Drugs for topical application of sex steroids in the treatment of dry eye syndrome, and methods of preparation and application

Abstract

A topical drug application for the alleviation of kerato-conjunctivitis sicca (dry eye syndrome) is comprised of a solution of sex steroids or their derivatives suspended or dissolved in a vehicle, and the method of preparation and application of the same. In the preferred embodiments, the sex steroid consists essentially of conjugated estrogen in a lipid vehicle or a derivative of estrogen known as 17 beta-Estradiol 3-phosphate disodium dissolved in an aqueous vehicle having a pH of between 6 and 8.

What is claimed is: 
     
       1. The method of treating Dry Eye Syndrome in postmenopausal or oophorectomized .[.females.]. .Iadd.women .Iaddend.which comprises topically applying to the .[.lacrimal.]. .Iadd.ocular surface and conjunctival .Iaddend.tissue to alleviate Dry Eye Syndrome in said .[.females.]. .Iadd.women .Iaddend.the drug comprising a water soluble ester of 17 beta-Estradiol or its derivatives having a concentration of at least 0.1% weight percent dissolved or suspended in a vehicle. 
     
     
       2. The method in accordance with claim 1 wherein said ester is dissolved or suspended in a lipid vehicle. 
     
     
       3. The method in accordance with claim 1 wherein the vehicle in which said ester is applied consists essentially of an aqueous solution having a pH within the range of 7-8. 
     
     
       4. The method in accordance with claim 1 wherein said derivative comprises the 3-phosphate disodium salt of 17 beta-Estradiol. 
     
     
       5. The method in accordance with claim 4 wherein said steroid is dissolved in a vehicle consisting essentially of the composition of the human tear. 
     
     
       6. The method in accordance with claim 4 wherein said steroid or derivative is dissolved in a vehicle consisting essentially of the following components, of which the amounts are indicated in percentages by volume:   ______________________________________                                    
Povidone USP            1.67%                                             
Hydroxy Ethylcellulose USP                                                
                        0.44%                                             
Sodium Chloride USP      0.6%                                             
Dried Sodium Phosphate (Na.sub.2 HPO.sub.4) USP                           
                         .3%                                              
Disodium Edetate USP     .1%                                              
Thimerosal USP          0.004%                                            
pH adjusted to 7 with dilute,                                             
                        qs                                                
HCl or NaOH                                                               
Purified Water USP      qs                                                
______________________________________                                    
     
     
     
       7. The method in accordance with claim 6 in which said sex steroid has a concentration in said vehicle within the range 7 to 8 of percentages by volume.