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Fluticasone and fluticasone ester/H1 receptor antagonist inhalant

A receptor antagonist, fluticasone technology, applied in the field of inhalants, can solve problems such as central nervous system adverse reactions

Inactive Publication Date: 2014-06-04
TIANJIN JINYAO GRP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] This kind of adverse reaction is mainly due to the fact that H1 receptor antagonists are used in systemic administration such as oral administration, and at the same time the drug dose is relatively large, basically above 5 mg / day. Central nervous system adverse reactions

Method used

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  • Fluticasone and fluticasone ester/H1 receptor antagonist inhalant
  • Fluticasone and fluticasone ester/H1 receptor antagonist inhalant
  • Fluticasone and fluticasone ester/H1 receptor antagonist inhalant

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Micronize the H1 receptor antagonist and other active ingredients with a flow energy mill, and micronize 10 g of anhydrous lactose with a flow energy mill to an average particle size of 56 μm. In capsule No. 3.

[0041]

Embodiment 2

[0046] active ingredient

[0047] Ethanol 500g

[0048] HFA227 1000.g

[0049] Preparation process: add the prescribed amount of active ingredients into ethanol, stir, fill in divided doses, seal the dose valve system, and then pressurize and inject HFA227 respectively to obtain the product.

[0050]

Embodiment 3

[0052] active ingredient

[0053] Ethanol 500g

[0054] HFA134a 1098g

[0055] Preparation process: add the prescribed amount of active ingredients into ethanol, stir, fill in divided doses, seal the dose valve system, and then pressurize and inject HFA134a respectively to obtain the product.

[0056]

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PUM

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Abstract

The invention relates to a fluticasone and fluticasone ester / H1 receptor antagonist inhalant which contains fluticasone and fluticasone ester and one or more H1 receptor antagonists used as active components, and one or more pharmaceutical auxiliary materials suitable for inhalation administration. The H1 receptor antagonist is one or more of loratadine, desloratadine, cetirizine, levocetirizine, astemizole, ketotifen, ebastine, fexofenadine, avastin, mequitazine, mizolastine and salts thereof, and preferably one or more of loratadine, desloratadine, cetirizine, levocetirizine, ebastine, mizolastine, avastin, mequitazine, ketotifen and hydrochlorides or fumarates thereof.

Description

Technical field: [0001] The present invention relates to inhalants containing glucocorticoid H1 receptor antagonists. Background technique: [0002] Glucocorticoids have anti-inflammatory, anti-allergic, anti-rheumatic, and immunosuppressive effects, and are widely used in the treatment of allergic and autoimmune inflammatory diseases. Such as connective tissue disease, active rheumatism, rheumatoid arthritis, lupus erythematosus, severe bronchial asthma, severe dermatitis, ulcerative colitis, acute leukemia, etc. It is also used for some serious infections, poisoning, and malignant lymphoma. treat. [0003] 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 t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K9/72A61K31/56A61P11/06
Inventor 孙亮赵琳
Owner TIANJIN JINYAO GRP
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