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H1-receptor-antagonist-containing inhalation preparation

A receptor antagonist, dry powder inhalation technology, applied in the field of inhalation preparations, can solve problems such as adverse reactions in the central nervous system

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

[0005] This kind of adverse reaction is mainly due to the fact that H1 receptor antagonists are used in the use of systemic administration routes 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
[0006] At present, there are literature reports at home and abroad (Research on the prevention and treatment effect and mechanism of loratadine on children with bronchial asthma and allergic rhinitis, Chinese General Practice Medicine, No. 1, 2008, pages 18-20) began to inhale glucocorticoid Corticosteroids such as fluticasone for basic treatment combined with oral H1 receptor antagonists such as loratadine are more effective than inhaled corticosteroids alone, but at the same time due to oral H1 receptor antagonists such as loratadine Treatment, the adverse reactions of the central nervous system such as fatigue and drowsiness cannot be avoided

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Micronize the H1 receptor antagonist 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. After mixing, pass through a 200-mesh sieve for 3 times and then pack in 1000 No. 3 capsules .

[0046] Example number

Embodiment 2

[0048] Dissolve the active ingredient in ethanol, filter, spray-dry the filtrate, micronize it so that the D90 particle size meets the requirements in the table below, micronize 20g of the carrier until the average particle size meets the requirements in the table below, mix well, and use a 200-mesh sieve to mix three times Divide evenly into 1000 No. 3 capsules.

[0049] 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.

[0050]

Embodiment 3

[0052] 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.

[0053]

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Abstract

The invention relates to an H1-receptor-antagonist-containing inhalation preparation which contains an H1 receptor antagonist 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 components and uses of inhalation formulations containing H1 receptor antagonists. Background technique: [0002] Histamine is a chemical mediator found in mast cells in human tissues and basophils in blood. When these cells are stimulated by immune reasons or other physical and chemical factors, the antigen combines with IgE on the cell surface, causing the cells to be injured and release a large amount of histamine. Histamine causes skin and mucous membrane telangiectasia and increased permeability through the H1 and H2 receptors of various tissues and organs, resulting in erythema and wheal; cerebral vasodilation (headache occurs); blood pressure drops; heart rate accelerates and cardiac output increases; And gastrointestinal smooth muscle spasm; increased gastric secretion; histamine stimulation of nerve endings also leads to itching and pain. [0003] H1 receptor antagonists selectively bind to H1 receptors on h...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/72A61K9/12A61K9/14A61K45/00A61K45/06A61P11/06
Inventor 孙亮赵琳
Owner TIANJIN JINYAO GRP
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