Pharmaceutical formulation of fluticasone propionate

Abstract

There is provided according to the invention a pharmaceutical aerosol formulation which comprises: (i) fluticasone propionate and (ii) a hydrofluoroalkane (HFA) propellant, characterised in that the fluticasone propionate is completely dissolved in the formulation. The invention also provided canisters containing the formulation and uses thereof.

What is claimed is:  
     
         1 . A pharmaceutical aerosol formulation which comprises: 
 (i) fluticasone propionate and    (ii) a hydrofluoroalkane (HFA) propellant, characterised in that the fluticasone propionate is completely dissolved in the formulation.    
     
     
         2 . A pharmaceutical formulation according to  claim 1  which comprises: 
 (i) fluticasone propionate;  
 (ii) a hydrofluoroalkane (HFA) propellant;  
 (iii) a low volatility component to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler, and  
 (iv) a solubilisation agent in sufficient quantity to solubilise the fluticasone propionate in the formulation.  
 
     
     
         3 . A pharmaceutical formulation according to  claim 1  wherein the hydrofluoroalkane (HFA) propellant is 1,1,1,2-tetrafluoroethane (HFA134a).  
     
     
         4 . A pharmaceutical formulation according to  claim 1  containing a low volatility component which is glycerol, propylene glycol or polyethylene glycol.  
     
     
         5 . A pharmaceutical formulation according to  claim 4  containing a low volatility component which is polyethylene glycol.  
     
     
         6 . A pharmaceutical formulation according to  claim 4  containing a low volatility component which is glycerol.  
     
     
         7 . A pharmaceutical formulation according to  claim 4  wherein the low volatility component is present at a concentration of 0.5 to 3% w/w.  
     
     
         8 . A pharmaceutical formulation according to  claim 1  which comprises: 
 (i) fluticasone propionate;  
 (ii) 1,1,1,2-tetrafluoroethane (HFA 134a);  
 (iii) 0.5-3% (w/w) glycerol; and  
 (iv) a solubilisation agent in sufficient quantity to solubilise the fluticasone propionate in the formulation.  
 
     
     
         9 . A pharmaceutical formulation according to  claim 1  which contains between 0.8 and 1.6% (w/w) glycerol.  
     
     
         10 . A pharmaceutical formulation according to  claim 9  which contains between 1.0 and 1.6% (w/w) glycerol.  
     
     
         11 . A pharmaceutical formulation according to  claim 10  which contains 1.3% (w/w) glycerol.  
     
     
         12 . A pharmaceutical formulation according to  claim 10  which contains 1.0% (w/w) glycerol.  
     
     
         13 . A formulation according to  claim 1  wherein the concentration of fluticasone propionate is 0.025 to 0.15% w/v.  
     
     
         14 . A formulation according to  claim 13  wherein the concentration of fluticasone propionate is 0.035 to 0.15% w/v.  
     
     
         15 . A formulation according to  claim 14  wherein the concentration of fluticasone propionate is 0.04 to 0.1% w/v.  
     
     
         16 . A formulation according to  claim 13  wherein the concentration of fluticasone propionate is 0.025 to 0.04% w/v.  
     
     
         17 . A formulation according to  claim 1  wherein a solubilisation agent is present which is ethanol or propylene glycol.  
     
     
         18 . A formulation according to  claim 1  wherein a solubilisation agent is present which is an alkane or ether.  
     
     
         19 . A formulation according to  claim 1  wherein a solubilisation agent is present which is dimethoxymethane.  
     
     
         20 . A formulation according to  claim 1  wherein a solubilisation agent is present which is ethylacetate.  
     
     
         21 . A formulation according to  claim 17  wherein a solubilisation agent is present which is ethanol.  
     
     
         22 . A formulation according to  claim 21  wherein the concentration of ethanol is 5 to 30% w/w.  
     
     
         23 . A formulation according to  claim 22  wherein the concentration of ethanol is 10 to 20% w/w.  
     
     
         24 . A formulation according to  claim 22  wherein the concentration of ethanol is 7 to 16% w/w.  
     
     
         25 . A formulation according to  claim 22  wherein the concentration of ethanol is 7 to 11% w/w.  
     
     
         26 . A formulation according to  claim 22  wherein the concentration of ethanol is 7 to 8% w/w.  
     
     
         27 . A formulation according to  claim 19  wherein the concentration of solubilisation agent is 14 to 16% w/w.  
     
     
         28 . A canister comprising a metering valve and containing a composition according to  claim 1 .  
     
     
         29 . A canister according to  claim 28  comprising an aluminium can which is anodised, lacquer-coated and/or plastic coated.  
     
     
         30 . A canister according to  claim 29  which is coated with a fluorocarbon polymer.  
     
     
         31 . A canister according to  claim 28  fitted with a metering valve of metering volume 100 μl.  
     
     
         32 . A metered dose inhaler which comprises a canister as claimed in  claim 28  fitted into a suitable channelling device.  
     
     
         33 . A metered dose inhaler according to  claim 32  wherein the channelling device comprises a mouthpiece actuator having an actuator orifice of diameter 0.25 mm or less.  
     
     
         34 . A method of treating respiratory disorders which comprises administration by inhalation of an effective amount of a pharmaceutical aerosol formulation according to  claim 1 .  
     
     
         35 . A formulation according to  claim 20  wherein the concentration of solubilisation agent is 14 to 16% w/w.  
     
     
         36 . A formulation according to  claim 14  wherein the propellant is 1,1,1,2-tetrafluoroethane and a solubilising agent is present which is ethanol.  
     
     
         37 . A formulation according to  claim 15  wherein the propellant is 1,1,1,2-tetrafluoroethane and a solubilising agent is present which is ethanol.  
     
     
         38 . A formulation according to  claim 36  wherein a low volatility to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler component is present which is glycerol at a concentration of 0.5-3% w/w.  
     
     
         39 . A formulation according to  claim 37  wherein a low volatility to increase the mass median aerodynamic diameter (MMAD) of the aerosol particles on actuation of the inhaler component is present which is glycerol at a concentration of 0.5-3% w/w.