Solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl) amino) caprylic acid

Patent metadata

Field	Value
Publication number	US-10960052-B2
Application number	US-201816118381-A
Country	US
Kind code	B2
Filing date	Aug 30, 2018
Priority date	Dec 16, 2010
Publication date	Mar 30, 2021
Grant date	Mar 30, 2021

Abstract

The present invention relates to solid compositions comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid and their use in medicine.

First claim

The invention claimed is:

1. A solid composition for oral administration comprising a GLP-1 agonist, a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, magnesium stearate, povidone, and microcrystalline cellulose,
wherein the GLP-1 agonist is semaglutide,
wherein the composition comprises at least 60% (w/w) of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.

2. The composition according to claim 1 , wherein the composition comprises 0.1-10% (w/w) of the magnesium stearate, 0.1-10% (w/w) of the povidone, and 5-40% (w/w) of the microcrystalline cellulose; and wherein the sum of the magnesium stearate, the povidone, and the microcrystalline cellulose is no more than 40% (w/w) of the composition.

3. The composition according to claim 2 , wherein the composition comprises 0.5-5% (w/w) of the magnesium stearate.

4. The composition according to claim 3 , wherein the composition comprises 1-3.5% (w/w) of the magnesium stearate.

5. The composition according to claim 4 , wherein the composition comprises 1% (w/w) of the magnesium stearate.

6. The composition according to claim 2 , wherein the composition comprises 0.2-4% (w/w) of the povidone.

7. The composition according to claim 6 , wherein the composition comprises 0.5-3% (w/w) of the povidone.

8. The composition according to claim 7 , wherein the composition comprises 1% (w/w) or 2% (w/w) of the povidone.

9. The composition according to claim 2 , wherein the composition comprises 10-30% (w/w) of the microcrystalline cellulose.

10. The composition according to claim 9 , wherein the composition comprises 5-25% (w/w) of the microcrystalline cellulose.

11. The composition according to claim 10 , wherein the composition comprises a percentage (w/w) of the microcrystalline cellulose selected from the group consisting of 10.9% (w/w), 18% (w/w), 19.5% (w/w), and 20.5% (w/w).

12. A solid composition for oral administration comprising a semaglutide, a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, a lubricant, a binder, and a filler,
wherein the composition comprises at least 60% (w/w) of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid,
wherein the composition comprises 1-3.5% (w/w) of the magnesium stearate,
wherein the composition comprises 0.5-3% (w/w) of the povidone, and
wherein the composition comprises 5-25% (w/w) of the microcrystalline cellulose.

13. The composition according to claim 12 , wherein the composition comprises 2% (w/w) of the povidone.

14. The composition according to claim 12 , wherein the composition comprises at least 70% (w/w) of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.

15. The composition according to claim 14 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC).

16. The composition according to claim 15 , wherein the composition comprises 2% (w/w) of the povidone.

17. A solid composition for oral administration comprising semaglutide, N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC), a lubricant, a binder, and a filler,
wherein the composition comprises 300 mg of SNAC,
wherein the composition comprises 1-3.5% (w/w) of the magnesium stearate,
wherein the composition comprises 0.5-3% (w/w) of the povidone, and
wherein the composition comprises 5-25% (w/w) of the microcrystalline cellulose.

18. The composition according to claim 17 , wherein the composition comprises 2% (w/w) of the povidone.

Assignees

• Novo Nordisk As

Inventors

• Sauerberg Per
• Bjerregaard Simon
• Nielsen Flemming Seier

Classifications

• A61K38/26 Primary

  Glucagons · CPC title

• A61K9/20 Primary

  Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} · CPC title

• A61K31/195

  having an amino group · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61K9/2077

  Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets · CPC title