Methods and formulations for treating scars and beta-catenin-mediated disorders

Abstract

A topical drug composition for treating a β-catenin-mediated disorder in a mammal is provided comprising a Nefopam compound selected from Nefopam, or a functionally equivalent analogue, prodrug, salt or solvate thereof.

1 - 24 . (canceled) 
     
     
         25 . A topical formulation of Nefopam comprising:
 (a) an effective amount of a compound selected from Nefopam or a functionally equivalent salt thereof;   (b) a solvent/penetration enhancer;   (c) at least one fatty alcohol emulsifier;   (d) an oil-in water emulsifier;   (e) at least one preservative;   
       and sodium hydroxide. 
     
     
         26 . The topical formulation of  claim 25 , wherein the penetration enhancer is selected from the group consisting of (a) diethylene glycol monoethyl and (b) isopropyl myristate, or both (a) and (b). 
     
     
         27 . The topical formulation of  claim 25 , wherein the at least one fatty alcohol emulsifier is selected from the group consisting of (a) cetyl alcohol and (b) stearyl alcohol, or both (a) and (b). 
     
     
         28 . The topical formulation of  claim 25 , wherein the oil-in-water emulsifier is polysorbate 60. 
     
     
         29 . The topical formulation of  claim 25 , wherein the preservative is propylparaben. 
     
     
         30 . The topical formulation of  claim 25 , wherein the Nefopam or functionally equivalent salt thereof is present in an amount of about 10 m/g. 
     
     
         31 . The topical formulation of  claim 26 , wherein the formulation comprises the penetration enhancer diethylene glycol monoethyl, present in an amount from about 30 mg/g to about 45 mg/g. 
     
     
         32 . The topical formulation of  claim 26 , wherein the formulation comprises the penetration enhancer isopropyl myristate, present in an amount from about 15 mg/g to about 22.5 mg/g. 
     
     
         33 . The topical formulation of  claim 27 , wherein the formulation comprises the fatty acid emulsifier cetyl alcohol, present in an amount of about 40 mg/g. 
     
     
         34 . The topical formulation of  claim 27 , wherein the formulation comprises the fatty acid emulsifier stearyl alcohol, present in an amount of about 30 mg/g. 
     
     
         35 . The topical formulation of  claim 28 , wherein the formulation comprises the oil-in-water emulsifier polysorbate 60, present in an amount of about 40 mg/g. 
     
     
         36 . The topical formulation of  claim 29 , wherein the formulation comprises the preservative propyl paraben, present in an amount of about 0.5 mg/g. 
     
     
         37 . The topical formulation of  claim 25 , wherein the formulation further comprises an anti-fungal agent. 
     
     
         38 . The topical formulation of  claim 37 , wherein the anti-fungal agent is methylparaben present in an amount of about 1.0 mg/g. 
     
     
         39 . The topical formulation of  claim 25 , wherein the formulation further comprises a chelating agent. 
     
     
         40 . The topical formulation of  claim 39 , wherein the chelating agent is EDTA present in an amount of about 0.2 mg/g. 
     
     
         41 . The topical formulation of  claim 25 , wherein the formulation further comprises a form of calcium. 
     
     
         42 . The topical formulation of  claim 41 , wherein the form of calcium is calcium gluconate present in an amount of about 5.0 mg/g. 
     
     
         43 . A topical formulation of Nefopam comprising:
 (a) an effective amount of a compound selected from Nefopam or a functionally equivalent salt thereof;   (b) a penetration enhancer selected from (1) diethylene glycol monoethyl in an amount from about 30 mg/g to about 45 mg/g; (2) isopropyl myristate in an amount from about 15 mg/g to about 22.5 mg/g; or both (1) and (2);   (c) a fatty alcohol emulsifier selected from (1) cetyl alcohol in an amount of about 40 mg/g; (2) stearyl alcohol in an amount of about 30 mg/g; or both (1) and (2).   (d) an oil-in water emulsifier polysorbate 60 in an amount of about 40 mg/g.   (e) a preservative propylparaben in an amount of about 0.5 mg/g.   (f) a chelating agent EDTA in an amount of 0.02 mg/g;   
       and sodium hydroxide. 
     
     
         44 . The topical formulation of  claim 43 , wherein the sodium hydroxide is added in an amount sufficient to reach a pH of about 5.0 to about 5.6.