Tablet formulation comprising semaglutide and a delivery agent

Patent metadata

Field	Value
Publication number	US-9993430-B2
Application number	US-201314409021-A
Country	US
Kind code	B2
Filing date	Jun 19, 2013
Priority date	Jun 20, 2012
Publication date	Jun 12, 2018
Grant date	Jun 12, 2018

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.

First claim

The invention claimed is:

1. A tablet comprising a granulate wherein said granulate comprises i) no more than 15% (w/w) semaglutide, and ii) at least 50% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC), and wherein said tablet has
a) a bulk density of at least 1.0 g/cm 3 ,
b) a median pore diameter of no more than 1.5 μm,
c) a maximum pore diameter of no more than 4 μm,
d) a crushing strength of at least 50 N, and
e) a disintegration time of 12-18 minutes for a tablet with a total weight of 300-500 mg comprising at least 60% (w/w) salt of NAC.

2. A tablet comprising a granulate according to claim 1 , wherein said granulate comprises at least 55% (w/w) salt of N-(8-(2-hydroxybenzoyl)amino)caprylic acid (NAC).

3. A tablet comprising a granulate according to claim 2 , wherein said granulate comprises at least 60% (w/w) salt of NAC.

4. A tablet according to claim 1 , wherein said salt of NAC is monosodium NAC (SNAC).

5. A tablet according to claim 1 , wherein said tablet comprises an intragranular and an extragranular part, wherein said extragranular part comprises a lubricant and optionally a filler.

6. A tablet according to claim 1 , wherein said tablet comprises
a) a granulate comprising
i) 1-15% (w/w) semaglutide,
ii) 55-85% (w/w) salt of NAC, and
iii) 1-20% (w/w) binder;

b) 10-35% (w/w) filler; and
c) 0.5-3% (w/w) lubricant.

7. A tablet according to claim 1 , wherein said tablet does not contain a disintegrant.

8. A tablet according to claim 1 , wherein said tablet is for oral administration.

9. A tablet according to claim 1 , wherein said tablet was prepared by exerting a compression force of at least 5 kN.

10. A tablet according to claim 6 , wherein said salt of NAC is monosodium NAC (SNAC).

Assignees

• Novo Nordisk As

Inventors

• Jensen Simon Bjerregaard
• Sauerberg Per
• Nielsen Flemming S
• Pedersen Betty L
• Skibsted Erik

Classifications

• A61P3/10

  for hyperglycaemia, e.g. antidiabetics · CPC title

• A61K38/26 Primary

  Glucagons · CPC title

• A61K9/2095

  Tabletting processes · CPC title

• A61P3/04

  Anorexiants; Antiobesity agents · CPC title

• A61K9/2013 Primary

  Organic compounds, e.g. phospholipids, fats · CPC title