in 1990, it is mainly used clinically for the treatment of moderate to severe asthma and asthma caused by exercise, or asthma aggravated by physical activity. Its chemical name is 4-hydroxy-α-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol. Because of its remarkable curative effect in related medical fields, it has been valued by the medical and academic circles. The demand for salmeterol in the market has also been on the rise. It is estimated that by 2022, with the aging of the global population, the global demand for salmeterol and its derivatives will increase by more than 50% compared with 2018. [0003] Fluticasone propionate ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/137A61K31/56A61K47/24A61K47/28A61P11/00A61P11/06
CPCA61K9/127A61K31/137A61K31/56A61K47/24A61K47/28A61P11/00A61P11/06A61K2300/00
Inventor 胡永煌
Owner 长沙而道新能源科技有限公司
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