Solid compositions comprising a glp-1 agonist and a salt of n-(8-(2-hydroxybenzoyl)amino)caprylic acid

Abstract

The present invention relates to solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and their use in medicine.

1 . A solid composition for oral administration comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, wherein the amount of said salt of N(8-(2-hydroxybenzoyl)amino)caprylic acid is at least 0.6 or at least 0.8 mmol; and said GLP-1 agonist optionally comprises one substituent. 
     
     
         2 . A composition according to  claim 1 , wherein said composition is in the form of a tablet. 
     
     
         3 . A composition according to  claim 1 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC). 
     
     
         4 . A composition according to  claim 1 , wherein the amount of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is in the range of 0.6-2.1 mmol, such as 0.6-1.9 mmol, 0.7-1.7 mmol or 0.8-1.3 mmol. 
     
     
         5 . A composition according to  claim 1 , wherein the amount of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is up to 2.1 mmol, such as selected from the group consisting of up to 2.1 mmol, up to 2 mmol, up to 1.9 mmol, up to 1.8 mmol, up to 1.7 mmol, up to 1.6 mmol, up to 1.5 mmol, up to 1.4 mmol, up to 1.3 mmol, up to 1.2 mmol and up to 1.1 mmol. 
     
     
         6 . A composition according to  claim 1 , wherein the amount of the GLP-1 agonist is in the range of 0.01 mg to 100 mg. 
     
     
         7 . A composition according to  claim 1 , wherein said GLP-1 agonist is GLP-1 (7-37), GLP-1 (7-36)amide, exendin-4 or an analogue thereof comprising up to 10 substitutions, deletions, additions and/or insertions, and wherein said GLP-1 agonist optionally comprises one substituent. 
     
     
         8 . A composition according to  claim 7 , wherein said substituent comprises a fatty acid or a fatty diacid. 
     
     
         9 . A composition according to  claim 8 , wherein said substituent comprises formula (X) 
       
         
           
           
               
               
           
         
         wherein n is at least 13, such as n is 13, 14, 15, 16, 17, 18 or 19. 
       
     
     
         10 . A composition according to  claim 1 , wherein the amount of GLP-1 is in the range of 0.05 to 25 μmol, such as in the range of 0.5 to 2.5 μmol. 
     
     
         11 . A composition according to  claim 1 , wherein said composition comprises at least one additional pharmaceutically acceptable excipient.