A kind of erdosteine ​​inhalation powder mist and preparation method thereof

Abstract

The invention belongs to the field of medicines, and particularly relates to an erdosteine powder inhalation which is actively inhaled in a superfine powder mode and directly delivers a medicine to the lung to exert effect, solving the problem of low degradation effect and liver first pass elimination effect bioavailability of a medicine in gastrointestinal tracts. The erdosteine powder inhalation is prepared by mixing superfine erdosteine powder and superfine poloxamer 188 powder, wherein the average particle size of the superfine erdosteine powder at the weight ratio of 20:3-2:1 is 1-5 micrometers, and the maximum particle size is not more than 10 micrometers; the average particle size of the superfine poloxamer 188 powder is 60-80 micrometers, and the maximum particle size is not more than 100 micrometers. A preparation method comprises the following steps: grinding erdosteine, carrying out superfine crushing by using a superfine crusher to obtain the superfine powder of which the average particle size is 1-5 micrometers; carrying out superfine crushing on poloxamer 188 by using the superfine crusher to obtain the superfine powder of which the average particle size is 60-80 micrometers; and uniformly mixing the crushed superfine powder according to a proportion of 20:3-2:1, and then subpackaging.

Description

technical field

[0001] The invention belongs to the field of medicine, and in particular relates to an erdosteine ​​inhalation powder spray and a preparation method thereof. Background technique

[0002] Erdosteine ​​is a prodrug with a non-free closed sulfhydryl group in its structure and has no active effect on local mucin. After oral administration, it is metabolized to produce three metabolites containing free sulfhydryl groups to exert pharmacological effects. Erdosteine ​​metabolites in the body can break the disulfide bonds of mucin in bronchial secretions, change the composition and rheological properties of the secretions, reduce the viscosity of sputum, and improve the inhibited respiratory function. This product can scavenge free radicals , effectively protect a1-antitrypsin from the oxidative inactivation induced by smoke and dust, and prevent damage to lung elastin and neutrophils. It can significantly increase the ratio of IgA / albumin and lactoferrin / albumin, ...

Examples

preparation example Construction

[0069] The present invention also provides a preparation method for erdosteine ​​inhalation powder, comprising the following steps:

[0070] Step 1: grind erdosteine ​​into fine powder, and use an ultrafine pulverizer to perform ultrafine pulverization to obtain erdosteine ​​superfine powder with an average particle diameter of 1 μm to 5 μm; preferably, the obtained erdosteine ​​superfine powder The average particle size is 2 μm to 4 μm.

[0071] Step 2: Ultrafine pulverize Poloxamer 188 with an ultrafine pulverizer to obtain Poloxamer 188 ultrafine powder with an average particle size of 60 μm to 80 μm; preferably, the obtained Poloxamer 188 ultrafine powder The average particle size is 65 μm to 75 μm.

[0072] Step 3: Mix the pulverized erdosteine ​​superfine powder and poloxamer 188 superfine powder at a mass ratio of 20:3 to 2:1, and pack them in capsules. In order to improve the effectiveness of the proportioning, preferably, after mixing the ground erdosteine ​​superfi...

Embodiment 1

[0075] Grind the erdosteine ​​drug finely, and perform ultrafine pulverization with an ultrafine pulverizer to obtain ultrafine dry powder of erdosteine ​​with a particle diameter of 1 μm to 5 μm: pulverize Poloxamer 188 with a high-speed grinding pulverizer to obtain granules Poloxamer 188 ultrafine powder with a diameter of 60 μm to 80 μm; weigh 200 g of erdosteine ​​ultrafine powder and 60 g of poloxamer 188 micropowder, and mix them in equal increments. After mixing well, fill No. 2 capsules, each Fill 260mg, make 1000 capsules, that is.

Embodiment 2

[0077] Grind the erdosteine ​​drug finely, and use an ultrafine pulverizer for ultrafine pulverization to obtain an ultrafine powder with a particle size of 1 μm to 2 μm: pulverize Poloxamer 188 with a high-speed grinding pulverizer to obtain a particle size of 60 μm to 65 μm Poloxamer 188 superfine powder; weigh 200g of erdosteine ​​superfine powder and 80g of poloxamer 188 micropowder, mix them according to the method of increasing in equal amounts, after mixing thoroughly, fill No. 2 capsules, each filled with 280mg, and make 1000 capsules, ready to serve.

technical field

[0001] The invention belongs to the field of medicine, and in particular relates to an erdosteine ​​inhalation powder spray and a preparation method thereof. Background technique

[0002] Erdosteine ​​is a prodrug with a non-free closed sulfhydryl group in its structure and has no active effect on local mucin. After oral administration, it is metabolized to produce three metabolites containing free sulfhydryl groups to exert pharmacological effects. Erdosteine ​​metabolites in the body can break the disulfide bonds of mucin in bronchial secretions, change the composition and rheological properties of the secretions, reduce the viscosity of sputum, and improve the inhibited respiratory function. This product can scavenge free radicals , effectively protect a1-antitrypsin from the oxidative inactivation induced by smoke and dust, and prevent damage to lung elastin and neutrophils. It can significantly increase the ratio of IgA / albumin and lactoferrin / albumin, ...

Examples

preparation example Construction

[0069] The present invention also provides a preparation method for erdosteine ​​inhalation powder, comprising the following steps:

[0070] Step 1: grind erdosteine ​​into fine powder, and use an ultrafine pulverizer to perform ultrafine pulverization to obtain erdosteine ​​superfine powder with an average particle diameter of 1 μm to 5 μm; preferably, the obtained erdosteine ​​superfine powder The average particle size is 2 μm to 4 μm.

[0071] Step 2: Ultrafine pulverize Poloxamer 188 with an ultrafine pulverizer to obtain Poloxamer 188 ultrafine powder with an average particle size of 60 μm to 80 μm; preferably, the obtained Poloxamer 188 ultrafine powder The average particle size is 65 μm to 75 μm.

[0072] Step 3: Mix the pulverized erdosteine ​​superfine powder and poloxamer 188 superfine powder at a mass ratio of 20:3 to 2:1, and pack them in capsules. In order to improve the effectiveness of the proportioning, preferably, after mixing the ground erdosteine ​​superfi...

Embodiment 1

[0075] Grind the erdosteine ​​drug finely, and perform ultrafine pulverization with an ultrafine pulverizer to obtain ultrafine dry powder of erdosteine ​​with a particle diameter of 1 μm to 5 μm: pulverize Poloxamer 188 with a high-speed grinding pulverizer to obtain granules Poloxamer 188 ultrafine powder with a diameter of 60 μm to 80 μm; weigh 200 g of erdosteine ​​ultrafine powder and 60 g of poloxamer 188 micropowder, and mix them in equal increments. After mixing well, fill No. 2 capsules, each Fill 260mg, make 1000 capsules, that is.

Embodiment 2

[0077] Grind the erdosteine ​​drug finely, and use an ultrafine pulverizer for ultrafine pulverization to obtain an ultrafine powder with a particle size of 1 μm to 2 μm: pulverize Poloxamer 188 with a high-speed grinding pulverizer to obtain a particle size of 60 μm to 65 μm Poloxamer 188 superfine powder; weigh 200g of erdosteine ​​superfine powder and 80g of poloxamer 188 micropowder, mix them according to the method of increasing in equal amounts, after mixing thoroughly, fill No. 2 capsules, each filled with 280mg, and make 1000 capsules, ready to serve.

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