Sustained release delivery of a thrombin inhibitor

• US 20040213850A1
• Filed: 04/22/2004
• Published: 10/28/2004
• Est. Priority Date: 04/25/2003
• Status: Abandoned Application

• Current Assignee: Eleni Dokou, John Kirsch, Kendal G. Pitt, Maneesh Nerurkar, Sally Harding, Shyam B. Karki
• Original Assignee: Eleni Dokou, John Kirsch, Kendal G. Pitt, Maneesh Nerurkar, Sally Harding, Shyam B. Karki
• Inventors: Dokou, Eleni, Harding, Sally, Nerurkar, Maneesh, Pitt, Kendal G., Kirsch, John, Karki, Shyam B.
• Application Number:
  US10/829,737
• Publication Number:
  US 20040213850A1
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 31/497 containing further heterocyclic rings
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose

Abstract

The invention is an oral pharmaceutical composition comprising

a) a tablet core comprising a therapeutically effective amount of 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide, or a pharmaceutically acceptable salt thereof, a water swellable polymer, and a neutralizing agent, and

b) a water insoluble film coating surrounding the tablet core,

wherein the water insoluble film coated tablet core has a plurality of apertures.

Claims

1. An oral pharmaceutical composition comprising

a) a tablet core comprising a therapeutically effective amount of 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide, or a pharmaceutically acceptable salt thereof, a water swellable polymer, and a neutralizing agent, and

b) a water insoluble film coating surrounding the tablet core,

wherein the water insoluble film coated tablet core has a plurality of apertures.

2. The composition of claim 1, wherein the tablet core comprises an amount of 3-fluoro-2-pyridylmethyl-3-(2,2-difluoro-2-(2-pyridyl)ethylamino)-6-chloropyrazin-2-one-1-acetamide between about 10% and about 60% by weight of the total core mass, an amount of neutralizing agent between about 10% and about 50% by weight of the total core mass, and an amount of water swellable polymer between about 5% and about 30% by weight of the total core mass

3. The composition of claim 1, wherein the water insoluble film coating comprises between about 60% and about 95%. film forming polymeric material and between about 5% and about 30% plasticizer.

4. The composition of claim 1, wherein the film coating has a thickness of between about 10 and 1000 microns.

5. The composition of claim 4, wherein the film coating has a thickness of from about 100 to about 500 microns.

6. The composition of claim 1, wherein the plurality of apertures is between about 6 and about 200.

7. The composition of claim 6, wherein the apertures have a diameter of between about 0.1 and about 0.9 mm.

8. The composition of claim 7, wherein the apertures have a diameter 5 of about 0.5 mm.