Granted Patent B2

US 7,879,832 · App. 10/524,821 · Granted Feb 1, 2011

Abstract

Claims (33)

1. A pharmaceutical composition for application to the mucosa comprising as the sole active ingredients a combination of

a.) 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)phthalazinone (AZELASTINE), or a stereoisomer, a pharmaceutically acceptable salt or physiologically functional derivative thereof, and

b.) ciclesonide, or a pharmaceutically acceptable salt of ciclesonide, an epimer of ciclesonide, or a physiologically functional derivative of ciclesonide,

and a pharmaceutically acceptable carrier and/or one or more excipients, wherein said pharmaceutical composition has an osmotic pressure of less than 290 mOsm.

2. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein said osmotic pressure is 150 mOsm or less.

3. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein said osmotic pressure is 60 mOsm or less.

4. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein said osmotic pressure is 40 mOsm or less.

5. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein said osmotic pressure is 20 mOsm or less.

6. The pharmaceutical composition for application to the mucosa according to claim 1 , further comprising an osmotic pressure-controlling agent.

7. The pharmaceutical composition for application to the mucosa according to claim 1 , further comprising a water-insoluble and/or water-low soluble substance.

8. The pharmaceutical composition for application to the mucosa according to claim 7 , wherein said water-insoluble and/or water-low soluble substance is a cellulose.

9. The pharmaceutical composition for application to the mucosa according to claim 8 , wherein said cellulose is microcrystalline cellulose.

10. The pharmaceutical composition for application to the mucosa according to claim 7 , wherein said one or more water-insoluble and/or water-low soluble substances is/are present as solid particles in an aqueous medium.

11. The pharmaceutical composition for application to the mucosa according to claim 7 , further comprising a water-soluble polymer substance.

12. The pharmaceutical composition for application to the mucosa according to claim 11 , wherein a combination of said water-insoluble substance and water-soluble polymer consists of microcrystalline cellulose and carboxymethyl cellulose sodium.

13. The pharmaceutical composition for application to the mucosa according to claim 1 , further comprising a surfactant and/or a wetting agent.

14. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein said mucosa is nasal mucosa.

15. A method for the treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal, which comprises administration of a therapeutically effective amount of a pharmaceutical formulation comprising as the sole active ingredients a combination of

a.) 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)phthalazinone (AZELASTINE) or a stereoisomer, a pharmaceutically acceptable salt or physiologically functional derivative thereof, and

b.) ciclesonide, or a pharmaceutically acceptable salt of ciclesonide, an epimer of ciclesonide, or physiologically functional derivative of ciclesonide,

and a pharmaceutically acceptable carrier and/or one or more excipients, wherein said pharmaceutical formulation has an osmotic pressure of less than 290 mOsm.

16. The pharmaceutical composition according to claim 1 , wherein said epimer of ciclesonide is [11β,16α(S)]-16,17-[(cyclohexylmethylen)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)-pregna-1,4-dien-3,20-dion and is present in any mixing ratio with ciclesonide, [11β,16α(R)]-16,17-[(cyclohexylmethylen)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)-pregna-1,4-dien-3,20-dion.

17. The method of claim 15 , wherein said mammal is a human.

18. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein the sole active ingredients are a combination of azelastine or a pharmaceutically acceptable salt thereof, and ciclesonide, or a pharmaceutically acceptable salt of ciclesonide, an epimer of ciclesonide, or a physiologically functional derivative of ciclesonide.

19. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein the pharmaceutically acceptable salt of azelastine is azelastine hydrochloride.

20. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein ciclesonide is [11β,16α(R)]-16,17-[(cyclohexylmethylen)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)-pregna-1,4-dien-3,20-dion.

21. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein the sole active ingredients are a combination of azelastine or a pharmaceutically acceptable salt thereof and ciclesonide.

22. The pharmaceutical composition for application to the mucosa according to claim 1 , wherein the sole active ingredients are a combination of azelastine hydrochloride and ciclesonide.

23. The method for the treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal according to claim 15 , wherein the sole active ingredients are a combination of azelastine or a pharmaceutically acceptable salt thereof and ciclesonide, or a pharmaceutically acceptable salt of ciclesonide, an epimer of ciclesonide, or a physiologically functional derivative of ciclesonide.

24. The method for the treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal according to claim 15 , wherein the pharmaceutically acceptable salt of azelastine is azelastine hydrochloride.

25. The method for the treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal according to claim 15 , wherein ciclesonide is [11β,16α(R)]-16,17-[(cyclohexylmethylen)bis(oxy)]-11-hydroxy-21-(2-methyl-1-oxopropoxy)-pregna-1,4-dien-3,20-dion.

26. The method for the treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal according to claim 15 , wherein the sole active ingredients are a combination of azelastine or a pharmaceutically acceptable salt thereof and ciclesonide.

27. The method for the treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal according to claim 15 , wherein the sole active ingredients are a combination of azelastine hydrochloride and ciclesonide.

Assignments (18)