Solid glp-1 derivative compositions for oral administration

Patent metadata

Field	Value
Publication number	US-2022016216-A1
Application number	US-202117496831-A
Country	US
Kind code	A1
Filing date	Oct 8, 2021
Priority date	Jun 9, 2017
Publication date	Jan 20, 2022
Grant date	—

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.

First claim

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.

Assignees

• Novo Nordisk As

Inventors

• Vegge Andreas
• Scheele Susanne
• Bjerregaard Simon

Classifications

• A61K31/7034

  attached to a carbocyclic compound, e.g. phloridzin · CPC title

• A61K45/06

  Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca · CPC title

• A61K38/26 Primary

  Glucagons · CPC title

• A61K9/0053

  Mouth and digestive tract, i.e. intraoral and peroral administration · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title