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Inhalable effervescent powder mist and its application in the preparation of infectious pneumonia medicine

A powder aerosol and effervescent technology, applied in the field of pharmaceutical preparations, can solve the problems of large particle size and poor dissolution speed of powder aerosol, and achieve the effects of accelerating dissolution, improving dispersion ability, and avoiding phagocytosis and removal

Active Publication Date: 2022-04-29
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Traditional powder aerosols have large particle size and poor dissolution rate, and are easily cleared by the rhythmic movement of cilia after entering the lungs; at the same time, drug powder particles that are not cleared by cilia may still be phagocytized and cleared by lung macrophages

Method used

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  • Inhalable effervescent powder mist and its application in the preparation of infectious pneumonia medicine
  • Inhalable effervescent powder mist and its application in the preparation of infectious pneumonia medicine
  • Inhalable effervescent powder mist and its application in the preparation of infectious pneumonia medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032]

[0033] Preparation process: Precisely weigh 2,5-diketone-3,6-bis(4-fumaryl-aminobutyl)piperazine and citric acid, add deionized water to dissolve and dissolve with 1% ammonia water (v / v) Adjust the pH of the solution to 8.0, filter the insoluble matter through a 0.45 μm filter membrane, and seal it as an acid source solution; accurately weigh the prescribed amount of sodium bicarbonate, add deionized water to dissolve, and filter out the insoluble matter through a 0.45 μm filter membrane Substance; Accurately weigh the recipe amount of azithromycin, add 10% glacial acetic acid solution (v / v) to dissolve, cross a 0.45 μm filter membrane to filter out insoluble matter and adjust the pH of the solution to 8.0 with 1% ammonia water (v / v); The sodium hydrogen solution and the azithromycin solution were added dropwise into the acid source solution, the stirring was continued for 10 minutes, and the spray drying was carried out rapidly to obtain the azithromycin effervesc...

Embodiment 2

[0035]

[0036] Preparation process: Precisely weigh 2,5-diketone-3,6-bis(4-fumaryl-aminobutyl)piperazine and citric acid, add deionized water to dissolve and dissolve with 1% ammonia water (v / v) Adjust the pH of the solution to 8.0, pass through a 0.45 μm filter membrane to filter out insoluble substances, use it as an acid source solution, and seal; accurately weigh the prescription amount of sodium bicarbonate, add deionized water to dissolve, pass through a 0.45 μm filter membrane to filter out insoluble substances Precisely weigh the prescription amount of azithromycin, add 10% glacial acetic acid solution (v / v) to dissolve, filter the insoluble matter through a 0.45 μm filter membrane and adjust the pH of the solution to 8.0 with 1% ammonia water (v / v); Add the sodium solution and azithromycin solution dropwise into the acid source solution, continue to stir for 10 minutes, and quickly carry out spray drying to obtain azithromycin effervescent powder aerosol granules....

Embodiment 3

[0038] Prescription: 2,5-diketo-3,6-bis(4-fumaryl-aminobutyl)piperazine 12.64g

[0039] Sodium bicarbonate 2.36g

[0040] Azithromycin 10.00g

[0041]Preparation process: Precisely weigh the prescribed amount of 2,5-diketone-3,6-bis(4-fumaryl-aminobutyl)piperazine, add deionized water to dissolve and dissolve with 1% ammonia water (v / v) Adjust the pH of the solution to 8.0, pass through a 0.45 μm filter membrane to filter out insoluble substances, use it as an acid source solution, and seal; accurately weigh the prescription amount of sodium bicarbonate, add deionized water to dissolve, pass through a 0.45 μm filter membrane to filter out insoluble substances; Measure the prescribed amount of azithromycin, add 10% glacial acetic acid solution (v / v) to dissolve, filter the insoluble matter through a 0.45 μm filter membrane and adjust the pH of the solution to 8.0 with 1% ammonia water (v / v); Add the azithromycin solution dropwise into the acid source solution, continue to sti...

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Abstract

The invention discloses an inhalable effervescent powder mist and its application in the preparation of medicines for treating infectious pneumonia, belonging to the technical field of medicine. The inhalable effervescent powder mist comprises active agent and effervescent agent, and the mass ratio of active agent and effervescent agent is 1:1~50; Described effervescent agent is made up of acid and alkali, and described acid comprises at least Diketopiperazine can optionally include one or more of citric acid, malic acid, fumaric acid, maleic acid, succinic acid or tartaric acid, and the base is selected from sodium carbonate, potassium carbonate, sodium bicarbonate or One or more of potassium bicarbonate. The effervescent powder mist of the present invention can provide a driving force for the active agent, that is, the drug powder, to accelerate the dissolution of the drug in the mucus layer on the surface of the bronchi and alveoli, and avoid macrophages from engulfing and clearing the drug.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an inhalable effervescent powder mist and its application in preparing medicines for treating infectious pneumonia. Background technique [0002] Lower respiratory tract infection refers to respiratory system infection caused by viruses, bacteria, mycoplasma, chlamydia, Legionella and other microorganisms that occur below the throat. According to different infection sites, it can be divided into bronchitis, bronchitis, pneumonia, etc. Viral pneumonia caused by a new type of coronavirus is spreading globally. Pneumonia caused by lower respiratory tract infection has become the third leading cause of death in the world, thus posing a serious threat to human health. [0003] Antibiotics or antiviral drugs used for the treatment of lower respiratory tract infection need to be effectively enriched in the lesion site. The existing conventional treatment...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/72A61K9/14A61K47/22A61K47/12A61K47/02A61K45/00A61K45/06A61K31/7052A61K31/351A61P11/00A61P31/04A61P31/12A61P31/14
CPCA61K9/0007A61K9/0073A61K9/14A61K47/22A61K47/12A61K47/02A61K45/00A61K45/06A61K31/7052A61K31/351A61P11/00A61P31/04A61P31/12A61P31/14
Inventor 涂家生王祺玥孙春萌沈雁
Owner CHINA PHARM UNIV
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