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-9278123-B2
Application number	US-201113994262-A
Country	US
Kind code	B2
Filing date	Dec 16, 2011
Priority date	Dec 16, 2010
Publication date	Mar 8, 2016
Grant date	Mar 8, 2016

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 and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, wherein
the amount of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is in the range of 0.8-1.3 mmol, and the GLP-1 agonist is N-epsilon26-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxyheptadecanoylamino) butyrylamino] ethoxy} ethoxy)acetylamino] ethoxy} ethoxy)acetyl] [Aib8, Arg34] GLP-1(7-37).

2. The composition according to claim 1 , wherein said composition is in the form of a tablet.

3. The composition according to claim 1 , wherein the amount of the GLP-1 agonist is in the range of 5 to 20 mg.

4. The composition according to claim 1 , wherein said salt of N-(8-(2-hydroxybenzoyl) amino)caprylic acid is selected from the group consisting of the sodium salt, potassium salt and calcium salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.

5. The composition according to claim 4 , wherein the amount of the GLP-1 agonist is in the range of 5 to 20 mg.

6. The composition according to claim 4 , wherein said salt of N-(8-(2-hydroxybenzoyl) amino)caprylic acid is sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC).

7. The composition according to claim 6 , wherein the amount of the GLP-1 agonist is in the range of 5 to 20 mg.

8. A method for treatment of type II diabetes or obesity comprising administering a composition according to claim 1 to a patient in need thereof.

9. A solid composition for oral administration comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, wherein the amount of said GLP-1 agonist is in the range of from 5 to 20 mg, and the GLP-1 agonist is N-epsilon26-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxyheptadecanoylamino) butyrylamino]ethoxy}ethoxy)acetylamino]ethoxy}ethoxy)acetyl][Aib8, Arg34]GLP-1(7-37).

10. The composition according to claim 9 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is selected from the group consisting of the sodium salt, potassium salt and calcium salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.

11. The composition according to claim 10 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC).

12. The composition according to claim 11 , wherein the amount of SNAC is in the range of 250 mg to 400 mg.

13. The composition according to claim 11 , wherein the amount of SNAC is 300 mg.

14. The composition according to claim 9 , wherein said composition is in the form of a tablet.

15. A method for treatment of type II diabetes or obesity comprising administering a composition according to claim 9 to a patient in need thereof.

16. A solid composition for oral administration comprising a GLP-1 agonist and a salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid, wherein
the amount of said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is in the range of 0.6-2.1 mmol, and the GLP-1 agonist is N-epsilon26-[2-(2-{2-[2-(2-{2-[(S)-4-carboxy-4-(17-carboxyheptadecanoylamino) butyrylamino]ethoxy}ethoxy)acetylamino]ethoxy}ethoxy)acetyl][Aib8, Arg34]GLP-1(7-37), wherein the amount of the GLP-1 agonist is in the range of 5 to 20 mg.

17. The composition according to claim 16 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is selected from the group consisting of the sodium salt, potassium salt and calcium salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid.

18. The composition according to claim 17 , wherein said salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid is sodium N-(8-(2-hydroxybenzoyl)amino)caprylate (SNAC).

19. The composition according to claim 18 , wherein said composition is in the form of a tablet.

Assignees

• Sauerberg Per
• Bjerregaard Simon
• Nielsen Flemming Seier
• Novo Nordisk As

Inventors

• Sauerberg Per
• Bjerregaard Simon
• Nielsen Flemming Seier

Classifications

• A61P9/00

  Drugs for disorders of the cardiovascular system · CPC title

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P3/06

  Antihyperlipidemics · CPC title

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61P3/00

  Drugs for disorders of the metabolism (of the blood or the extracellular fluid A61P7/00) · CPC title