Use of the combination of ciclesonide and antihistamines for the treatment of allergic rhinitis

• US 20050245493A1
• Filed: 08/29/2003
• Published: 11/03/2005
• Est. Priority Date: 08/30/2002
• Status: Active Grant

• Current Assignee: Covis Pharma GmbH (Apollo Global Management, Inc.)
• Original Assignee: Nycomed GmbH (Takeda Pharmaceutical Company Limited)
• Inventors: Marx, Degenhard, Muller, Helgert
• Granted Patent: US 7,879,832 B2
• Time in Patent Office: Days
• US Class Current: 514/171
• 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 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61P 11/00 Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/14 Decongestants or antiallergics
• CPC Class Codes: A61P 37/00 Drugs for immunological or allergic disorders
• CPC Class Codes: A61P 37/08 Antiallergic agents antiasthmatic agents A61P11/06; ophthalmic antiallergics A61P27/14
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

The present invention relates to a combination of ciclesonide with antihistamines.

Claims

1. Pharmaceutical composition for the treatment of allergic rhinitis and/or allergic conjunctivitis comprising as active ingredients a combination of at least one antihistamine, a stereoisomer, a Pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof and ciclesonide, pharmaceutically acceptable salts of ciclesonide, epimers of ciclesonide optionally in any mixing ratio with ciclesonide, solvates of ciclesonide, physiologically functional derivatives of ciclesonide or solvates thereof and a pharmaceutically acceptable carrier and/or one or more excipients.

2. Pharmaceutical composition according to claim 1 for the treatment of allergic rhinitis for application to the mucosa, which is an aqueous pharmaceutical composition comprising the active ingredients together with one or more water-insoluble and/or water-low soluble substance and having an osmotic pressure of less than 290 mOsm.

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

4. The pharmaceutical composition for application to the mucosa according to claim 2, wherein said osmotic pressure is 60 mOsm or less.

5. The pharmaceutical composition for application to the mucosa according to claim 2, wherein said osmotic pressure is 40 mOsm or less.

6. The pharmaceutical composition for application to the mucosa according to claim 2, wherein said osmotic pressure is 20 mOsm or less.

7. The pharmaceutical composition for application to the mucosa according to claim 2, further comprising an osmotic pressure-controlling agent.

8. The pharmaceutical composition for application to the mucosa according to claim 2, 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 2, wherein said one or more water-insoluble and/or water-low soluble substance is present as solid particles in an aqueous medium.

11. The pharmaceutical composition for application to the mucosa according to claim 2, further comprising a water-soluble polymer substance.

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

13. The pharmaceutical composition for application to the mucosa according to claim 2, further comprising a surfactant and/or a wetting agent.

14. The pharmaceutical composition for application to the mucosa according to claim 2, wherein said mucosa is nasal mucosa.

15. Pharmaceutical composition according to claims 1 through 14, wherein the antihistamine is selected from the group of (E)-6-[(E)-3-(1-pyrrolidinyl)-1-p-tolylpropenyl]-2-pyridineacrylic acid [INN:

ACRIVASTINE], 6,11-Dihydro-11-(1-methyl-4-piperidyliden)-5H-benzo[5,6]cyclohepta-[1,2-b]pyridin [INN;

AZATADINE], 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)phthalazinone [INN;

AZELASTINE], (+)-(S)-4-[4-[1-(4-chlorophenyl)-1-(2-pyridyl)methoxy]piperidin-1-yl]-butanoic acid [INN;

BEPOTASTINE], (plus/minus)-[2-[4-(p-chloro-alpha-phenylbenzyl)-1-piperazinyl]ethoxy]-acetic acid [INN;

CETIRIZINE], (+)-2-{2-[(p-Chlor-alpha-methyl-alpha phenylbenzyl)oxy]-ethyl}-1-methylpyrrolidin [INN;

CLEMASTINE], 8-chloro-6,11-dihydro-11-(4-piperidylidene)-5H-benzo[5,6]cyclohepta-[1,2-b]pyridine [INN;

DESLORATADINE], [3-(4-Chlorophenyl)-3-pyridin-2-yl-propyl]-dimethylamine [INN;

DEXCHLORPHENIRAMINE], 4′

-tert-butyl-4-[4-(diphenylmethoxy)-piperidino]butyrophenone [INN;

EBASTINE], [2-[4-[bis(p-fluorophenyl)methyl]-1-piperazinyl]ethoxy]-acetic acid [INN;

EFLETIRIZINE], 1-(2-ethoxyethyl)-2-(hexahydro-4-methyl-1H-1,4-diazepin-1-yl)-benzimidazole [INN;

EMEDASTINE], 3-amino-9,13b-dihydro-1H-dibenz[c,f]imidazo[1,5-a]azepine [INN;

EPINASTINE], (plus/minus)-p-[1-hydroxy-4-[4-(hydroxydiphenylmethyl)piperidino]-butyl]-alpha-methylhydratropic acid [INN;

FEXOFENADINE], 3-[4-(8-fluoro-5,11-dihydrobenz[b]oxepino[4,3-b]pyridin-11-ylidene)-piperidin-1-yl]propionic acid [Research Code;

HSR-609], (−

)-(3S,4R)-1-[cis4-cyano-4-(p-fluorophenyl)cyclohexyl]-3-methyl-4-phenylisonipecotic acid [INN;

LEVOCABASTINE], [2-[4-[(R)-p-chloro-alpha-phenylbenzyl)-1-piperazinyl]ethoxy]-acetic acid [INN;

LEVOCETIRIZINE], ethyl 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-1-piperidinecarboxylate [INN;

LORATADINE], 2-[N-[1-(4-fluorobenzyl)-1H-benzimidazol-2-yl]-4-piperidinyl]-N-methyl-amino]pyrimidin-4(3H)-one [INN;

MIZOLASTINE], 1-(4-fluorobenzyl)-2-(piperidin-4-ylamino)-1H-benzimidazole [INN;

NORASTEMIZOLE], 3-(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-ylidene)-N-methyl-1-propanamine [INN;

NORTRIPTYLINE], 9-methyl-3-(1H-tetrazol-5-yl)-4H-pyrido[1,2-a]pyrimidin-4-one [INN;

PEMIROLAST], 8-chloro-11-[1-(5-methylpyridin-3-ylmethyl)-piperidin-4-ylidene]-6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridine [INN;

RUPATADINE], 1-[2-[(p-chloro-alpha-methyl-alpha-phenylbenzyl)oxy]ethyl]hexahydro-1H-azepine [INN;

SETASTINE], S-(7-carboxy-4-hexyl-9-oxoxanthen-2-yl)-S-methylsulfoximine [INN;

SUDEXANOX], 1-(p-tert-butylphenyl)-4-[4′

-(alpha-hydroxydiphenylmethyl)-1′

-piperidyl]-butanol [INN;

TERFENADINE], N-benzyl-N,N′

-dimethyl-N(2-pyridyl)-ethylenediamine [INN;

TRIPELENAMINE] and 1-(4-fluorobenzyl)-2-(piperidin-4-ylamino)-1H-benzimidazole [INN;

TECASTEMIZOLE] and mixtures, stereoisomers thereof, pharmaceutically acceptable salts and/or solvates thereof.

16. Pharmaceutical composition according to claims 1 through 14, wherein the antihistamine is azelastine, levocabastine, a salt or solvate thereof.

17. Use of ciclesonide in combination with at least one antihistamine for the manufacture of a pharmaceutical composition for the treatment of allergic rhinitis and/or allergic conjunctivitis.

18. Method for the prophylaxis or treatment of allergic rhinitis and/or allergic conjunctivitis in a mammal, such as a human, which comprises administration of a therapeutically effective amount of a pharmaceutical formulation comprising at least one antihistamine or a pharmaceutical acceptable salt, solvate, or physiologically functional derivative thereof and ciclesonide or a pharmaceutical acceptable salt, solvate, or physiologically functional derivative thereof, and a pharmaceutical acceptable carrier and/or one or more excipients.