Compositions comprising a delivery agent and preparation thereof

Abstract

The invention relates to granules and pharmaceutical compositions comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant obtained by mixing hereof for more than 5 minutes prior to granulation as well as processes for their preparation and use thereof in medicine.

1 . A granule comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant, wherein said granule is obtained by mixing said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic and said lubricant for more than 5 minutes, prior to granulation. 
     
     
         2 . A granule according to  claim 1 , wherein the amount of said lubricant is at least 0.25% (w/w) of said granule. 
     
     
         3 . A granule according to  claim 1 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is SNAC. 
     
     
         4 . A pharmaceutical composition comprising said granule as defined in  claim 1 . 
     
     
         5 . A pharmaceutical composition according to  claim 4 , wherein said composition further comprises a GLP-1 peptide. 
     
     
         6 . A pharmaceutical composition according to  claim 5 , wherein said GLP-1 peptide comprises an albumin binding moiety. 
     
     
         7 . A pharmaceutical composition according to  claim 6 , wherein said GLP-1 peptide is N-epsilon26-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxyheptadecanoylamino) butyrylamino]ethoxy}ethoxy)acetylamino]ethoxy}ethoxy)acetyl][Aib8,Arg34]GLP-1(7-37). 
     
     
         8 . A pharmaceutical composition according to  claim 4 , wherein said composition comprises granules which have been manufactured by roller compaction. 
     
     
         9 . A process of producing a granule comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a lubricant, such a magnesium stearate, wherein said process comprises the steps:
 a) mixing said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and said lubricant for more than 5 minutes; and   b) optionally roller compacting the mixture of step a.   
     
     
         10 . A process according to  claim 9 , wherein the duration of said mixing in step a is at least 20 minutes. 
     
     
         11 . A process according to  claim 9 , wherein the amount of said lubricant is at least 0.25% (w/w) of said composition. 
     
     
         12 . A granule obtained by the process as defined in  claim 9 . 
     
     
         13 . A pharmaceutical composition obtained by the process as defined in  claim 9 . 
     
     
         14 . A pharmaceutical composition according to  claim 4 , wherein said composition is in the form of a solid dosage form. 
     
     
         15 . A method for treating diabetes or obesity in a subject in need of such treatment, said method comprising administering orally to said subject a therapeutically effective amount of a composition according to  claim 5 .