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Oral lung inhalation aerosol powder

A technology of powder aerosol and lung inhalation, which is applied in the field of inhalation powder aerosol and its preparation, can solve problems such as pulmonary adverse reactions, difficulty in industrialization, and influence on treatment effect, so as to improve lung deposition rate, improve curative effect, and achieve good results. Effect of lung deposition rate

Active Publication Date: 2010-06-30
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the experiment, we found that the lung deposition rate of the active ingredient of the powder aerosol prepared according to the technical scheme disclosed in this invention is only 15% to 17%, and, because the particle size of the powder is too small, most of the carriers will It enters the lungs and deposits with the inhaled airflow, and it is easy to cause adverse reactions to the lungs such as pulmonary fibrosis when used for a long time
In addition, after a certain period of storage of too fine powder, it is very easy to cause particle aggregation due to static electricity and affect the therapeutic effect.
In addition, the cost of crushing all the auxiliary materials to a particle size of 0.1-10 μm is high, requires a large amount of energy consumption, and is difficult to industrialize

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0025] Micronize 0.2 g of budesonide with a flow energy mill so that the average particle size reaches 2 μm, and micronize 10 g of lactose with a flow energy mill to an average particle size of 20 μm. After mixing, pass through a 200-mesh sieve for 3 times before mixing Packed in capsule size 3.

Embodiment 1-2

[0027] According to the formulation of Example 1-1, budesonide was micronized with a flow energy mill to make the average particle size reach 1 μm, and the carrier was changed to octaacetate-D-cellobiose ester with an average particle size of 25 μm, according to Example 1- The process of 1 prepares the powder spray.

Embodiment 2-1

[0029] Dissolve 0.1 g of mometasone furoate in ethanol, filter, spray-dry the filtrate, and micronize it so that the average particle size reaches 4 μm, and micronize 20 g of lactose to an average particle size of 30 μm with a fluid energy mill, mix well, and use 200 Mesh sieve 3 times and mix evenly, then pack into No. 3 capsules.

[0030] The process conditions are as follows: inlet temperature is 105°C, outlet temperature is 68°C, air flow rate is 90%, nozzle outlet inner diameter is 0.1cm, nozzle air flow rate is 800ml / min, and sample injection speed is 50mL / h.

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Abstract

The invention discloses an oral lung inhalation aerosol powder, which can improve the lung deposition rate of active ingredients of the aerosol powder, avoid the deposition of carrier micropowder in the lung, and increase the stability of the composition. The oral lung inhalation aerosol powder consists of the active ingredients and the carrier micropowder. The oral lung inhalation aerosol powder is characterized in that: the mean grain size of the micropowder of the active ingredients is between 0.5 and 10 mu m, and the mean grain size of the carrier micropowder is between 20 and 45 mu m.

Description

Technical field: [0001] The invention relates to a medicine for treating respiratory diseases, especially asthma, in particular to an inhalation powder spray and a preparation method thereof. Background technique: [0002] Asthma is a chronic airway inflammation characterized by reversible airway obstruction and increased airway responsiveness. Airway obstruction is caused by two factors: increased secretions caused by bronchial mucosal inflammation, mucosal edema, and smooth muscle spasm stimulated by inflammation; while asthma Increased airway reactivity is also a result of damage to the bronchial epithelium due to airway inflammation. It is recognized that only by controlling the inflammation of the airway mucosa can the ultimate goal of reducing airway hyperresponsiveness and relieving asthma symptoms be achieved. The current drugs for the treatment of asthma and other lung diseases mainly include the following: [0003] (1) β2-receptor agonists [0004] (2) Xanthine ...

Claims

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Application Information

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IPC IPC(8): A61K9/72A61K47/26A61P11/14
Inventor 张其婉李静
Owner TIANJIN JINYAO GRP
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