Pharmaceutical formulations containing corticosteroids for topical administration

Abstract

Pharmaceutical compositions for topical application to skin are provided. In some embodiments, the pharmaceutical compositions comprise a corticosteroid and further comprise a liquid oil component comprising one or more dicarboxylic acid esters and/or monocarboxylic acid esters.

1 . A pharmaceutical composition for topical application to the skin of an individual comprising:
 a corticosteroid, wherein the corticosteroid is selected from the group consisting of budesonide, hydrocortisone valerate, hydrocortisone butyrate, and fluticasone propionate;   a liquid oil component comprising one or more of a monocarboxylic acid ester, a dicarboxylic acid ester, or a combination thereof; and   an aqueous component comprising water;   wherein at least 25% of the corticosteroid in solubilized in the liquid oil component at a temperature of 22° C. ± 2° C., and wherein the pharmaceutical composition is formulated as a lotion or a cream.   
     
     
         2 . The pharmaceutical composition of  claim 1 , wherein the corticosteroid is budesonide. 
     
     
         3 . The pharmaceutical composition of  claim 2 , wherein the budesonide is present at a concentration of about 0.01 to about 0.05%. 
     
     
         4 . The pharmaceutical composition of  claim 2 , wherein the budesonide is present at a concentration of 0.04% or less. 
     
     
         5 . The pharmaceutical composition of  claim 2 , wherein the budesonide is present at a concentration of 0.03% or less. 
     
     
         6 . The pharmaceutical composition of  claim 1 , wherein the corticosteroid is hydrocortisone valerate. 
     
     
         7 . The pharmaceutical composition of  claim 6 , wherein the hydrocortisone valerate is present at a concentration less than 0.2%. 
     
     
         8 . The pharmaceutical composition of  claim 1 , wherein the corticosteroid is hydrocortisone butyrate. 
     
     
         9 . The pharmaceutical composition of  claim 8 , wherein the hydrocortisone butyrate is present at a concentration of less than 0.1%. 
     
     
         10 . The pharmaceutical composition of  claim 1 , wherein the corticosteroid is fluticasone propionate. 
     
     
         11 . The pharmaceutical composition of  claim 10 , wherein the fluticasone propionate is present at a concentration of 0.05% or less. 
     
     
         12 . The pharmaceutical composition of  claim 1  wherein the concentration of the liquid oil component is between 1.5 and 3.0 times that required to completely solubilize the corticosteroid in the composition at a temperature of 22° C. ± 2° C. 
     
     
         13 . The pharmaceutical composition of  claim 1 , wherein the concentration of the esters in the liquid oil component is at least 30% of the concentration of the liquid oil component in the composition. 
     
     
         14 . The pharmaceutical composition of  claim 1 , wherein the liquid oil component comprises a dicarboxylic acid ester. 
     
     
         15 . The pharmaceutical composition of  claim 14 , wherein the dicarboxylic acid ester is diethyl sebacate. 
     
     
         16 . The pharmaceutical composition of  claim 1 , wherein the liquid oil component comprises a monocarboxylic acid ester. 
     
     
         17 . The pharmaceutical composition of  claim 16 , wherein the monocarboxylic acid ester is isopropyl myristate. 
     
     
         18 . The pharmaceutical composition of  claim 1 , wherein the liquid oil component comprises a dicarboxylic acid ester and a monocarboxylic acid ester. 
     
     
         19 . The pharmaceutical composition of  claim 1 , wherein the liquid oil component further comprises mineral oil or light mineral oil. 
     
     
         20 . A pharmaceutical composition for topical application to the skin of an individual comprising:
 a corticosteroid, wherein the corticosteroid is budesonide, and the budesonide is present at a concentration of about 0.01% to about 0.05%;   a liquid oil component comprising one or more of a monocarboxylic acid ester, a dicarboxylic acid ester, or a combination thereof; and   an aqueous component comprising water;   wherein at least 25% of the corticosteroid in solubilized in the liquid oil component at a temperature of 22° C. ± 2° C., and wherein the pharmaceutical composition is formulated as a lotion or a cream.   
     
     
         21 . A method for treating a dermatological or muscosal disorder or condition in a subject in need thereof, the method comprising topically applying to the skin of the subject having the dermatological or muscosal disorder or condition a pharmaceutical composition of any one of  claims 1 to 20 . 
     
     
         22 . The method of  claim 21 , wherein the dermatological or mucosal disorder or condition is psoriasis, atopic dermatitis, contact dermatitis, hand dermatitis, eczema, or poison ivy dermatitis.