Compositions and methods for treating a posterior segment of an eye

Abstract

Compositions, and methods of using such compositions, useful for injection into the posterior segments of human or animal eyes are provided. Such compositions include corticosteroid component-containing particles present in a therapeutically effective amount, a viscosity inducing component, and an aqueous carrier component. The compositions have viscosities of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity is in the range of from about 140,000 cps to about 300,000 cps. The compositions advantageously suspend the particles for prolonged periods of time.

1 . A composition useful for injection into a posterior segment of an eye of a human or animal comprising: 
 a corticosteroid component present in a therapeutically effective amount, the corticosteroid component being present in a plurality of particles;    a viscosity inducing component in an amount effective in increasing the viscosity of the composition; and    an aqueous carrier component, the composition having a viscosity of at least about 10 cps at a shear rate of 0.1/second and being effectively injectable into a posterior segment of an eye of a human or animal.    
     
     
         2 . The composition of  claim 1  which has a viscosity of at least 100 cps at a shear rate of 0.1/second.  
     
     
         3 . The composition of  claim 1  which has a viscosity of at least 10,000 cps at a shear rate of 0.1/second.  
     
     
         4 . The composition of  claim 1  which has a viscosity of from about 140,000 cps—about 300,000 cps at a shear rate of 0.1/second.  
     
     
         5 . The composition of  claim 1  which is effectively injectable through a 27 gauge needle into a posterior segment of an eye of a human or animal.  
     
     
         6 . The composition of  claim 1  which is effectively injectable through a 30 gauge needle into a posterior segment of an eye of a human or animal.  
     
     
         7 . The composition of  claim 1  wherein the particles are substantially uniformly suspended in the composition.  
     
     
         8 . The composition of  claim 7  wherein the particles remain substantially uniformly suspended in the composition for at least about 1 week without requiring resuspension processing.  
     
     
         9 . The composition of  claim 7  wherein the particles remain substantially uniformly suspended in the composition for at least about 1 month without requiring resuspension processing.  
     
     
         10 . The composition of  claim 7  wherein the particles remain substantially uniformly suspended in the composition for at least about 6 months without requiring resuspension processing.  
     
     
         11 . The composition of  claim 7  wherein the particles remain substantially uniformly suspended in the composition for at least about 1 year without requiring resuspension processing.  
     
     
         12 . The composition of  claim 7  wherein the particles remain substantially uniformly suspended in the composition for at least about 2 years without requiring resuspension processing.  
     
     
         13 . The composition of  claim 1  wherein the corticosteroid component is present in an amount of up to about 25% (w/v) of the composition.  
     
     
         14 . The composition of  claim 1  wherein the corticosteroid component is present in an amount of at least about 10 mg per ml of composition.  
     
     
         15 . The composition of  claim 1  wherein the corticosteroid component is present in an amount in a range of about 1% to about 20% (w/v) of the composition.  
     
     
         16 . The composition of  claim 1  wherein the corticosteroid component is present in an amount in a range of about 1% to about 10% (w/v) of the composition.  
     
     
         17 . The composition of  claim 1  wherein the corticosteroid component has a solubility in water at 25° C. of less than 10 mg/ml.  
     
     
         18 . The composition of  claim 1  wherein the corticosteroid component is selected from the group consisting of cortisone, prednisolone, triamcinolone, fluorometholone, dexamethasone, medrysone, loteprednol, derivatives thereof and mixtures thereof.  
     
     
         19 . The composition of  claim 1  wherein the corticosteroid component is triamcinolone acetonide.  
     
     
         20 . The composition of  claim 1  wherein the carrier component includes an effective amount of at least one of a preservative component, a tonicity component and a buffer component.  
     
     
         21 . The composition of  claim 1  which includes no added preservative component.  
     
     
         22 . The composition of  claim 1  which includes no added resuspension component.  
     
     
         23 . The composition of  claim 1  wherein the viscosity inducing component is present in an amount in a range of about 0.05% to about 20% (w/v) of the composition.  
     
     
         24 . The composition of  claim 1  wherein the viscosity inducing component comprises a polymeric component.  
     
     
         25 . The composition of  claim 1  wherein the viscosity inducing component comprises at least one viscoelastic agent.  
     
     
         26 . The composition of  claim 1  wherein the viscosity inducing component is selected from the group consisting of polymeric hyaluronic acid, carbomers, polyacrylic acid, cellulosic derivatives, polycarbophil, polyvinylpyrrolidone, gelatin, dextrin, polysaccharides, polyacrylamide, polyvinyl alcohol, polyvinyl acetate, derivatives thereof and mixtures thereof.  
     
     
         27 . The composition of  claim 1  wherein the viscosity inducing component comprises a hyaluronate component.  
     
     
         28 . The composition of  claim 27  wherein the hyaluronate component comprises sodium hyaluronate.  
     
     
         29 . A method of treatment comprising administering the composition of  claim 1  to a posterior segment of an eye of a human or animal, thereby obtaining a desired therapeutic effect.  
     
     
         30 . The method of  claim 29  wherein the administering step comprises intravitreal injecting.  
     
     
         31 . The method of  claim 29  wherein the administering step comprises subconjunctival injecting.  
     
     
         32 . The method of  claim 29  wherein the administering step comprises sub-tenon injecting.  
     
     
         33 . The method of  claim 29  wherein the administering step comprises retrobulbar injecting.  
     
     
         34 . The method of  claim 29  wherein the administering step comprises suprachoroidal injecting.  
     
     
         35 . A composition useful for injection into a posterior segment of an eye of a human or animal comprising: 
 a corticosteroid component present in a therapeutic effect amount, the corticosteroid component being present in a plurality of particles;    a viscosity inducing component in an amount effective in increasing the viscosity of the composition; and    an aqueous carrier component, the particles being substantially uniformly suspended in the composition and remaining substantially uniformly suspended in the composition for at least about 1 week without requiring resuspension processing.    
     
     
         36 . The composition of  claim 35  wherein the particles remain substantially uniformly suspended in the composition for at least about 2 weeks without requiring resuspension processing.  
     
     
         37 . The composition of  claim 35  wherein the particles remain substantially uniformly suspended in the composition for at least about 1 month without requiring resuspension processing.  
     
     
         38 . The composition of  claim 35  wherein the particles remain substantially uniformly suspended in the composition for at least about 6 months without requiring resuspension processing.  
     
     
         39 . The composition of  claim 35  wherein the particles remain substantially uniformly suspended in the composition for at least about 1 year without requiring resuspension processing.  
     
     
         40 . The composition of  claim 35  wherein the particles remain substantially uniformly suspended in the composition for at least about 2 years without requiring resuspension processing.  
     
     
         41 . The composition of  claim 35  wherein the corticosteroid component is present in an amount of up to about 25% (w/v) of the composition.  
     
     
         42 . The composition of  claim 35  wherein the corticosteroid component is present in an amount of at least about 10 mg per ml of composition.  
     
     
         43 . The composition of  claim 35  wherein the corticosteroid component is present in an amount in a range of about 1% to about 20% (w/v) of the composition.  
     
     
         44 . The composition of  claim 35  wherein the corticosteroid component is present in an amount in a range of about 1% to about 10% (w/v) of the composition.  
     
     
         45 . The composition of  claim 35  wherein the corticosteroid component has a solubility in water at 25° C. of less than 10 mg/ml.  
     
     
         46 . The composition of  claim 35  wherein the corticosteroid component is selected from the group consisting of cortisone, prednisolone, triamcinolone, fluorometholone, dexamethasone, medrysone, loteprednol, derivatives thereof and mixtures thereof.  
     
     
         47 . The composition of  claim 35  wherein the corticosteroid component is triamcinolone acetonide.  
     
     
         48 . The composition of  claim 35  wherein the carrier component includes an effective amount of at least one of a preservative component, a tonicity component and a buffer component.  
     
     
         49 . The composition of  claim 35  which includes no added preservative component.  
     
     
         50 . The composition of  claim 35  which includes no added resuspension component.  
     
     
         51 . The composition of  claim 35  wherein the viscosity inducing component is present in an amount in a range of about 0.05% to about 20% (w/v) of the composition.  
     
     
         52 . The composition of  claim 35  wherein the viscosity inducing component comprises a polymeric component.  
     
     
         53 . The composition of  claim 35  wherein the viscosity inducing component comprises at least one viscoelastic agent.  
     
     
         54 . The composition of  claim 35  wherein the viscosity inducing component is selected from the group consisting of polymeric hyaluronic acid, carbomers, polyacrylic acid, cellulosic derivatives, polycarbophil, polyvinylpyrrolidone, gelatin, dextrin, polysaccharides, polyacrylamide, polyvinyl alcohol, polyvinyl acetate, derivatives thereof and mixtures thereof.  
     
     
         55 . The composition of  claim 35  wherein the viscosity inducing component comprises a hyaluronate component.  
     
     
         56 . The composition of  claim 55  wherein the hyaluronate component comprises sodium hyaluronate.  
     
     
         57 . A method of treatment comprising administering the composition of  claim 35  to a posterior segment of an eye of a human or animal, thereby obtaining a desired therapeutic effect.  
     
     
         58 . The method of  claim 57  wherein the administering step comprises intravitreal injecting.  
     
     
         59 . The method of  claim 57  wherein the administering step comprises subconjunctival injecting.  
     
     
         60 . The method of  claim 57  wherein the administering step comprises sub-tenon injecting.  
     
     
         61 . The method of  claim 57  wherein the administering step comprises retrobulbar injecting.  
     
     
         62 . The method of  claim 57  wherein the administering step comprises suprachoroidal injecting.