Low dose compositions of aramchol salts

Abstract

The present invention relates to salts of arachidyl amido cholanoic acid (Aramchol), pharmaceutical compositions comprising Aramchol salts, methods for their preparation, and methods of use thereof in medical treatment.

1 . A pharmaceutically acceptable salt of 3β-arachidylamido-7α,12α-dihydroxy-5β-cholan-24-oic acid (Aramchol), wherein said salt is an amine salt selected from the group consisting of ammonium, benzathine, trimethylglycine (betaine), ethanolamine, diethanolamine, diethylamine, arginine, lysine, choline, deanol, 2-diethylaminoethanol, N-methylglucamine (meglumine), N-ethylglucamine (eglumine), and tromethamine salt. 
     
     
         2 . The pharmaceutically acceptable salt of  claim 1 , wherein the salt is N-methylglucamine (meglumine), lysine or tromethamine salt. 
     
     
         3 . The pharmaceutically acceptable salt of  claim 2 , wherein the salt is N-methylglucamine (meglumine) salt. 
     
     
         4 . The pharmaceutically acceptable salt of  claim 2 , wherein the salt is lysine salt. 
     
     
         5 . The pharmaceutically acceptable salt of  claim 2 , wherein the salt is tromethamine salt. 
     
     
         6 . The pharmaceutically acceptable salt of  claim 1 , wherein the ratio between the Aramchol and the amine is about 1:1. 
     
     
         7 . A pharmaceutical composition in unit dosage form comprising a therapeutically effective amount of the salt of  claim 1 , and at least one pharmaceutically acceptable carrier, diluent, vehicle or excipient. 
     
     
         8 . The pharmaceutical composition of  claim 7 , wherein said composition is in a form suitable for oral administration to a human subject. 
     
     
         9 . The pharmaceutical composition of  claim 7 , wherein said composition is formulated in a form selected from the group consisting of tablets, pills, capsules, pellets, granules, powders, lozenges, sachets, cachets, patches, elixirs, suspensions, dispersions, emulsions, solutions, syrups, aerosols, ointments, soft and hard gelatin capsules, suppositories, sterile injectable solutions, sterile packaged powders and sustained release preparations. 
     
     
         10 . A method of treating a condition associated with fatty liver in a human subject in need thereof, comprising the step of administering to the subject the pharmaceutical composition of  claim 7 . 
     
     
         11 . The method of  claim 10 , wherein said pharmaceutical composition is administered to said subject in a dosage regimen selected from the group consisting of: (i) once a day; (ii) 2 to 4 separate administrations per day; (iii) 2 to 4 separate administrations per week; and (iv) 2 to 4 separate administrations per month. 
     
     
         12 . The method of  claim 10 , wherein the amine is N-methylglucamine (meglumine). 
     
     
         13 . The method of  claim 10 , wherein said disease is Non Alcoholic Steato Hepatitis (NASH).