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Inhalation preparation containing calcitriol and fluticasone propionate and preparation method thereof

A technology of fluticasone propionate and calcitriol, which is applied in the field of drugs for the treatment of respiratory diseases, especially asthma, can solve problems such as hypercalcemia and application restrictions of calcitriol, reduce serum IgE, and facilitate long-term use , good therapeutic effect

Inactive Publication Date: 2011-11-23
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the literature also pointed out that due to the large dose required for immunomodulatory therapy, long-term application is likely to cause side effects such as hypercalcemia, and the application of calcitriol is limited to a certain extent.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] Dissolve 200 mg of fluticasone propionate and 1 mg of calcitriol in ethanol. After filtration, the filtrate is spray-dried and micronized to make the average particle size reach 2 μm. 10 g of lactose is micronized to an average particle size of 20 μm with a fluid energy mill. After mixing, pass The 200-mesh sieve was mixed for 3 times and divided into No. 3 capsules. Each capsule contains fluticasone propionate 200μg, calcitriol 1μg

[0038] The process conditions are: the inlet temperature is 105°C, the outlet temperature is 68°C, the air flow rate is 90%, the inner diameter of the nozzle outlet is 0.1cm, the air flow rate of the nozzle is 800ml / min, and the injection speed is 50mL / h

Embodiment 2-1

[0040] Dissolve 100 mg of fluticasone propionate and 1 mg of calcitriol in ethanol. After filtration, the filtrate is spray-dried and micronized so that the average particle size reaches 4 μm. Lactose 20 g is micronized by a fluid energy mill to an average particle size of 30 μm, and mixed evenly. Mix evenly with a 200-mesh sieve for 3 times and distribute into No. 3 capsules. Each capsule contains 100 μg of fluticasone propionate and 1 μg of calcitriol.

[0041] 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.

Embodiment 2-2

[0043] According to the formula in Example 2-1, fluticasone propionate and calcitriol were micronized with a fluid energy mill so that the average particle size reached 3 μm, and the carrier was changed to octaacetate-D-cellobiose ester with an average particle size of 35 μm , according to the process of Example 2-1 to prepare powder spray.

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PUM

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Abstract

The invention relates to an inhalation preparation containing calcitriol and fluticasone propionate and a preparation method thereof. The inhalation preparation comprises calcitriol, and fluticasone propionate as active components, and one or more of pharmaceutic adjuvants which are suitable for inhalation administration, a mass ratio of ciclesonide to calcitriol is 100-800:1, and the inhalation preparation is used for treating airway diseases of humans or mammals.

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. At present, the drugs for the treatment of asthma and other lung diseases mainly include the following: (1) β2-receptor agonists, (2) xanthine drugs, (3) anti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/593A61K31/56A61K9/72A61P11/06
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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