Formoterol and ciclesonide aerosol formulations

• US 20050207984A1
• Filed: 04/01/2003
• Published: 09/22/2005
• Est. Priority Date: 04/05/2002
• Status: Abandoned Application

• Current Assignee: 3M Innovative Properties Company (3M Company)
• Original Assignee: 3M Innovative Properties Company (3M Company)
• Inventors: Oliver, Martin J., Jinks, Philip A.
• Application Number:
  US10/510,147
• Publication Number:
  US 20050207984A1
• Time in Patent Office: Days
• US Class Current: 424/45
• 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 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• 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 11/08 Bronchodilators
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

A pharmaceutical aerosol formulation comprising particles of formoterol or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, said particles being suspended in the formulation; a compound of the formula (I), in which: R₁ is 1-butyl, 2-butyl, cyclohexyl or phenyl and R₂ is acetyl or isobutanoyl, said compound of formula (I) being dissolved in the formulation; and a propellant selected from 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and a mixture thereof.

Claims

1. A pharmaceutical aerosol formulation comprising

particles of formoterol or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, said particles being suspended in the formulation;

a compound of the formula (I);

in which;

R₁ is 1-butyl, 2-butyl, cyclohexyl or phenyl and R₂ is acetyl or isobutanoyl, said compound of formula (I) being dissolved in the formulation; and

a propellant selected from 1,1,1,2-tetrafluoroethane, 1,1,1,2,3,3,3-heptafluoropropane and a mixture thereof.

2. A pharmaceutical aerosol formulation according to claim 1, wherein the formoterol is in the form of fomoterol fumarate.

3. A pharmaceutical aerosol formulation according to claim 1, wherein the compound of formula (I) is ciclesonide.

4. A pharmaceutical aerosol formulation according to claim 1, wherein the formulation further comprises ethanol.

5. A pharmaceutical aerosol formulation according to claim 4, wherein ethanol is present in an amount from 3 to 20% by weight of the formulation.

6. A pharmaceutical aerosol formulation according to claim 5, wherein ethanol is present in an amount from 3.5 to 20% by weight of the formulation.

7. A pharmaceutical aerosol formulation according to claim 6, wherein ethanol is present in an amount from 5 to 20% by weight of the formulation.

8. A pharmaceutical aerosol formulation according to claim 1, wherein the propellant is 1,1,1,2-tetrafluoroethane or a mixture of 1,1,1,2-tetrafluoroethane and 1,1,1,2,3,3,3-heptafluoropropane.

9. A pharmaceutical aerosol formulation according to any one of the claim 1, wherein 1,1,1,2-tetrafluoroethane is the only propellant component.

10. A pharmaceutical aerosol formulation according claim 1, wherein the formulation further comprises a bulking agent having a mass median diameter of less than one micron.

11. A pharmaceutical aerosol formulation according to claim 10, wherein the bulking agent has a mass median diameter of not more than 300 nm.

12. A pharmaceutical aerosol formulation according to claim 10, wherein the weight ratio of formoterol or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof to bulking agent is in the range 1:

0.1 to 1;

25.

13. A dispenser comprising an aerosol vial equipped with a dispensing valve, said aerosol vial containing a formulation according to claim 1.

14. A dispenser according to claim 13, wherein an interior surface of the aerosol vial is coated with a coating comprising a fluorocarbon polymer.

15. A method of preparing a formulation according to claim 1, the method comprising the steps of (i) providing a solution of the compound of formula (I) in 1,1,1,2-tetrafluoroethane and/or 1,1,1,2,3,3,3-heptafluoropropane and (ii) dispersing particles of formoterol or a pharmaceutically acceptable.