Method of preparing a latanoprost ophthalmic solution and the resulting solution

Abstract

A method of solubilizing an analog active agent of the prostaglandin F2α, such as latanoprost, is described and a method of preparing an ophthalmic solution of the solubilized latanoprost for the treatment of distinct ocular ailments. This invention also refers to an ophthalmic aqueous solution resulting from the aforementioned method, which is characterized by its chemical stability at room temperature, its safety, and innocuousness and efficiency in the treatment of the patient. The new ophthalmic aqueous solution is distinguished because its pharmaceutical value is found in the handling of a vehicle of easy access that not only permits the solubility of latanoprost, but also promotes its chemical stability and, a greater tolerance of the patient with its ophthalmic application for the treatment of the patient's ailment.

1 - 6 . (canceled) 
     
     
         7 . An ophthalmic solution for the treatment of ocular ailments, prepared by means of the method disclosed in the preceding claims, which comprises: an analog drug of the prostaglandalin, such as latanoprost, at a concentration of approximately 0.005%; a solubilizing agent deriving from the cyclodextrins, at a concentration of approximately 7.5%; a viscosity agent and lubricator, such as hyaluronic acid at 0.2%; a pH damper system such as sodium phosphate; and a preservative agent such as benzalkonium chloride at 0.02%. 
     
     
         8 . The ophthalmic solution of  claim 7 , which is chemically stable at room temperature and does not require refrigeration. 
     
     
         9 . The ophthalmic solution of  claim 7 , in which the values of latanoprost in the solution, exposed to different temperatures, are within the following ranges: 
       
         
           
                 
               
                   TABLE 2 
                 
                     
                 
                   New Solution % Latanoprost (Labeled 0.005 g/100 ml) 
                 
                 
                 
                 
                 
                 
                 
               
                     
                     
                   Refrigeration 
                     
                     
                     
                 
                     
                   Time 
                   (2° C.-8° C.) 
                   25° C. 
                   30° C. 
                   40° C. 
                 
                     
                     
                 
                 
                 
                 
                 
                 
                 
               
                     
                   0 
                   100.0 
                   100.0 
                   100.0 
                   100.0 
                 
                     
                   1 month 
                   100.0 
                   101.4 
                   100.8 
                   99.2 
                 
                     
                   2 months 
                   99.0 
                   100.0 
                   100.2 
                   99.8 
                 
                     
                   3 months 
                   98.8 
                   99.4 
                   99.2 
                   99.6 
                 
                     
                     
                 
             
                
               
               
                
                
               
            
             
                
                
                
               
            
             
                
                
                
                
                
               
            
           
         
       
     
     
         10 - 12 . (canceled)