AEROSOL FORMULATION FOR COPD

• US 20110146677A1
• Filed: 12/23/2010
• Published: 06/23/2011
• Est. Priority Date: 12/23/2009
• Status: Abandoned Application

• Current Assignee: Chiesi Farmaceutici SPA (Valline Srl)
• Original Assignee: Chiesi Farmaceutici SPA (Valline Srl)
• Inventors: BONELLI, Sauro, Usberti, Francesca, Zambelli, Enrico
• Application Number:
  US12/977,223
• Publication Number:
  US 20110146677A1
• Time in Patent Office: Days
• US Class Current: 128/203.12
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/40 having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 47/10 Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
• CPC Class Codes: A61K 9/008 comprising drug dissolved or suspended in liquid propellant for inhalation via a pressurized metered dose inhaler [MDI]
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/06 Antiasthmatics
• CPC Class Codes: A61P 11/08 Bronchodilators
• CPC Class Codes: B65B 3/00 Packaging plastic material, semiliquids, liquids or mixed solids and liquids, in individual containers or receptacles, e.g. bags, sacks, boxes, cartons, cans, or jars
• CPC Class Codes: B65B 7/16 Closing semi-rigid or rigid containers or receptacles not deformed by, or not taking-up shape of, contents, e.g. boxes or cartons

Abstract

The stable aerosol solution formulations comprising glycopyrronium chloride are useful for administration to patients with COPD and other respiratory conditions.

Claims

1. A pharmaceutical composition, comprising glycopyrronium chloride dissolved in an HFA propellant and optionally a co-solvent, wherein said composition comprises an amount of acid equivalent to 0.05 to 0.4 mg/μ

l of 1M HCl.

2. A composition according to claim 1, wherein said composition comprises an amount of acid equivalent to 0.19 to 0.25 μ

g/μ

l of 1M HCl.

3. A composition according to claim 1, wherein the co-solvent is ethanol.

4. A composition according claim 1, comprising glycopyrronium chloride in an amount of 0.005 to 0.83% w/w of the composition.

5. A composition according to claim 1, further comprising one or more pharmaceutically active ingredients selected from the group consisting of beta-2-agonists, corticosteroids, antimuscarinic agents, and phosphodiesterase (IV) inhibitors.

6. A composition according to claim 5, further comprising formoterol fumarate.

7. A composition according to claim 5, further comprising beclometasone dipropionate.

8. A metered dose inhaler, comprising a pharmaceutical composition according to claim 1.

9. A kit-of-parts, comprising a pharmaceutical composition according to claim 1 and further comprising one or more pharmaceutically active ingredients for separate, sequential or simultaneous administration, wherein said pharmaceutically active ingredients are selected from the group consisting of beta-2-agonists, corticosteroids, antimuscarinic agents, and phosphodiesterase (IV) inhibitors.

10. A method of filling an aerosol canister with a pharmaceutical composition according to claim 1, comprising:

a) preparing a solution comprising glycopyrronium chloride, a co-solvent, a mineral acid and optionally a low volatility component;

b) filling an open canister with the solution;

c) placing a valve onto the canister and crimping; and

d) pressure-filling the canister with HFA propellant through the valve.

11. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 1 to a subject in need thereof.

12. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 2 to a subject in need thereof.

13. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 3 to a subject in need thereof.

14. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 4 to a subject in need thereof.

15. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 5 to a subject in need thereof.

16. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 6 to a subject in need thereof.

17. A method for the prevention and/or treatment of chronic obstructive pulmonary disease, comprising administering an effective amount of a composition according to claim 7 to a subject in need thereof.