Pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof suitable for local administration

Abstract

The present invention relates in general to the field of modulators of the innate immune system, particularly to pharmaceutical compositions comprising imidazoquinolin(amines) and derivatives thereof, preferably suitable for local administration, such as, intravesical administration. In addition, the present invention concerns the use of imidazoquinolin(amines) and derivatives thereof for intravesical treatment of bladder diseases, such as, for example, bladder cancer and cystitis. The present invention furthermore comprises methods of treatment for these diseases as well as methods of administration of the inventive pharmaceutical compositions.

1 - 25 . (canceled) 
     
     
         26 . A pharmaceutical composition comprising imiquimod, lactic acid and two or more polaxamers, wherein the composition is for bladder instillation. 
     
     
         27 . The pharmaceutical composition of  claim 26 , wherein the lactic acid is at a concentration of about 0.025 M to about 0.200 M. 
     
     
         28 . The pharmaceutical composition of  claim 27 , wherein the lactic acid is at a concentration of about 0.075 M to about 0.125 M. 
     
     
         29 . The pharmaceutical composition of  claim 26 , wherein the imiquimod is in an amount of about 0.005% (w/v) to about 5% (w/v), 
     
     
         30 . The pharmaceutical composition of  claim 29 , wherein the imiquimod is in an amount of about 0.1% (w/v) to about 1% (w/v). 
     
     
         31 . The pharmaceutical composition of  claim 26 , further comprising a cyclodextrin. 
     
     
         32 . The pharmaceutical composition of  claim 31 , wherein the cyclodextrin is selected from α-cyclodextrins, β-cyclodextrins, γ-cyclodextrins, δ-cyclodextrins, ε-cyclodextrins, and hydroxypropyl-β-cyclodextrin (HP-β-CD). 
     
     
         33 . The pharmaceutical composition of  claim 32 , wherein the cyclodextrin is hydroxypropyl-β-cyclodextrin (HP-β-CD). 
     
     
         34 . The pharmaceutical composition of  claim 31 , wherein the cyclodextrin in an amount of about 0.1% (w/v) to about 30% (w/v). 
     
     
         35 . The pharmaceutical composition of  claim 34 , wherein the cyclodextrin in an amount of about 2% (w/v) to about 6% (w/v). 
     
     
         36 . The pharmaceutical composition of  claim 26 , wherein the polaxamers are in an (overall) amount of about 10% (w/v) to about 30% (w/v) or in an (overall) amount of about 20% (w/v) to about 25% (w/v). 
     
     
         37 . The pharmaceutical composition of  claim 26 , wherein a poloxamer is Poloxamer 407. 
     
     
         38 . The pharmaceutical composition of  claim 26 , wherein a poloxamer is Poloxamer 188. 
     
     
         39 . The pharmaceutical composition of  claim 26 , wherein the poloxamers are Poloxamer 407 and Polaxamer 188. 
     
     
         40 . The pharmaceutical composition of  claim 37 , wherein Poloxamer 407 in an amount of about 10% (w/v) to about 25% (w/v) or in an amount of about 12% (w/v) to about 20% (w/v). 
     
     
         41 . The pharmaceutical composition of  claim 39 , wherein Poloxamer 407 and Poloxamer 188 are in an (overall) amount of about 22.5% (w/v)/(w/w) to about 27.5% (w/v)/(w/w) or in an overall amount of about 20% (w/v)/(w/w) to about 25% (w/v)/(w/w). 
     
     
         42 . The pharmaceutical composition of  claim 26 , wherein the composition is aqueous. 
     
     
         43 . A pharmaceutical composition comprising imiquimod in an amount of about 0.1% (w/v) to about 1% (w/v), lactic acid in a concentration of about 0.075 M to about 0.125 M and Poloxamer 407 and Poloxamer 188 in an (overall) amount of about 20% (w/v) to about 25% (w/v), the composition is aqueous and is for bladder instillation.