Combination of azelastine and mometasone for nasal administration

• US 8,318,709 B2
• Filed: 07/23/2009
• Issued: 11/27/2012
• Est. Priority Date: 06/14/2002
• Status: Expired due to Fees

• Current Assignee: Cipla (EU) Limited
• Original Assignee: Cipla (EU) Limited
• Inventors: Lulla, Amar, Malhotra, Geena
• Primary Examiner(s): Richter, Johann
• Assistant Examiner(s): Nielsen, Thor
• Application Number:
  US12/508,388
• Publication Number:
  US 20090291143A1
• Time in Patent Office: 1,223 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 pharmaceutical formulation comprising:

azelastine, or a pharmaceutically acceptable salt thereof, and

a pharmaceutically acceptable ester of mometasone, wherein said pharmaceutical formulation is in a dosage form suitable for nasal administration.

2. The pharmaceutical formulation according to claim 1, wherein said pharmaceutically acceptable salt of azelastine is azelastine hydrochloride.

3. The pharmaceutical formulation according to claim 1, wherein said pharmaceutically acceptable ester of mometasone is mometasone furoate or mometasone furoate monohydrate.

4. The pharmaceutical formulation according to claim 1, which contains from 0.001 to 1% (weight/weight of the formulation) of said azelastine, or a pharmaceutically acceptable salt thereof, and from 0.5% to 1.5% (weight/weight of the formulation) of said pharmaceutically acceptable ester of mometasone.

5. The pharmaceutical formulation according to claim 1, wherein said pharmaceutically acceptable salt of azelastine is azelastine hydrochloride and said pharmaceutically acceptable ester of mometasone is mometasone furoate.

6. The pharmaceutical formulation according to claim 1, wherein said pharmaceutically acceptable salt of azelastine is azelastine hydrochloride and said pharmaceutically acceptable ester of mometasone is mometasone furoate monohydrate.

7. The pharmaceutical formulation according to claim 1, which is an aqueous suspension or solution.

8. The pharmaceutical formulation according to claim 1, wherein said dosage form suitable for nasal administration comprises nasal drops or a nasal spray.

9. The pharmaceutical formulation according to claim 1, wherein said dosage form suitable for nasal administration comprises nasal drops.

10. The pharmaceutical formulation according to claim 1, wherein said dosage form suitable for nasal administration comprises nasal spray.

11. The pharmaceutical formulation according to claim 1, further comprising at least one additive selected from the group consisting of a buffer, a preservative, a suspending agent, a thickening agent, a surfactant, an isotonic agent, and combinations thereof.

12. The pharmaceutical formulation according to claim 11, wherein the buffer, when present, maintains the pH of the aqueous phase from 3 to 7.

13. The pharmaceutical formulation according to claim 11, wherein the surfactant, when present, comprises a polysorbate, poloxamer or combinations thereof.

14. The pharmaceutical formulation according to claim 11, wherein the isotonic agent, when present, comprises sodium chloride, saccharose, glucose, glycerine, sorbitol, 1,2-propylene glycol, or combinations thereof.

15. The pharmaceutical formulation according to claim 11, wherein said preservative, when present, comprises edetic acid and its alkali salts, lower alkyl p-hydroxybenzoates, chlorhexidine, phenyl mercury borate, benzoic acid or a salt, a quaternary ammonium compound, sorbic acid or a salt thereof, or combinations thereof.

16. The pharmaceutical formulation according to claim 11, wherein the suspending agent or thickening agent, when present, comprises cellulose derivatives, gelatin, polyvinylpyrrolidone, tragacanth, alginic acid, polyvinyl alcohol, polyacrylic acid, pectin, or combinations thereof.

17. The pharmaceutical formulation according to claim 11, wherein the buffer, when present, comprises a citric acid-citrate buffer.

18. A pharmaceutical product comprising (i) azelastine, or a pharmaceutically acceptable salt thereof, and (ii) a pharmaceutically acceptable ester of mometasone, as a combined preparation for use in medicine as an antihistamine and anti-inflammatory agent, said (i) azelastine, or a pharmaceutically acceptable salt thereof and (ii) said pharmaceutically acceptable ester of mometasone being in a dosage form suitable for nasal administration.

19. The pharmaceutical product according to claim 18, wherein said pharmaceutically acceptable salt of azelastine is azelastine hydrochloride and said pharmaceutically acceptable ester of mometasone is mometasone furoate.

20. The pharmaceutical product according to claim 18, wherein said pharmaceutically acceptable salt of azelastine is azelastine hydrochloride and said pharmaceutically acceptable ester of mometasone is mometasone furoate monohydrate.

21. The pharmaceutical product according to claim 18, wherein said product is formulated for use as a nasal spray in the treatment of seasonal allergic rhinitis or perennial allergic rhinitis.

22. The pharmaceutical product according to claim 18, wherein said product is formulated for use as nasal drops in the treatment of seasonal allergic conjunctivitis or perennial allergic conjunctivitis.