Stabilization of retinoid compounds

Abstract

The present invention relates to a method of administering a compound of Formula I: wherein R 1 is hydrogen or C 1-6 -alkyl; R 2 is C 1-6 -alkyl or adamantyl; R 3 is C 1-6 -alkyl or hydroxy; or R 2 and R 3 taken together are —(CR 6 R 7 ) n —; R 4 is C 2-8 -alkyl, C 2-8 -alkenyl, C 2-8 -alkynyl, —OCH 2 R 5 or C 2-8 -alkanoyl, or hydrogen when R 3 is hydroxy; R 5 is C 1-6 -alkyl, C 2-6 -alkenyl or C 2-6 -alkynyl; R 6 and R 7 are hydrogen or C 1-6 -alkyl; Y is oxygen or sulfur; and n is 3, 4, or 5, or a pharmaceutically acceptable salts of carboxylic acid of formula I, wherein said method comprises the step of admixing said compound in solid form with a topical carrier to form a topical formulation within seven days prior to first topical administration of said compound.

1  (canceled)  
     
     
         2  (canceled)  
     
     
         3  (canceled)  
     
     
         4  (canceled)  
     
     
         5  (canceled)  
     
     
         6  (canceled)  
     
     
         7  (canceled)  
     
     
         8  (canceled)  
     
     
         9  (canceled)  
     
     
         10  (canceled)  
     
     
         11  A kit comprising two chambers, wherein said first chamber comprises a compound in solid form and the second chamber comprises a topical carrier in an amount capable of dissolving or dispersing said compound where said compound is of Formula I  
       
         
           
           
               
               
           
         
         wherein  
         R 1  is hydrogen or C 1-6 -alkyl;  
         R 2  is C 1-6 -alkyl or adamantyl;  
         R 3  is C 1-6 -alkyl or hydroxy; or  
         R 2  and R 3  taken together are —CR 6 R 7 ) n —;  
         R 4  is C 2-8 -alkyl, C 2-8 -alkenyl, C 2-8 -alkynyl, —OCH 2 R 5  or C 2-8 -alkanoyl, or hydrogen when R 3  is hydroxy;  
         R 5  is C 1-6 -alkyl, C 2-6 -alkenyl or C 2-6 -alkynyl;  
         R 6  and R 7  are hydrogen or C 1-6 -alkyl;  
         Y is oxygen or sulfur; and  
         n is 3, 4, or 5,  
         or a pharmaceutically acceptable salts of carboxylic acid of formula I.  
       
     
     
         12  A kit of  claim 11 , wherein said topical carrier is in an amount capable of substantially dissolving said compound.  
     
     
         13  A kit of  claim 11 , wherein said topical carrier is in an amount capable of suspending said compound.  
     
     
         14  A kit of  claim 12 , wherein said second chamber comprises a unit dose of said compound and said topical carrier comprises an alcohol.  
     
     
         15  A kit of  claim 14 , wherein said alcohol is selected from the group consisting of ethanol, isopropyl alcohol or propylene glycol.  
     
     
         16  A kit of  claim 11 , wherein said first chamber further comprises a gelling agent.  
     
     
         17  A kit of  claim 12 , wherein said first chamber comprises multiple unit dosages of said compound and said solvent is selected from the group consisting of diisopropyl adipate, diisopropyl sebacate, diisocetyl adipate, triacetin, caprylic/capric triglyceride, and isopropyl myristate.  
     
     
         18  A kit of  claim 17 , wherein said kit further comprises a label instructing the user to refrigerate said formulation.  
     
     
         19  A kit of  claim 11 , wherein said compound is in an amount of about 0.01% to about 0.1%, by weight, of the combined weight of the compound and the topical carrier.  
     
     
         20  A kit of  claim 12 , wherein said kit further comprises a third chamber comprising a cream or a gel.