Combination of azelastine and ciclesonide for nasal administration

• US 8,933,060 B2
• Filed: 10/03/2012
• Issued: 01/13/2015
• Est. Priority Date: 06/14/2002
• Status: Expired due to Term

• Current Assignee: Cipla (EU) Limited
• Original Assignee: Cipla (EU) Limited
• Inventors: Lulla, Amar, Malhotra, Geena
• Primary Examiner(s): Liu, Sue
• Assistant Examiner(s): NIELSEN, THOR B
• Application Number:
  US13/644,126
• Publication Number:
  US 20130029951A1
• Time in Patent Office: 832 Days
• Field of Search: None
• 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 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 31/56 Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
• CPC Class Codes: A61K 31/573 substituted in position 21, e.g. cortisone, dexamethasone, prednisone or aldosterone
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• 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 47/26 Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
• CPC Class Codes: A61K 47/38 Cellulose; Derivatives thereof
• CPC Class Codes: A61K 9/0043 Nose
• CPC Class Codes: A61K 9/10 Dispersions; Emulsions A61K9/06 takes precedence; composition of dispersions, emulsions A61K47/00
• 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 11/06 Antiasthmatics
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• 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

Abstract

A pharmaceutical product or formulation, which comprises azelastine or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and a steroid, or a pharmaceutical acceptable salt, solvate or physiologically functional derivative thereof, preferably the product or formulation being in a form suitable for nasal or ocular administration.

Claims

1. A method for the prophylaxis or treatment of rhinitis or conjunctivitis in a mammal, comprising intranasal administration to said mammal of a therapeutically effective amount of a pharmaceutical composition comprising (a) azelastine, or a pharmaceutically acceptable salt thereof;

and (b) and ciclesonide, or a pharmaceutically acceptable salt or ester thereof.

2. The method of claim 1, wherein the pharmaceutical composition comprises a dosage form suitable for nasal administration.

3. The method of claim 2, wherein the dosage form suitable for nasal administration is in the form of an aerosol, an ointment, nasal drops, or a nasal spray or an inhalation solution.

4. The method of claim 2, wherein the pharmaceutical composition is in the form of a nasal spray.

5. The method of claim 2, wherein the pharmaceutical composition is in the form of nasal drops.

6. The method of claim 1, wherein the pharmaceutical composition is in the form of an aqueous suspension or solution.

7. The method of claim 1, wherein the pharmaceutical composition has a particle size of less than 10 μ

m.

8. The method of claim 1, wherein the pharmaceutically acceptable salt of azelastine is azelastine hydrochloride.

9. The method of claim 1, wherein the pharmaceutical composition further comprises at least one additive selected from the group consisting of a surfactant, an isotonic agent, a buffer, a preservative, and a suspending agent or a thickening agent, and combinations thereof.

10. The method of claim 9, wherein the surfactant is selected from the group consisting of a polysorbate surfactant, a poloxamer surfactant, and combinations thereof.

11. The method of claim 9, wherein the isotonic agent is selected from the group consisting of sodium chloride, saccharose, glucose, glycerine, sorbitol, 1,2-propylene glycol, and combinations thereof.

12. The method of claim 9, wherein the buffer comprises a citric acid-citrate buffer.

13. The method of claim 9, wherein the preservative is selected from the group consisting of edetic acid and its alkali salts, lower alkyl p-hydroxybenzoates, chlorhexidine, phenyl mercury borate, benzoic acid or a salt thereof, a quaternary ammonium compound, sorbic acid or a salt thereof, and combinations thereof.

14. The method of claim 9, wherein the suspending agent or thickening agent is selected from the group consisting of cellulose derivatives, gelatin, polyvinylpyrrolidone, tragacanth, ethoxose, alginic acid, polyvinyl alcohol, polyacrylic acid, pectin, and combinations thereof.

15. The method of claim 9, wherein the buffer, when present, maintains the pH of the aqueous phase at from 3 to 7.

16. The method of claim 1, wherein the mammal is a human.

17. The method of claim 1, wherein the method is prophylaxis or treatment of allergic rhinitis.

18. The method of claim 1, wherein the method is prophylaxis or treatment of allergic conjunctivitis.

19. The method of claim 1, wherein the pharmaceutical composition is formulated for use as a nasal spray or nasal drops in the treatment of seasonal allergic rhinitis or perennial allergic rhinitis.

20. The method of claim 1, wherein the pharmaceutical composition is formulated for use as nasal spray or nasal drops in the treatment of seasonal allergic conjunctivitis or perennial allergic conjunctivitis.

21. The method of claim 8, wherein the pharmaceutical composition is formulated for use as a nasal spray or nasal drops in the treatment of seasonal allergic rhinitis or perennial allergic rhinitis.

22. The method of claim 8, wherein the pharmaceutical composition is formulated for use as nasal spray or nasal drops in the treatment of seasonal allergic conjunctivitis or perennial allergic conjunctivitis.

23. The method of claim 1, wherein the method is prophylaxis or treatment of seasonal allergic rhinitis.

24. The method of claim 1, wherein the method is prophylaxis or treatment of perennial allergic rhinitis.

25. The method of claim 1, wherein the method is prophylaxis or treatment of seasonal allergic conjunctivitis,

26. The method of claim 1, wherein the method is prophylaxis or treatment of perennial allergic conjunctivitis.