Stable cyclosporine containing ophthalmic emulsion for treating dry eyes

Abstract

Disclosed herein are stable oil-in-water emulsion ophthalmic topical liquid compositions having an average particle size less than 1 μm including at least one plant-derived oil other than castor oil wherein the oil comprises only aliphatic side chains free of polar pendent groups. The oil-in-water emulsion ophthalmic topical liquid compositions also include a hydrophilic surfactant having an HLB value between approximately 10 and 14, a vegetable oil-derived hydrophobic non-co-block surfactant having unsaturated side chains that contain less than four oxygen atoms having an HLB value between approximately 4 and 6 and is a liquid at room temperature. The oil-in-water emulsion ophthalmic topical liquid compositions disclosed herein can further include an amount of cyclosporine A effective to relieve dry eye symptoms.

1 . A stable oil-in-water emulsion ophthalmic topical liquid composition having an average particle size less than 1 μm comprising:
 at least one plant-derived oil other than castor oil wherein said oil comprises only aliphatic side chains free of polar pendent groups;   a hydrophilic surfactant having an HLB value between approximately 10 and 14;   a vegetable oil-derived hydrophobic non-co-block surfactant having unsaturated side chains that contain less than four oxygen atoms, an HLB value between approximately 4 and 6 and is a liquid at room temperature; and   wherein in said ophthalmic composition further comprises an amount of cyclosporine A effective to relieve dry eye symptoms.   
     
     
         2 . The ophthalmic composition according to  claim 1  wherein the hydrophilic surfactant is Lumulse® GRH-25 and the hydrophobic surfactant is Brij 93. 
     
     
         3 . The ophthalmic composition according to  claim 1  wherein the plant-derived non-polar oil is sesame oil. 
     
     
         4 . A stable oil-in-water emulsion ophthalmic topical liquid composition having an average particle size less than 0.6 μm consisting essentially of:
 at least one plant-derived oil other than castor oil wherein said oil comprises aliphatic side chains free of polar pendent groups;   a hydrophilic surfactant having an HLB value between approximately 10 and 11;
 a vegetable oil-derived hydrophobic non-co-block surfactant having unsaturated side chains that contain less than four oxygen atoms, an HLB value between approximately 4 and 6 and is a liquid at room temperature; and 
 wherein in said ophthalmic composition further comprises an amount of cyclosporine A effective to relieve dry eye symptoms. 
   
     
     
         5 . The ophthalmic composition according to  claim 4  wherein the hydrophilic surfactant is Lumulse® GRH-25 and the hydrophobic surfactant is Brij 93. 
     
     
         6 . The ophthalmic composition according to  claim 4  wherein the plant-derived non-polar oil is sesame oil. 
     
     
         7 . A stable oil-in-water emulsion ophthalmic topical liquid composition having an average particle size less than 0.6 μm consisting essentially of sesame oil, a hydrophilic surfactant consisting of Lumulse® GRH-25, a hydrophobic non-co-block surfactant consisting of Brij 93 and wherein in said ophthalmic composition further comprises an amount of cyclosporine A effective to relieve dry eye symptoms.