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Aerosol containing muscarine receptor antagonist and beta 2 receptor stimulant, and preparation method thereof

A technology of muscarinic receptors and β2 receptors, applied in aerosol delivery, medical preparations containing active ingredients, medical preparations with non-active ingredients, etc., can solve the problem of large differences in physical and chemical properties, compound aerosol Difficulty in preparation of preparations, inability to ensure the stability of preparations for effective distribution in the respiratory tract, etc., to achieve high delivery efficiency and stable delivery dose

Inactive Publication Date: 2017-07-14
SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the large difference in the physical and chemical properties of the two types of drugs, it brings great difficulties to the preparation of compound aerosols, and the conventional suspension-type aerosol prescription process often cannot guarantee the effective distribution of the respiratory tract and the stability of the preparation.

Method used

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  • Aerosol containing muscarine receptor antagonist and beta 2 receptor stimulant, and preparation method thereof
  • Aerosol containing muscarine receptor antagonist and beta 2 receptor stimulant, and preparation method thereof
  • Aerosol containing muscarine receptor antagonist and beta 2 receptor stimulant, and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Prescription: (parts by weight)

[0052] Propellant 100 parts

[0053] LABA particles 0.024 parts

[0054] LAMA particles 0.208 part

[0055] The weight ratio of LABA particles and LAMA particles is: LABA particles: LAMA particles=1:9.625;

[0056] Indacaterol maleate (IND) was micronized using a jet mill to form active drug granules.

[0057]The micronized particle size distribution was measured by laser diffraction. 50% of the volume of the micronized particles has an optical diameter of less than 1.9 μm, and 90% of the volume of the particles has a particle size of less than 5 μm.

[0058] Glycopyrrolate (GP)-loaded particles were prepared by the following method:

[0059] Homogenize 3.74 g of phospholipids, DSPC (1,2-distearoyl-sn-glycero-3-phosphocholine) and 0.26 g of calcium chloride in 80 mL of hot water (75 °C) using a high shear mixer For homogenization, slowly add 20mL PFOB during homogenization. The resulting coarse emulsion was further homogenized 5 ...

Embodiment 2

[0071] prescription:

[0072] Propellant 100 parts (containing PEG1000 0.01% w / w)

[0073] LABA particles 0.047 parts

[0074] LAMA Granules 0.146 servings (prescription 1) / 0.220 servings (prescription 2)

[0075] The weight ratio of LABA particles and LAMA particles is: LABA particles: LAMA particles=1:3.1 / 4.7;

[0076] According to the method in Example 1, micronized active particles of indacaterol maleate and particles loaded with glycopyrronium bromide were prepared.

[0077] Indacaterol maleate micronized active particles, 90% of the volume of micronized particles have an optical diameter of less than 2.7 μm, and 50% of the volume of particles have a particle size of less than 1.4 μm.

[0078] GP: glycopyrronium bromide particles with phospholipid ratio of 1:6, 50% volume of drug-loaded particles is less than 3.5 μm, and 90% volume of drug-loaded particles is less than 6.6 μm. GP: phospholipid 1:15 glycopyrronium bromide particles, 50% of the volume of the drug-loaded...

Embodiment 3

[0084] prescription:

[0085] Propellant 100 parts

[0086] LABA particles 0.024 parts

[0087] LAMA particles 0.125 parts

[0088] The weight ratio of LABA particles and LAMA particles is: LABA particles: LAMA particles=1:5.2;

[0089] According to the method in Example 1, micronized active particles of indacaterol maleate were prepared.

[0090] Glycopyrrolate-loaded particles were prepared by:

[0091] Dissolve polyvinylpyrrolidone K30 and glycopyrronium bromide 5:1 (w / w weight) in water to obtain a solution with a weight solid content of 2% (w / v);

[0092] Spray drying was performed using the following spray drying conditions: inlet temperature 100°C, outlet temperature 72°C, emulsion feed rate 1.5 mL / min. The particle size distribution of the drug-loaded particles was determined by laser diffraction: 50% of the volume of the drug-loaded particles was smaller than 3.5 μm, and 90% of the volume of the drug-loaded particles was smaller than 6.3 μm.

[0093] Weigh the t...

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Abstract

The invention discloses an aerosol containing muscarine receptor antagonist and beta 2 receptor stimulant, and a preparation method thereof. The aerosol contains a propulsive agent, long-acting beta 2 receptor stimulant particles, and long-acting muscarine antagonist particles; in LABA particles, by volume, the geometric particle size of 90% particles is smaller than 10<mu>m, and the geometric particle size of 50% particles is smaller than 4<mu>m or even smaller; the middle particle size of LAMA particles ranges from 500nm to 10<mu>m; the LAMA particles are particles composed of LAMA, calcium chloride, and a surfactant; or the LAMA particles are particles composed of LAMA and an excipient. 1 to 100<mu>g of the aerosol is sprayed in each time of pressing of a MDI (metered dose inhaler), and the amount of LABA or LAMA in the aerosol ranges from 0.02 to 2mg / mL. The advantages of the aerosol are that: delivery efficiency is relatively high, and the delivery dosage is stable in long term of storing.

Description

technical field [0001] The present invention relates to an aerosol comprising a long-acting muscarinic antagonist and a long-acting β2 adrenergic receptor agonist. Background technique [0002] Chronic obstructive pulmonary disease (COPD) is a preventable and treatable disease characterized by airflow limitation, which is not fully reversible and develops progressively. It is related to the abnormal inflammatory response of harmful particles, mainly involving the lungs, and can also cause systemic (or extrapulmonary) adverse effects. COPD is an important respiratory system disease in my country and even in the world. Its prevalence rate, hospitalization rate, disability rate and mortality rate are high, and it has become an important social problem. According to statistics, 2.74 million people die from COPD every year in the world, and as many as 600 million people are troubled by it every year. WTO data and epidemiological data show that the prevalence and mortality of CO...

Claims

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Application Information

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IPC IPC(8): A61K9/12A61K9/72A61K45/06A61K31/4704A61K31/40A61K47/02A61K47/32A61K47/24A61K47/06A61P11/06A61P11/00
CPCA61K9/008A61K31/40A61K31/4704A61K45/06A61K47/02A61K47/06A61K47/24A61K47/32A61K2300/00
Inventor 吴闻哲侯惠民张琪朱万辉
Owner SHANGHAI MODERN PHARMA ENG INVESTIGATION CENT
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