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Inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components

A technology of mometasone furoate and eplerenone, which is applied in the directions of drug combinations, organic active ingredients, medical preparations containing active ingredients, etc., can solve the problems of side effects, large dosage, and insignificant effects.

Inactive Publication Date: 2012-03-14
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the effect of using spironolactone in the treatment of pulmonary fibrosis is not significant, and because spironolactone can only be effective through liver metabolism, the treatment of pulmonary fibrosis with spironolactone can only be administered orally, and the dosage is relatively large. avoid side effects

Method used

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  • Inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components
  • Inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components
  • Inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0023] Dissolve 1 g of eplerenone and 50 mg of mometasone furoate in ethanol. After filtration, the filtrate is spray-dried and micronized so that the average particle size reaches 2 μm. 10 g of lactose is micronized by a flow energy mill to an average particle size of 20 μm. After mixing, Sieve through a 200-mesh sieve for 3 times, mix well, and pack into No. 3 capsules. Each capsule contains 1 mg of eplerenone, 50 μg of mometasone furoate, and 10 mg of lactose.

Embodiment 1-2

[0025] According to the formula in Example 1-1, eplerenone and mometasone furoate were micronized with a fluid 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 the process of Example 1-1 to prepare powder spray. Each capsule contains 1 mg of eplerenone, 50 μg of mometasone furoate, and 10 mg of octaacetate-D-cellobiose ester.

Embodiment 2-1

[0027] Dissolve 2 g of eplerenone and 100 mg of mometasone furoate in ethanol. After filtration, the filtrate is spray-dried and micronized to an average particle size of 4 μm. Lactose 20 g is micronized to an average particle size of 30 μm with a flow energy mill, and mixed , mixed with a 200-mesh sieve for 3 times and distributed into No. 3 capsules.

[0028] Each capsule contains 2 mg of eplerenone, 100 μg of mometasone furoate, and 20 mg of lactose.

[0029] 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

An inhalation pharmaceutical composition with eplerenone and momestasone furoate as active components comprises eplerenone, momestasone furoate and one or more carriers suitable for inhalation drug delivery. The inhalation pharmaceutical composition is preferably prepared into a dry powder inhalation, is composed of eplerenone, momestasone furoate and carrier micropowders, wherein the average particle size of the eplerenone and momestasone furoate micropowders is 0.5-10 microns, and the average particle size of the carrier micropowder is 20-45 microns.

Description

technical field [0001] The invention relates to the application of eplerenone and mometasone furoate in the preparation of medicines for treating human diseases, and also relates to a compound inhalation preparation of eplerenone and mometasone furoate. Background technique: [0002] Pulmonary fibrosis is the abbreviation of "diffuse interstitial lung disease" or "interstitial lung disease". It is a large group of diffuse pulmonary parenchymal diseases characterized by diffuse chronic inflammation and interstitial fibrosis of alveolar walls (including respiratory bronchioles). Idiopathic pulmonary fibrosis (IPF) is the most common type of pulmonary fibrosis, accounting for 65% of all pulmonary fibrosis. Other types of pulmonary fibrosis mainly include pulmonary fibrosis caused by silicosis, drugs, and poisoning. The etiology of IPF is unknown, and the pathogenesis has not been fully elucidated, but there is sufficient evidence that it is related to immune inflammatory dam...

Claims

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Application Information

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IPC IPC(8): A61K31/585A61K31/58A61K9/72A61P11/00
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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