Improvements Relating To Inhalable Particles

Abstract

A powder formulation, or pharmaceutical composition comprising or consisting of particles of an antimuscarinic agent, said particles being obtainable by supercritical anti-solvent (SAS) precipitation and having a D 50 of 4 μm or less and a D 90 of 10 μm or less. Methods of forming the formulation and composition are also disclosed, as are uses of the composition.

1 . A powder formulation comprising particles of an antimuscarinic agent, said particles being obtainable by supercritical anti-solvent (SAS) precipitation and having a D 50  of 4 μm or less and a D 90  of 10 μm or less. 
     
     
         2 . The powder formulation of  claim 1 , wherein said particles have a D 50  of in the range of from 1 to 2.5 μm or less. 
     
     
         3 . The powder formulation of  claim 1 , wherein said particles have a D 90  of in the range of from 2 to 6 μm or less. 
     
     
         4 .- 5 . (canceled) 
     
     
         6 . The powder formulation of  claim 1 , wherein the volume mean diameter of said particles is 7 μm or less. 
     
     
         7 . The powder formulation of  claim 1 , wherein said particles have a monomodal particle size distribution. 
     
     
         8 . The powder formulation of  claim 1 , wherein the antimuscarinic agent acts on the M 2  and M 3  subtypes. 
     
     
         9 . The powder formulation of  claim 1 , wherein the antimuscarinic agent is tolterodine or a tolterodine-related compound, or a pharmaceutically acceptable salt thereof. 
     
     
         10 . The powder formulation of  claim 1 , wherein the antimuscarinic agent comprises tolterodine. 
     
     
         11 . The powder formulation of  claim 1 , wherein the particles of antimuscarinic agent are in crystalline form. 
     
     
         12 . The powder formulation of  claim 1 , wherein the antimuscarinic agent has an acicular crystal habit under solvent evaporation crystallization conditions. 
     
     
         13 . The powder formulation of  claim 1 , wherein the antimuscarinic agent is tolterodine L-tartrate. 
     
     
         14 .- 30 . (canceled) 
     
     
         31 . A pharmaceutical composition comprising a therapeutically effective amount of particles of an antimuscarinic agent, said particles being obtainable by supercritical anti-solvent (SAS) precipitation and having a D 50  of 4 μm or less and a D 90  of 10 μm or less. 
     
     
         32 . (canceled) 
     
     
         33 . The pharmaceutical composition according to  claim 31 , wherein the pharmaceutical composition is a mixture and comprises a suitable pharmaceutical excipient for the particles of antimuscarinic agent. 
     
     
         34 . The pharmaceutical composition according to  claim 31 , wherein the antimuscarinic agent is tolterodine or a tolterodine-related compound, or a pharmaceutically acceptable salt thereof. 
     
     
         35 . The pharmaceutical composition according to  claim 31 , wherein the antimuscarinic agent comprises tolterodine. 
     
     
         36 . The pharmaceutical composition according to  claim 31 , wherein the antimuscarinic agent is tolterodine L-tartrate. 
     
     
         37 . (canceled) 
     
     
         38 . A method of treatment of a disorder selected from the group consisting of: urinary disorder, asthma, COPD, and allergic rhinitis, the method comprising administering to a subject in need thereof a pharmaceutical composition according to  claim 31 . 
     
     
         39 . (canceled) 
     
     
         40 . The method according to  claim 38 , wherein said method comprises treatment of urinary disorder by inhalation or insufflation of said pharmaceutical composition. 
     
     
         41 . The method according to  claim 38 , wherein said method comprises treatment of urinary incontinence, in particular urge incontinence, stress incontinence or mixed incontinence by inhalation or insufflation of said pharmaceutical composition. 
     
     
         42 . A method according to  claim 38 , wherein the method provides rapid relief or fast onset of the antimuscarinic agent. 
     
     
         43 .- 46 . (canceled)