Combination medicament

• US 20060025392A1
• Filed: 12/11/2003
• Published: 02/02/2006
• Est. Priority Date: 12/12/2002
• Status: Active Grant

• Current Assignee: Covis Pharma GmbH (Apollo Global Management, Inc.)
• Original Assignee: Altana Pharma AG (Takeda Pharmaceutical Company Limited)
• Inventors: Weimar, Christian, Dietzel, Klaus, Mark, Degenhard, Muller, Helgert
• Granted Patent: US 7,879,833 B2
• Time in Patent Office: Days
• US Class Current: 514/171
• CPC Class Codes: A61K 31/575 substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol
• 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

Abstract

The invention relates to the combination of ciclesonide with formoterol.

Claims

2. A pharmaceutical composition comprising the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof;

and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, in fixed or free combination and together with a pharmaceutically acceptable excipient or vehicle in an administration form suitable for inhalative administration by means of a powder inhaler.

1. A pharmaceutical composition comprising the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof;

and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, in a fixed or free combination.

3. The pharmaceutical composition according to claim 2, wherein the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, are present ready mixed in a fixed combination.

4. The pharmaceutical composition according to claim 3, wherein lactose is present as an excipient or vehicle.

5. The pharmaceutical composition according to claim 2, wherein the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, are present in separate pack units, it being wherein it is possible to take out the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, from the separate pack units such that they are available for simultaneous inhalative administration.

6. The pharmaceutical composition according to claim 2, wherein the active compound ciclesonide is present as its R epimer in an amount greater than 95%.

7. The pharmaceutical composition according to claim 2, wherein the active compound ciclesonide is present as its R epimer in an amount greater than 95%, and the active compound R,R-formoterol is present as a hydrate, salt or hydrate of a salt thereof.

8. The pharmaceutical composition according to claim 7, wherein the active compound R,R-formoterol is present as a salt with an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, phosphoric acid, nitric acid, sulphuric acid, acetic acid, citric acid, D-gluconic acid, benzoic acid, 2-(4-hydroxybenzoyl) benzoic acid, butyric acid, sulphosalicylic acid, maleic acid, lauric acid, malic acid, fumaric acid, succinic acid, oxalic acid, tartaric acid, embonic acid, stearic acid, toluenesulphonic, methanesulphonic acid and 1-hydroxy-2-naphthoic acid.

9. The pharmaceutical composition according to claim 8, wherein the acid is fumaric acid or tartaric acid.

13. A method of treating an airway disease in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical composition according to claim 2 by means of a dry powder inhaler.

14. The method according to claim 13, wherein the airway disease is selected from the group consisting of bronchitis, obstructive bronchitis, COPD (chronic obstructive pulmonary disease), spastic bronchitis, allergic bronchitis, allergic asthma and bronchial asthma.

15. The method according to claim 13, wherein ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof is administered in a dose of 0.05 to 1 mg per day and R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof is administered in a dose of 10 to 50 μ

g per day.

16. The method according to claim 15, wherein the dose is administered once daily.

17. The pharmaceutical composition according to claim 3, wherein the active compound ciclesonide is present as its R epimer in an amount greater than 95%, and the active compound R,R-formoterol is present as a hydrate, salt or hydrate of a salt thereof.

18. The pharmaceutical composition according to claim 17, wherein the active compound R,R-formoterol is present as a salt with an acid selected from the group consisting of hydrochloric acid, hydrobromic acid, phosphoric acid, nitric acid, sulphuric acid, acetic acid, citric acid, D-gluconic acid, benzoic acid, 2-(4-hydroxybenzoyl) benzoic acid, butyric acid, sulphosalicylic acid, maleic acid, lauric acid, malic acid, fumaric acid, succinic acid, oxalic acid, tartaric acid, embonic acid, stearic acid, toluenesulphonic, methanesulphonic acid and 1-hydroxy-2-naphthoic acid.

19. The pharmaceutical composition according to claim 18, wherein the acid is fumaric acid or tartaric acid.

20. A method of treating an airway disease in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical composition according to claim 3 by means of a dry powder inhaler.

21. The method according to claim 20, wherein the airway disease is selected from the group consisting of bronchitis, obstructive bronchitis, COPD (chronic obstructive pulmonary disease), spastic bronchitis, allergic bronchitis, allergic asthma and bronchial asthma.

22. The method according to claim 21, wherein ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof is administered in a dose of 0.05 to 1 mg per day and R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof is administered in a dose of 10 to 50 μ

g per day.

23. The method according to claim 22, wherein the dose is administered once daily.

5-1. The pharmaceutical composition according to claim 2, wherein the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, are present in separate pack units, wherein it is possible to take out the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof and the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof, from the separate pack units such that they are available for successive inhalative administration.

10. A method of treating an airway disease in a patient comprising administering to a patient in need thereof a therapeutically effective amount of the active compound ciclesonide or a solvate, epimer, physiologically functional derivative or solvate of a physiologically functional derivative thereof in fixed or free combination with the active compound R,R-formoterol or a hydrate, solvate, salt, hydrate of a salt or solvate of a salt thereof.

11. The method according to claim 10, wherein the combination is a fixed combination and the active compounds are present in a form suitable for inhalative administration by means of a powder inhaler.

12. The method according to claim 10, wherein the active compound ciclesonide is present as its R epimer in an amount greater than 95%.