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Agent for Ameliorating Chronic Obstructive Pulmonary Disease

a chronic obstructive pulmonary disease and agent technology, applied in the direction of drug compositions, organic chemistry, dispersed delivery, etc., can solve the problems of copd development, alveolar destruction and bronchial mucous gland hypertrophy, copd is a very troublesome disease, etc., and achieve excellent effect of ameliorating copd

Inactive Publication Date: 2015-02-05
LTT BIO PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides an agent for ameliorating COPD that contains mepenzolate bromide as an active ingredient. Mepenzolate bromide has been used as a therapeutic drug for irritable bowel and is safe for use. The agent has been found to have excellent effects in treating COPD through airway and inhalation administration, as well as oral and rectal administration. It works by both bronchodilating and anti-inflammatory effects. Additionally, mepenzolate bromide has a unique mechanism of action that makes it effective in treating COPD. This agent offers a specific and safe treatment for COPD that previously had no effective therapy.

Problems solved by technology

The primary cause of COPD development is smoking.
It is believed that the inflammation leads to protease-antiprotease imbalance, oxidant-antioxidant imbalance, and the like, which in turn causes alveolar destruction and bronchial mucous gland hypertrophy.
Smoking cessation, pharmacotherapy by administration of e.g., a bronchodilator, an expectorant, and an antitussive drug, oxygen therapy, or the like can only relieve symptoms of COPD, and thus COPD is a very troublesome disease.
However, it is unknown that mepenzolate bromide is effective for COPD treatment.
Furthermore, there has been no known therapeutic agent for COPD that has both a bronchodilator effect and an anti-inflammatory effect so far.

Method used

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  • Agent for Ameliorating Chronic Obstructive Pulmonary Disease
  • Agent for Ameliorating Chronic Obstructive Pulmonary Disease
  • Agent for Ameliorating Chronic Obstructive Pulmonary Disease

Examples

Experimental program
Comparison scheme
Effect test

working example 1

Inhalation Formulation

[0144]A liquid formulation for inhalation is prepared by mixing 1% (w / w) of mepenzolate bromide, 0.05% (w / w) of benzalkonium chloride, 10% (w / w) of polyethylene glycol, 20% (w / w) of propylene glycol, and the remaining percentage of purified water.

working example 2

Tablet

[0145]

Mepenzolate bromide 50 mgLactose146 mgHydroxypropylcellulose150 mgMagnesium Stearate 4 mg

[0146]Based on the formulation described above, granules were prepared and then the granules were compressed to prepare tablets each weighing 350 mg by a conventional method.

working example 3

Enema Preparation

[0147]An enema preparation was prepared by dissolving 1 mg of mepenzolate bromide in 1 mL of water and adding adequate amounts of carboxymethylcellulose sodium and tris(hydroxymethyl)aminomethane thereto.

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Abstract

This invention provides a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect. The agent for ameliorating chronic obstructive pulmonary disease contains mepenzolate bromide as an active ingredient. More preferably the mode of administration of the agent for ameliorating chronic obstructive pulmonary disease is airway administration or inhalation administration, and furthermore the mode of administration thereof is oral administration or rectal administration. This invention is a safe and effective agent for ameliorating chronic obstructive pulmonary disease (COPD) that has both a bronchodilator effect and an anti-inflammatory effect of mepenzolate bromide.

Description

TECHNICAL FIELD[0001]The present invention relates to an agent for ameliorating chronic obstructive pulmonary disease, and specifically to an agent for ameliorating chronic obstructive pulmonary disease that contains mepenzolate bromide (hereinafter may be referred to simply as “mepenzolate”) as an active ingredient.BACKGROUND ART[0002]In recent years, bronchodilators (a β-agonist, a muscarinic antagonist, and the like) have been used for treatment of chronic obstructive pulmonary disease (COPD: chronic obstructive pulmonary disease, hereinafter may be referred to as “COPD”) and these are reported to improve airflow limitation temporarily (Non-Patent Literature 1).[0003]Furthermore, ipratropium bromide, which is a muscarinic antagonist, is reported to exhibit a bronchodilator effect by relaxing bronchial smooth muscle (Non-Patent Literature 2).[0004]Chronic obstructive pulmonary disease (COPD) is a disease in which various factors, particularly smoking causes chronic lung inflammati...

Claims

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Application Information

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IPC IPC(8): A61K31/452
CPCA61K31/452A61K9/0031A61K9/0078A61K9/2018A61P11/00A61K9/0053A61K9/007
Inventor MIZUSHIMA, TORULIU, HONGXING
Owner LTT BIO PHARMA