Pharmaceutical Formulations Comprising Azelastine and a Corticosteroid for the Treatment of Inflammatory or Allergic Conditions

• US 20090286762A1
• Filed: 07/26/2007
• Published: 11/19/2009
• Est. Priority Date: 07/28/2006
• Status: Abandoned Application

• Current Assignee: Glaxo Group Limited (Glaxosmithkline Holdings Ltd.)
• Original Assignee: Glaxo Group Limited (Glaxosmithkline Holdings Ltd.)
• Inventors: Richards, David Hugh, Myles, David Douglas
• Application Number:
  US12/374,523
• Publication Number:
  US 20090286762A1
• 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 31/55 having seven-membered rings, e.g. azelastine, pentylenetetrazole
• CPC Class Codes: A61K 31/58 containing heterocyclic rings, e.g. danazol, stanozolol, pancuronium or digitogenin digitoxin A61K31/7048
• 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 11/06 Antiasthmatics
• CPC Class Codes: A61P 17/00 Drugs for dermatological disorders
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
• 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 pharmaceutical formulations comprising an anti-inflammatory glucocorticoid compound of formula (II), (III), (IV)

or a solvate thereof
and a compound for formula (I)

or a salt or solvate thereof.

The present invention also relates to therapeutic uses thereof, particularly for the treatment of inflammatory and allergic conditions, specifically rhinitis.

Claims

1-38. -38. (canceled)

39. A pharmaceutical formulation comprising a compound of formula (I)

or a salt or solvate thereof

and a corticosteroid of formula (II)

or a solvate thereof.

40. A pharmaceutical formulation according to claim 39 wherein the compound of formula (II) is 6α

,9α

-difluoro-17α

-[(2-furanylcarbonyl)oxy]-11β

-hydroxy-16α

-methyl -3-oxo-androsta-1,4-diene-17β

-carbothioic acid S-fluoromethyl ester.

41. A pharmaceutical formulation according to claim 39 wherein the compound of formula (I) is azelastine either in racemic form or a single enantiomer thereof.

42. A pharmaceutical formulation according to claim 41 wherein the azelastine is present as the hydrochloride salt.

43. A pharmaceutical formulation according to claim 39 which further comprises one or more suspending agents.

44. A pharmaceutical formulation according to claim 39 which comprises one or more preservatives.

45. A pharmaceutical formulation according to claim 39 which comprises one or more wetting agents.

46. A pharmaceutical formulation according to claim 39 which comprises one or more isotonicity adjusting agents.

47. A pharmaceutical formulation according to claim 39 which comprises a buffer.

48. A pharmaceutical formulation according to claim 39 which comprises one or more taste-masking agents.

49. A pharmaceutical formulation according to claim 39 wherein the compound of formula (II) or solvate thereof is present within the formulation in an amount of from 0.005% to 1% (w/w), based on the total weight of the formulation.

50. A pharmaceutical formulation according to claim 39 wherein the compound of formula (I) or a salt or solvate thereof is present within the formulation in an amount of from 0.0005% to 2% (w/w), based on the total weight of the formulation.

51. A pharmaceutical formulation according to claim 39 which comprises

(i) an aqueous solution of a compound of formula (I) or a salt or solvate thereof;

(ii) an aqueous suspension of a corticosteroid which is a compound of formula (II);

(iii) one or more suspending agents;

(iv) one or more preservatives;

(v) one or more wetting agents;

(vi) a buffer;

(vii) one or more isotonicity adjusting agents; and

optionally

(viii) one or more taste-masking agents.

52. A method of treatment of allergic rhinitis which comprises administering to a patient a pharmaceutically acceptable amount of a pharmaceutical formulation according to claim 39.

53. The method according to claim 52 wherein the administration is once-per-day.

54. A method for the treatment of a human or animal subject with an inflammatory and/or allergic condition, which method comprises administering to said human or animal subject an effective amount of a pharmaceutical formulation according to claim 39.