Bromfenac bioavailability

Abstract

Formulations and methods that provided enhanced bromfenac penetration into ocular tissue when topically administered, compared to the currently available BROMDAY™ formulation and method when topically administered. The formulations and methods did so while retaining the patient convenience of a once-daily administration and advantageously lowered the bromfenac concentration dosed to the patient.

What is claimed is: 
     
         1 . A method for treating a patient in need thereof with a bromfenac formulation comprising bromofenac as a free acid, the method comprising:
 correlating bromfenac pH with bromfenac therapy but not bromfenac concentration by topically ocularly administering to the patient in need thereof the bromfenac formulation within a pH range between pH>6.0 and pH<8.3 and the bromfenac at a concentration between ≥0.02% w/v and ≤0.20% w/v,   wherein the pH range results in a bromfenac efficacy that is at least equal to an efficacy of bromfenac at 0.09% w/v and pH 8.3, and bromfenac is the only active.   
     
     
         2 . The method of  claim 1 , wherein the bromfenac formulation contains >0.02% w/v and <0.20% bromfenac. 
     
     
         3 . The method of  claim 1 , wherein the bromfenac formulation contains <0.09% w/v bromfenac. 
     
     
         4 . The method of  claim 1 , wherein the bromfenac formulation is within a pH range between pH≥7.0 and ≤7.8. 
     
     
         5 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.0. 
     
     
         6 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.1. 
     
     
         7 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.2. 
     
     
         8 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.3. 
     
     
         9 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.4. 
     
     
         10 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.5. 
     
     
         11 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.6. 
     
     
         12 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.7. 
     
     
         13 . The method of  claim 1 , wherein the bromfenac formulation comprises 0.07% w/v bromfenac at pH 7.8. 
     
     
         14 . The method of  claim 1 , wherein the bromfenac formulation further comprises tyloxapol, sodium sulfite, benzalkonium chloride, or a mixture thereof. 
     
     
         15 . The method of  claim 1 , wherein the bromfenac formulation further comprises tyloxapol at a concentration of 0.01% w/v to 0.5% w/v, sodium sulfite, benzalkonium chloride at a concentration of ≤0.01% w/v, or a mixture thereof. 
     
     
         16 . A method for treating a patient in need thereof with bromfenac as a free acid, the method comprising:
 (a) topically administering a first dose of bromfenac as the only active to an eye of the patient in need thereof, the bromfenac in a formulation where pH is >6.0 and <8.3 and where the bromfenac concentration is less than 0.09% w/v,   (b) administering at least a second dose of bromfenac to the eye of the patient in need thereof at a longer interval that exceeds twice a day administration of 0.09% w/v bromfenac at a pH>8.3, and   (c) assessing equal or greater efficacy in the patient administered bromfenac doses at the longer interval in the absence of bromfenac concentrations ≥0.09% w/v.   
     
     
         17 . The method of  claim 16 , wherein the formulation is within a pH range between pH≥7.0 and ≤7.8. 
     
     
         18 . The method of  claim 16 , wherein the formulation comprises 0.07% w/v bromfenac. 
     
     
         19 . The method of  claim 16 , wherein the formulation further comprises tyloxapol, sodium sulfite, benzalkonium chloride, or a mixture thereof. 
     
     
         20 . The method of  claim 16 , wherein the formulation further comprises tyloxapol at a concentration of 0.01% w/v to 0.5% w/v, sodium sulfite, benzalkonium chloride at a concentration of ≤0.01% w/v, or a mixture thereof.