Inhalant preparation containing calcitriol and mometasone furoate and preparation method thereof

A technology of mometasone furoate 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 benefit Long-term use, the effect of inhibiting bone density decline

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 mometasone furoate and 1 mg of calcitriol in ethanol. After filtration, the filtrate is spray-dried and micronized to an average particle size of 2 μm. 10 g of lactose is micronized to an average particle size of 20 μm by a flow energy mill. After mixing, Sieve through a 200-mesh sieve for 3 times and mix well, then pack into No. 3 capsules. Each capsule contains mometasone furoate 200μg and 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 mometasone furoate 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 , mixed with a 200-mesh sieve for 3 times and distributed into No. 3 capsules. Each capsule contains 100 μg of mometasone furoate 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, mometasone furoate and calcitriol were micronized with a fluid energy mill to make the average particle size reach 3 μm, and the carrier was changed to octaacetate-D-cellobiose with an average particle size of 35 μm Esters, according to the process of embodiment 2-1 to prepare powder spray.

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Abstract

An inhalant preparation containing calcitriol and mometasone furoate and a preparation method thereof. The preparation comprises mometasone furoate and calcitriol which are used as active components, and one or more pharmaceutic adjuvants which are suitable for inhalation administration, wherein the mass ratio of ciclesonide and calcitriol is 100-800:1; and the preparation is applicable to the treatment of airway diseases of human being or mammalian.

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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IPC IPC(8): A61K31/593A61K31/58A61K9/72A61P11/06
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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