Solid glp-1 derivative compositions for oral administration

Abstract

The present invention relates to solid compositions for oral administration comprising (i) a GLP-1 derivative and the SGLT2 inhibitor dapagliflozin or (ii) a GLP-1 derivative and a salt of NAC in combination with an SGLT2 inhibitor.

1 . A pharmaceutical composition comprising:
 semaglutide and dapagliflozin,   wherein the composition is an oral administration in a single solid dosage form, and   wherein the oral bioavailability of semaglutide is increased in the presence of dapagliflozin.   
     
     
         2 . The pharmaceutical composition according to  claim 1 , wherein the-composition further comprises an absorption enhancer. 
     
     
         3 . The pharmaceutical composition according to  claim 1 , wherein one or both of the semaglutide and the dapagliflozin is in the form of a pharmaceutically acceptable salt, ester, or solvate. 
     
     
         4 . The pharmaceutical composition according to  claim 1 , wherein the dosage of the dapagliflozin is 0.5-50 mg per day and the dosage of semaglutide is 0.1-100 mg per day. 
     
     
         5 . The pharmaceutical composition according to  claim 1 , wherein the composition comprises one or more additional pharmaceutically acceptable excipients. 
     
     
         6 . The composition according to  claim 2 , wherein the absorption enhancer is N-(8-(2-hydroxybenzoyl)amino)caprylate (NAC). 
     
     
         7 . The pharmaceutical composition according to  claim 10 , wherein the absorption enhancer is a salt of NAC. 
     
     
         8 . The pharmaceutical composition according to  claim 7 , wherein the salt of NAC is monosodium N-[8-(2-hydroxybenxoyl) amino] caprylate (SNAC) or polymorphs thereof. 
     
     
         9 . The pharmaceutical composition according to  claim 1 , wherein the dosage of the composition administered is in the range of 200-1000 mg. 
     
     
         10 . The pharmaceutical composition according to  claim 1 , wherein the composition is administered once daily. 
     
     
         11 . The pharmaceutical composition according to  claim 1 , wherein the composition comprises 5-300 mg dapagliflozin and 20-800 mg of a salt of NAC. 
     
     
         12 . The pharmaceutical composition according to  claim 11 , wherein the salt of NAC is SNAC or polymorphs thereof. 
     
     
         13 . The pharmaceutical composition according to  claim 1 , wherein the composition is in a form selected from the group consisting of a tablet, a capsule, and a sachet. 
     
     
         14 . A method of treating type 2 diabetes in a subject in need of such method comprising administering to the subject a therapeutically effective amount of the pharmaceutical composition according to  claim 1  and one or more pharmaceutically acceptable excipients.