Claims for Patent: 11,033,499

Summary for Patent: 11,033,499

Title:	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.
Inventor(s):	Simon Bjerregaard Jensen, Per Sauerberg, Flemming S. Nielsen, Betty L. Pedersen, Erik Skibsted
Assignee:	Novo Nordisk AS
Application Number:	US15/958,236
Patent Claims:	1. A tablet comprising a granulate, wherein said granulate comprises: i) no more than 15% (w/w) GLP-1 peptide, wherein the GLP-1 peptide is a peptide; and ii) at least 50% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC); wherein said tablet has a) a bulk density of at least 1.0 g/cm3; b) a median pore diameter of no more than 1.5 μm; and c) a feature selected from the group consisting of a maximum pore diameter of no more than 4 μm, a crushing strength of 50-400 N, and a disintegration time of 22 minutes or less. 2. The tablet according to claim 1, wherein the GLP-1 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. The tablet according to claim 1, wherein the GLP-1 peptide is semaglutide. 4. The tablet according to claim 1, wherein the salt of NAC is monosodium NAC (SNAC). 5. The tablet according to claim 1, wherein the amount of the salt of NAC is 50-90% (w/w). 6. The tablet according to claim 1, wherein the tablet comprises an intragranular and an extragranular part, and wherein the extragranular part comprises a lubricant. 7. The tablet according to claim 1, wherein the granulate comprises i) 1-15% (w/w) GLP-1 peptide, ii) 55-85% (w/w) salt of NAC, and iii) 1-20% (w/w) binder; and wherein the tablet further comprises 10-35% (w/w) filler and 0.5-3% (w/w) lubricant. 8. The tablet according to claim 1, wherein the tablet does not comprise a superdisintegrant. 9. The tablet according to claim 1, wherein the tablet is for oral administration. 10. The tablet according to claim 1, wherein the tablet is prepared by exerting a compression force in the range of 2-25 kN. 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. The tablet according to claim 4, wherein the SNAC is anhydrous SNAC monosodium salt. 13. The tablet according to claim 6, wherein the extragranular part further comprises a filler. 14. The tablet according to claim 1, wherein said granulate comprises: i) no more than 15% (w/w) GLP-1 peptide, wherein the GLP-1 peptide is a peptide and ii) at least 50% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC); wherein said tablet has a) a bulk density of at least 1.0 g/cm3; b) a median pore diameter of no more than 1.5 μm; and c) a maximum pore diameter of no more than 4 μm. 15. The tablet according to claim 1, wherein said granulate comprises: i) no more than 15% (w/w) GLP-1 peptide, and ii) at least 50% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC); wherein said tablet has a) a bulk density of at least 1.0 g/cm3; b) a median pore diameter of no more than 1.5 μm; and c) a crushing strength of 50-400 N. 16. The tablet according to claim 1, wherein said granulate comprises: i) no more than 15% (w/w) GLP-1 peptide, and ii) at least 50% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC); wherein said tablet has a) a bulk density of at least 1.0 g/cm3; b) a median pore diameter of no more than 1.5 μm; and c) a disintegration time of 22 minutes or less.