Compositions of glp-1 peptides and preparation thereof

Abstract

The invention relates to pharmaceutical compositions comprising a first type of granules and a second type of granules, wherein said first type of granules comprises a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and no GLP-1 peptide, and wherein said second type of granules comprises a GLP-1 peptide and no salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, as well as the intermediate granules, processes for the preparation of the granules and compositions, and use thereof in medicine.

1 . A process of producing a pharmaceutical composition comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a GLP-1 peptide, wherein the process comprises the steps:
 a) mixing a GLP-1 peptide with a filler and/or a binder;   b) dry granulation of the mixture of step a;   c) mixing the granules obtained in step b with a composition comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid; and   d) optionally adding further lubricant,   wherein the mixture of step a does not comprise a salt of N-(8-(2-hydroxybenzoyl)amino) caprylic acid.   
     
     
         2 . A process of producing a pharmaceutical composition comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a GLP-1 peptide, wherein the process comprises the steps:
 a) mixing a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid with a lubricant and/or a filler;   b) dry granulation of the mixture of step a;   c) mixing the granules obtained in step b with a composition comprising a GLP-1 peptide; and   d) optionally adding further lubricant   wherein the mixture of step a does not comprise a GLP-1 peptide.   
     
     
         3 . A process of producing a pharmaceutical composition comprising a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and a GLP-1 peptide, wherein the process comprises the steps:
 a) mixing a GLP-1 peptide with a filler and/or a binder;   b) dry granulation of the mixture of step a;   c) mixing a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, optionally a lubricant and/or a filler;   d) dry granulation of the mixture of step c;   e) mixing the granules obtained in step b with the granules obtained in step d; and   f) optionally adding further lubricant,   wherein the mixture of step a does not comprise a salt of N-(8-(2-hydroxybenzoyl)amino) caprylic acid and wherein the mixture of step c does not comprise a GLP-1 peptide.