Tablet formulation comprising a glp-1 peptide and a delivery agent

Abstract

The present invention relates to solid compositions comprising a GLP-1 peptide and a delivery agent, such as SNAC, as well as uses thereof.

1 . A tablet comprising a granulate comprising:
 i) no more than 15% (w/w) GLP-1 peptide, and   ii) at least 50%, 55%, or 60% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC).   
     
     
         2 . A tablet according to  claim 1 , wherein said peptide comprises a substituent comprising a fatty acid or a fatty diacid, of formula (X) 
       
         
           
           
               
               
           
         
         wherein n is at least 13; 
         and wherein said peptide optionally comprises one or more 8-amino-3,6-dioxaoctanoic acid (OEG). 
       
     
     
         3 . A tablet according to  claim 1 , wherein said GLP-1 peptide is semaglutide. 
     
     
         4 . A tablet according to  claim 1 , wherein said salt of NAC is monosodium NAC (SNAC), anhydrous SNAC monosodium salt. 
     
     
         5 . A tablet according to  claim 1 , wherein the amount of said salt of NAC is 50-90% (w/w), 55-85% (w/w), or 70-80% (w/w). 
     
     
         6 . A tablet according to  claim 1 , wherein said tablet comprises an intragranular and an extragranular part, wherein said extragranular part comprises a lubricant and optionally a filler. 
     
     
         7 . A tablet according to  claim 1 , wherein said tablet comprises
 a) a granulate comprising
 i) 1-15% (w/w) GLP-1 peptide, 
 ii) 55-85% (w/w) salt of NAC, and 
 iii) 1-20% (w/w) binder; 
   b) 10-35% (w/w) filler; and   c) 0.5-3% (w/w) lubricant.   
     
     
         8 . A tablet according to  claim 1 , wherein said tablet does not comprise a superdisintegrant. 
     
     
         9 . A tablet according to  claim 1 , wherein said tablet is for oral administration. 
     
     
         10 . A tablet according to  claim 1 , wherein said tablet was prepared by exerting a compression force of at least 5 kN, such as 5-25 kN, at least 10 kN or at least 15 kN, or at least 4 kN/cm 2 , such as at least 6 kN/cm 2  or at least 8 kN/cm 2 . 
     
     
         11 . A method of treating type 2 diabetes or obesity comprising administering to a subject in need of such treatment a tablet according to  claim 1 . 
     
     
         12 . A process for the preparation of a tablet comprising a granulate comprising i) no more than 15% (w/w) GLP-1 peptide, and ii) at least 50% (w/w) salt of NAC, said method further comprising the step of exerting a compression force when punching said tablet of a) at least 5 kN, such as 5-25 kN, at least 10 kN or at least 15 kN, and/or b) at least 4 kN/cm 2 , such as at least 6 kN/cm 2  or at least 8 kN/cm 2 ,
 wherein said process optionally comprises a pre-compression step.   
     
     
         13 . A method for controlling porosity of the tablet of  claim 1 , said method comprising the steps of:
 a) determining the near-infrared (NIR) spectrum of one or more of said tablets,   b) comparing said spectrum to a reference NIR spectrum or performing a statistical analysis of said spectrum to determine the tablet porosity,   c) optionally adjusting the tabletting parameters during tabletting in order to improve the NIR spectrum or porosity of the tablets, and   d) selecting a subgroup of tablets with a NIR spectrum or porosity within a predetermined range,   
       wherein said method optionally is an at-line or an in-line NIR method.