Pharmaceutical formulation comprising an androstane derivative and a solubilising agent in an aqueous liquid carrier

Abstract

A pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) a glucocorticoid of formula (I) wherein R represents a 5 membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from O, N and S, optionally substituted by one or more methyl or halogen atoms or a solvate thereof, as a medicament; and (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid.

1 . A pharmaceutical formulation comprising an aqueous carrier liquid having dissolved therein (a) a glucocorticoid of formula (I)  
       
         
           
           
               
               
           
         
         wherein r represents a 5 membered heterocyclic aromatic ring containing 1 to 3 heteroatoms selected from 0, n and s, optionally substituted by one or more methyl or halogen atoms or a solvate thereof, as a medicament; and  
         (b) a solubilising agent for assisting the solubilisation of the medicament in the aqueous carrier liquid:  
       
     
     
         2 - 3 . (canceled)  
     
     
         4 . A pharmaceutical formulation according to  claim 1  wherein R represents 4-methyl-1,3-thiazol-5-yl  
     
     
         5 . A pharmaceutical formulation according to  claim 1  wherein the solubilising agent is a surfactant.  
     
     
         6 . A pharmaceutical formulation according to  claim 5  wherein the surfactant is selected from the group consisting of a α-[4-(1,1,3,3-tetramethylbutyl)phenyl]-ω-hydroxypoly(oxy-1,2-ethanediyl) polymer (also known as a octylphenoxypolyethoxyethanol) and a 4-(1,1,3,3-Tetramethylbutyl)phenol polymer with formaldehyde and oxirane.  
     
     
         7 . A pharmaceutical formulation according to  claim 6  wherein the surfactant is a 4-(1,1,3,3-Tetramethylbutyl)phenol polymer with formaldehyde and oxirane.  
     
     
         8 . A pharmaceutical formulation according to  claim 1  which further has dissolved therein a hydroxy containing organic co-solvating agent or phosphatidyl choline.  
     
     
         9 . A pharmaceutical formulation according to  claim 8  wherein the hydroxy containing organic co-solvating agent is dextrose.  
     
     
         10 . A pharmaceutical formulation according to  claim 1  which has one or more a solubilising agents selected from the group consisting of polysorbate, glycerine, benzyl alcohol, polyoxyethylene castor oil derivatives, polyethylene glycol, and polyoxyethylene alkyl ethers.  
     
     
         11 . A pharmaceutical formulation according to  claim 10  wherein the solubilising agent is selected from the group consisting of polysorbate 80, polyoxyl 35 castor oil, polyoxy 40 hydrogenated castor oil, and a polyoxyl 35 castor oil/polyethylene glycol 200 mixture.  
     
     
         12 . A pharmaceutical formulation according to  claim 1  wherein the formulation comprises chloride as an isotonic agent.  
     
     
         13 . A pharmaceutical formulation according to  claim 1  which comprises another therapeutically active agent.  
     
     
         14 . A pharmaceutical formulation according to  claim 13  wherein the other therapeutically active agent is an anti-histamine or an anti-allergic.  
     
     
         15 . A container containing a pharmaceutical formulation according to  claim 1  fitted with a metering valve.  
     
     
         16 . A device adapted for intranasal delivery of a pharmaceutical formulation comprising a container according to  claim 15 .  
     
     
         17 . A method of treatment of inflammatory and/or allergic conditions of the nasal passages which comprises administering to the nose a pharmaceutical formulation according to  claim 1 .  
     
     
         18 . The method according to  claim 17  wherein the administration is once-per-day.  
     
     
         19 - 22 . (canceled)