Ophthalmic Formulations Of Cetirizine And Methods Of Use

Abstract

The present invention provides stable topical formulations of cetirizine that provide a comfortable formulation when instilled in the eye and is effective in the treatment of allergic conjunctivitis and/or allergic conjunctivitis. The invention further provides methods of treating allergic conjunctivitis rhinitis, and/or allergic rhinoconjunctivitis in a subject in need of such treatment by topical application of the cetirizine formulations of the invention directly to the eye.

We claim: 
     
         1 . A topical ophthalmic formulation comprising about 0.1% cetirizine (w/v) or a pharmaceutically acceptable salt thereof and about 0.005% fluticasone (w/v). 
     
     
         2 . The ophthalmic formulation of  claim 1 , wherein the fluticasone is present as fluticasone propionate. 
     
     
         3 . The ophthalmic formulation of  claim 1 , wherein the cetirizine is present as cetirizine hydrochloride or dihydrochloride. 
     
     
         4 . The ophthalmic formulation of  claim 1 , further comprising glycerin. 
     
     
         5 . The ophthalmic formulation of  claim 4 , wherein the glycerin is at a concentration of 0.1% to 3% (v/v). 
     
     
         6 . The ophthalmic formulation of  claim 1 , further comprising a preservative. 
     
     
         7 . The ophthalmic formulation of  claim 6 , wherein the preservative is benzalkonium chloride or a derivative thereof, or a stabilized, oxychloro complex. 
     
     
         8 . The ophthalmic formulation of  claim 7 , wherein the preservative is benzalkonium chloride present in amount ranging from 0.005% to 0.02% (v/v). 
     
     
         9 . The ophthalmic formulation of  claim 1 , wherein the pH of the composition is about 5.0 to 8.0. 
     
     
         10 . The ophthalmic formulation of  claim 1 , wherein the formulation is an aqueous formulation, an ointment, oil, a suspension, an emulsion, or incorporated in a drug delivery device. 
     
     
         11 . The ophthalmic formulation of  claim 9 , wherein the formulation is in an aqueous formulation. 
     
     
         12 . The ophthalmic formulation of  claim 1 , wherein the cetirizine is in solution and the Fluticasone is in suspension. 
     
     
         13 . A topical ophthalmic formulation comprising 0.1% cetirizine (w/v), 0.005% fluticasone (w/v), 1% Polyethylene Glycol 400, NF, 0.2% Dibasic Sodium Phosphate, Anhydrous, USP, 0.25% Hypromellose, USP, 0.1% Polysorbate 80, NF, 1.8% Glycerin, USP, 0.025% Edetate Disodium, USP, 0.01% Benzalkonium Chloride, NF. 
     
     
         14 . The formulation of  claim 13 , wherein the pH is about 5.0-8.0 
     
     
         15 . The formulation of  claim 13 , wherein the pH is 7.0. 
     
     
         16 . A method of treating a sign or symptom of an allergic disorder by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of  claim 1 . 
     
     
         17 . The method of  claim 16 , wherein the allergic disorder is against an airborne allergen. 
     
     
         18 . The method of  claim 16 , wherein the allergic disorder is an ocular allergy or a nasal allergy. 
     
     
         19 . The method of  claim 16 , wherein the sign or symptom is selected from the group comprising, ocular itching, redness, lid swelling, chemosis, tearing rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear itching, redness, lid swelling, chemosis, tearing rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear. 
     
     
         20 . The method of  claim 16 , wherein the allergic disorder is allergic conjunctivitis, allergic rhinoconjunctivitis or rhinitis 
     
     
         21 . A method for treating a sign or a symptom of allergic conjunctivitis by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of  claim 1 . 
     
     
         22 . The method of  claim 21 , wherein said sign and symptom is selected from the group consisting of ocular itching, redness, lid swelling, chemosis or tearing. 
     
     
         23 . A method for treating a sign or a symptom of allergic rhinoconjunctivitis by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of  claim 1 . 
     
     
         24 . The method of  claim 23 , wherein said sign and symptom is selected from the group consisting of ocular itching, redness, lid swelling, chemosis, tearing, rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear. 
     
     
         25 . A method for treating a sign or a symptom of rhinitis by topically administering to the eye of a subject in need of such treatment the ophthalmic formulation of  claim 1 . 
     
     
         26 . The method of  claim 25 , wherein said sign and symptom is selected from the group consisting of rhinorrhea, sneezing, nasal congestion, nasal itching, itching of the palate, or itching of the ear. 
     
     
         27 . The method of  claim 16 , wherein the ophthalmic formulation is administered once or twice daily.