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aerosol formulations for copd

A dosage and co-solvent technology, applied in the field of aerosol pharmaceutical solution formulations, can solve the problems of unpublished evidence of glycopyrronium chloride preparation, difficulty in grinding and the like

Active Publication Date: 2014-10-01
CHIESI FARM SPA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

WO2006 / 100453 proposes the use of iodide, acetate and sulfate as alternatives to glycopyrronium bromide because of the grinding difficulties associated with the latter
[0006] Until the disclosure of this specification, there has been no published evidence that glycopyrronium chloride is clinically effective or can be formulated in a manner suitable for administration to patients with respiratory diseases

Method used

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Experimental program
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Effect test

preparation example Construction

[0028] The present invention also relates to a process for the preparation of a pharmaceutical composition comprising adding 1M HCl to a solution of glycopyrronium chloride in HFA propellant and co-solvent, wherein the amount of 1M HCl added is between 0.05-0.4 μg / μl of the final solution.

[0029] The pharmaceutical composition of the present invention may also contain other additional pharmaceutically active ingredients for separate, sequential or simultaneous use. Optional additional pharmaceutical actives of the composition include any pharmaceutically active ingredient known in the art to be useful in the prophylaxis or treatment of respiratory diseases and symptoms thereof. Examples of such active ingredients are: beta-2-agonists such as formoterol, salbutamol, fenoterol, camoterol (TA 2005), indacaterol, miviterol, vilanterol ( GSK 642444), Terbutaline, Salmeterol, Bitoterol and Oxinaline, all their single stereoisomeric forms or their mixtures and their salts; corticos...

Embodiment

[0074] Stability of glycopyrronium chloride during storage

[0075] Solution formulations were prepared using the compositions shown in Table 1.

[0076] Table 1

[0077]

[0078] Acid-containing samples were prepared by adding 1 M HCl in an amount corresponding to 0.222 μg / μl solution.

[0079] This solution was poured into inverted storage tanks under different conditions: 5°; 25°C / 60%RH; 30°C / 75%RH. The samples were analyzed for glycopyrronium chloride content by chromatography after 1, 2 and 3 months of storage.

[0080] The results show the stabilizing effect of adding acid to glycopyrronium chloride solution formulations.

[0081] The formulation was found to maintain a constant content in the presence of 1M HCl, but was highly dependent on storage time and temperature if no acid was used. See Table 2 below when the formulations were stored with or without acid for 3 months at 25°C / 60% relative humidity.

[0082] Table 2

[0083] active ingredient

Res...

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Abstract

The present invention relates to stable aerosol solution formulations comprising glycopyrronium chloride for administration to patients with COPD and other respiratory diseases.

Description

field of invention [0001] The present invention relates to an aerosol pharmaceutical solution formulation comprising glycopyrronium chloride intended for use in pressurized metered dose inhalers. The invention also relates to the use of such formulations in the prevention and treatment of respiratory disorders including COPD. Background of the invention [0002] Glycopyrrolate (also known as glycopyrrolate) is a muscarinic M3 anticholinergic used to reduce salivation associated with the administration of some anesthetics and as an adjunctive therapy for peptic ulcer disease. It has also been reported to be effective in the treatment of asthmatic symptoms (Hansel et al., Chest 2005;128:1974-1979). [0003] WO 2005 / 107873 relates to the use of glycopyrronium bromide in the treatment of asthma in children. [0004] WO 01 / 76575 discloses controlled release formulations for pulmonary delivery of glycopyrronium bromide. The formulation is intended for use in respiratory disease...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/00A61K31/40
CPCA61K31/40B65B3/00B65B7/16A61K45/06A61K47/10A61K9/008A61P11/00A61P11/06A61P11/08A61K2300/00A61K9/12
Inventor S·邦奈利F·尤斯伯特E·扎姆贝里
Owner CHIESI FARM SPA