Methods and related compositions for reduction of fat and skin tightening

Abstract

Compositions and methods useful in the reduction of localized fat deposits and tightening of loose skin in subjects in need thereof using pharmacologically active detergents are disclosed. The pharmacologically active detergent compositions can additionally include anti-inflammatory agents, analgesics, dispersion or anti-dispersion agents and pharmaceutically acceptable excipients. The pharmacologically active detergent compositions are useful for treating localized accumulations of fat including, for example, lower eyelid fat herniation, lipodystrophy and fat deposits associated with cellulite and do not require surgical procedures such as liposuction.

1 . A pharmaceutical solution for subcutaneous injection comprising:
 a therapeutically effective amount of a bile acid or salt thereof;   a pharmaceutical excipient; and   optionally a lipid, wherein when the lipid is present, the therapeutically effective amount of the bile acid or salt thereof has a greater mass than a mass of the lipid in the solution, and wherein the solution does not include lipase or colipase.   
     
     
         2 . The solution of  claim 1  wherein said solution further comprises a second therapeutic agent selected from the group consisting of: anti-microbial agents, vasoconstrictors, anti-thrombotic agents, anticoagulation agents, suds-depressants, anti-inflammatory agents, analgesics', dispersion agents, anti-dispersion agents, penetration enhancers, steroids, tranquilizers, muscle relaxants, and anti-diarrhea agents. 
     
     
         3 . The solution of  claim 1  wherein said solution is in a container that contains up to 500 mL of solution. 
     
     
         4 . The solution of  claim 1  wherein said bile acid is selected from the group consisting of: deoxycholic acid, cholic acid, chenodeoxycholic acid, 7-alpha-dehydroxylate chenodeoxycholic acid, lithocholic acid, ursodeoxycholic acid, dihydroxytaurin acid, trihydroxytaurine acid, and glycine conjugates of any of the above. 
     
     
         5 . The solution of  claim 1  wherein said bile salt comprises a cation selected from the group consisting of sodium (Na + ), potassium (K + ), lithium (Li + ), magnesium (Mg 2+ ), calcium (Ca 2+ ), barium (Ba 2+ ), strontium (Sr 2+ ), and ammonium (NH 4   + ). 
     
     
         6 . The solution of  claim 1  wherein said bile salt comprises an alkali metal or an alkaline earth metal. 
     
     
         7 . The solution of  claim 6  wherein said alkali metal is selected from the group consisting of alkali metal is sodium (Na + ), potassium (K + ), and lithium (Li + ). 
     
     
         8 . The solution of  claim 6  wherein said alkaline earth metal is selected from the group consisting of magnesium (Mg 2+ ), calcium (Ca 2+ ), barium (Ba 2+ ), and strontium (Sr 2+ ). 
     
     
         9 . The solution of  claim 1  wherein said bile acid salt is sodium deoxycholate. 
     
     
         10 . The solution of  claim 1  comprising up to 5% w/w lipids. 
     
     
         11 . The solution of  claim 1  wherein said lipid is phosphatidylcholine. 
     
     
         12 . The solution of  claim 1  wherein said bile acid or bile salt is at a concentration of about 0.001% w/w to about 10% w/w. 
     
     
         13 . The solution of  claim 1  wherein said bile acid or salt thereof is at a concentration of about 0.01% w/w to about 5% w/w. 
     
     
         14 . The solution of  claim 1  wherein said solution is aqueous. 
     
     
         15 . The solution of  claim 1  wherein said therapeutically effective amount is effective for fat dissolution or skin tightening. 
     
     
         16 .- 48 . (canceled) 
     
     
         49 . A syringe loadable container comprising:
 a fat-dissolving or skin-tightening effective amount of a bile acid or a bile salt;   a pharmaceutical or veterinary excipient; and   optionally a lipid wherein when the lipid is present, the therapeutically effective amount of the bile acid or salt thereof has a greater mass than a mass of the lipid in the solution, and wherein the solution does not contain lipase or colipase.   
     
     
         50 . The syringe loadable container of claim  47  wherein said bile salt is sodium deoxycholate. 
     
     
         51 . The syringe loadable container of claim  47  further comprising an organic solvent. 
     
     
         52 . The syringe loadable container of claim  47  comprising up to 10 g of said bile acid or bile salt. 
     
     
         53 . The solution of  claim 1  wherein a weight ratio of the lipid to the bile acid or bile salt is less than 1.