Inhalation medicinal composition prepared from eplerenone and glucocorticoid serving as active ingredients

A technology of glucocorticoids and eplerenone, applied in the direction of drug combinations, organic active ingredients, medical preparations containing active ingredients, etc., can solve problems such as side effects, large doses, and insignificant effects

Active 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 medicinal composition prepared from eplerenone and glucocorticoid serving as active ingredients
  • Inhalation medicinal composition prepared from eplerenone and glucocorticoid serving as active ingredients
  • Inhalation medicinal composition prepared from eplerenone and glucocorticoid serving as active ingredients

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-1

[0024] Dissolve 1 g of eplerenone and 50 mg of fluticasone propionate 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 with a flow energy mill. After mixing, pass 200-mesh sieve and mixed for 3 times, divided into No. 3 capsules, each capsule contains 1 mg of eplerenone, 50 μg of fluticasone propionate, and 10 mg of lactose.

Embodiment 1-2

[0026] According to the formula of Example 1-1, eplerenone and fluticasone propionate 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, The powder spray was prepared according to the process of Example 1-1. Each capsule contains 1 mg of eplerenone, 50 μg of fluticasone propionate, and 10 mg of octaacetate-D-cellobiose ester.

Embodiment 2-1

[0028] Dissolve 2 g of eplerenone and 100 mg of fluticasone propionate in ethanol. After filtration, the filtrate is spray-dried and micronized to an average particle size of 4 μm, and 20 g of lactose 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 2 mg of eplerenone, 100 μg of fluticasone propionate, 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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PUM

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Abstract

The invention discloses an inhalation medicinal composition prepared from eplerenone and glucocorticoid serving as active ingredients. The inhalation medicinal composition consists of eplerenone, glucocorticoid and one or more carriers suitable for inhalation administration. The glucocorticoid is one or more of ciclesonide, desonide, fluticasone propopnate, mometasone furoate, beclomethasone dipropionate, flunisolide, and triamcinolone acetonide and medicinal salts or esters thereof; the inhalation medicinal composition is preferably prepared into aerosol powder which consists of eplerenone, glucocorticoid and carrier micro powder; the average grain diameter of the eplerenone and glucocorticoid micro powder is 0.5 to 1.0 mu m; and the average grain diameter of the carrier micro powder is 20 to 45 mu m.

Description

technical field [0001] The invention relates to the application of eplerenone and glucocorticoid in the preparation of medicines for treating human diseases, and also relates to a compound preparation of eplerenone and glucocorticoid. 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 damage. Many autoimmun...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/585A61P11/00
Inventor 孙亮陈松赵琳
Owner TIANJIN JINYAO GRP
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