Compositions comprising azelastine and methods of use thereof

Abstract

The present invention provides pharmaceutical compositions comprising azelastine, or a pharmaceutically acceptable salt or ester thereof including azelastine hydrochloride, and optionally one or more additional active agents. Preferred such compositions further comprise one or more pharmaceutically acceptable carriers or excipients that reduce the amount of post-nasal drip, and/or that minimize or mask the unpleasant bitter taste associated with post-nasal drip, of the compositions into the oral cavity, upon intranasal or ocular administration of the compositions. Especially effective excipients used in the compositions of the present invention are hypromellose as a viscosity modifier and sucralose as a taste-masking agent. The invention also provides methods of treating or preventing certain disorders, or symptomatic relief therefrom, by administering the compositions of the invention to a patient, e.g., for the symptomatic relief of allergic rhinitis, non-allergic vasomotor rhinitis, allergic conjunctivitis, as well as other disorders. The compositions and methods of the present invention provide significant value in terms of patient acceptability, convenience, and compliance.

1 . A pharmaceutical composition comprising a therapeutically effective dose of azelastine, or a pharmaceutically acceptable salt or ester thereof, at a concentration of from about 0.05% to about 5% by weight, one or more steroids, and one or more pharmaceutically acceptable carriers or excipients.  
   
   
       2 . The pharmaceutical composition of  claim 1 , wherein at least one of said pharmaceutically acceptable carriers or excipients is sucralose.  
   
   
       3 . The pharmaceutical composition of  claim 1 , wherein said one or more steroids are selected from the group consisting of fluoromethalone, a fluticasone, mometasone, triamcinolone, betamethasone, flunisolide, budesonide, beclomethasone, budesonide, rimexolone, a loteprednol, beloxil, prednisone and dexamethasone.  
   
   
       4 . The pharmaceutical composition of  claim 3 , wherein said fluticasone is fluticasone propionate.  
   
   
       5 . The pharmaceutical composition of  claim 3 , wherein said loteprednol is loteprednol etabonate.  
   
   
       6 . The pharmaceutical composition of  claim 1 , further comprising one or more additional active agents selected from the group consisting of one or more decongestants, one or more antihistamines, one or more non-steroidal anti-inflammatory agents and one or more leukotriene antagonists.  
   
   
       7 . The pharmaceutical composition of  claim 1 , wherein said azelastine is present in said composition at a concentration of from about 0.125% to about 0.15% by weight.  
   
   
       8 . The pharmaceutical composition of  claim 2 , wherein said sucralose is present in said composition at a concentration of from about 0.05% to about 0.15% by weight.  
   
   
       9 . The pharmaceutical composition of  claim 1 , wherein said composition is formulated for intranasal administration.  
   
   
       10 . A method of treating or preventing allergic rhinitis, non-allergic vasomotor rhinitis or allergic conjunctivitis in an animal suffering from or predisposed thereto, comprising administering an effective amount of the composition of  claim 1  to the animal.  
   
   
       11 . A method of treating or preventing allergic rhinitis, non-allergic vasomotor rhinitis or allergic conjunctivitis in an animal suffering from or predisposed thereto, comprising co-administering to said animal an effective amount of azelastine and an effective amount of one or more steroids.  
   
   
       12 . The method of  claim 11 , wherein the animal is a mammal.  
   
   
       13 . The method of  claim 12 , wherein the mammal is a human.  
   
   
       14 . The method of  claim 11 , wherein the azelastine is azelastine HCl.  
   
   
       15 . The method of  claim 11 , wherein the steroid is selected from the group consisting of fluoromethalone, a fluticasone, mometasone, triamcinolone, betamethasone, flunisolide, budesonide, beclomethasone, budesonide, rimexolone, a loteprednol, beloxil, prednisone and dexamethasone.  
   
   
       16 . The method of  claim 15 , wherein the fluticasone is fluticasone propionate.  
   
   
       17 . The method of  claim 11 , wherein said co-administration comprises administering the azelastine and the one or more steroids simultaneously.  
   
   
       18 . The method of  claim 11 , wherein said co-administration comprises administering azelastine and the one or more steroids separately, within less than about 30 minutes of each other.  
   
   
       19 . The method of  claim 18 , wherein said co-administration comprises administering azelastine and the one or more steroids separately, within less than about 20 minutes of each other.  
   
   
       20 . The method of  claim 19 , wherein said co-administration comprises administering azelastine and the one or more steroids separately, within less than about 15 minutes of each other.  
   
   
       21 . The method of  claim 11 , wherein said co-administration comprises administering the azelastine before the one or more steroids.  
   
   
       22 . The method of  claim 11 , wherein said co-administration comprises administering the one or more steroids before the azelastine.  
   
   
       23 . The method of  claim 11 , wherein said co-administration comprises administering the azelastine and the one or more steroids to the nasal passage.  
   
   
       24 . The method of  claim 11 , wherein said co-administration comprises administering the azelastine and said the or more steroids in the form of a single pharmaceutical composition comprising azelastine and one or more steroids.  
   
   
       25 . The method of  claim 11 , wherein said co-administration comprises administering the azelastine and the one or more steroids separately, in the form of two separate pharmaceutical compositions, one pharmaceutical composition comprising azelastine and a second pharmaceutical composition comprising one or more steroids.  
   
   
       26 . A method of treating or preventing allergic rhinitis, non-allergic vasomotor rhinitis or allergic conjunctivitis in an animal suffering from or predisposed thereto, comprising co-administering to said animal an effective amount of azelastine and an effective amount of a fluticasone.  
   
   
       27 . The method of  claim 26 , wherein the animal is a mammal.  
   
   
       28 . The method of  claim 27 , wherein the mammal is a human.  
   
   
       29 . The method of  claim 26 , wherein the azelastine is azelastine HCl.  
   
   
       30 . The method of  claim 26 , wherein the fluticasone is fluticasone propionate.  
   
   
       31 . The method of  claim 26 , wherein said co-administration comprises administering the azelastine and the fluticasone simultaneously.  
   
   
       32 . The method of  claim 26 , wherein said co-administration comprises administering the azelastine and the fluticasone separately, within less than about 30 minutes of each other.  
   
   
       33 . The method of  claim 32 , wherein said co-administration comprises administering the azelastine and the fluticasone separately, within less than about 20 minutes of each other.  
   
   
       34 . The method of  claim 33 , wherein said co-administration comprises administering the azelastine and the fluticasone separately, within about 15 minutes of each other.  
   
   
       35 . The method of  claim 26 , wherein said co-administration comprises administering the azelastine before the fluticasone.  
   
   
       36 . The method of  claim 26 , wherein said co-administration comprises administering the fluticasone before the azelastine.  
   
   
       37 . The method of  claim 26 , wherein said co-administration comprises administering the azelastine and the fluticasone to the nasal passage.  
   
   
       38 . The method of  claim 26 , wherein said co-administration comprises administering the azelastine and the fluticasone in the form of a single pharmaceutical composition comprising azelastine and fluticasone.  
   
   
       39 . The method of  claim 26 , wherein said co-administration comprises administering the azelastine and the fluticasone separately, in the form of two separate pharmaceutical compositions, one pharmaceutical composition comprising azelastine and a second pharmaceutical composition comprising fluticasone.  
   
   
       40 . A method of treating or preventing allergic rhinitis, non-allergic vasomotor rhinitis or allergic conjunctivitis in an animal suffering from or predisposed thereto, comprising co-administering to said animal an effective amount of azelastine HCl and an effective amount of fluticasone propionate separately, in the form of two separate pharmaceutical compositions, one pharmaceutical composition comprising azelastine HCl and a second pharmaceutical composition comprising fluticasone propionate, wherein the two pharmaceutical compositions are administered within about 30 minutes of each other.