GASTRIC RETENTIVE EXTENDED-RELEASE DOSAGE FORMS COMPRISING COMBINATIONS OF ACETAMINOPHEN AND PHENYLEPHRINE

• US 20110104272A1
• Filed: 11/05/2010
• Published: 05/05/2011
• Est. Priority Date: 11/05/2009
• Status: Abandoned Application

• Current Assignee: Assertio Therapeutics, Inc. (Assertio Holdings, Inc.)
• Original Assignee: Depomed Incorporated (Assertio Holdings, Inc.)
• Inventors: Hou, Sui Yuen Eddie
• Application Number:
  US12/940,911
• Publication Number:
  US 20110104272A1
• Time in Patent Office: Days
• US Class Current: 424/465
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61P 11/02 Nasal agents, e.g. decongestants
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Compositions and methods for the treatment of a mammal suffering from pain and from nasal congestion or ophthalmic disorders are described. More specifically, a dosage form designed for release of acetaminophen and phenylephrine is described, wherein the dosage form provides delivery of the drugs to the upper gastrointestinal tract (“GI”) of a mammal for an extended period of time.

Claims

1. A dosage form for extended release of acetaminophen and phenylephrine, comprising:

an extended release portion comprising a first dose of acetaminophen and a first dose of phenylephrine, both dispersed in a polymer matrix comprised of at least one hydrophilic polymer that swells upon imbibition of fluid to a size sufficient for gastric retention in a gastrointestinal tract of a subject in a fed mode, said first dose of acetaminophen released from the dosage form through erosion of the polymer matrix, and said first dose of phenylephrine released from the dosage form at a rate proportional to release of the acetaminophen during a period of gastric retention of between about 4 to about 8 hours.

2. The dosage form of claim 1, wherein the first dose of phenylephrine is released from the polymer matrix by diffusion.

3. The dosage form of claim 1, wherein the polymer matrix erodes during a period of drug release, wherein the period of drug release is at least 8, 9, 10, 11 or 12 hours.

4. The dosage form of claim 1, wherein the first dose of acetaminophen is approximately 400 mg to 800 mg and the first dose of phenylephrine is approximately 7.5-30 mg.

5. The dosage form of claim 1, wherein the polymer is a poly(ethylene oxide) having a molecular weight of between about 500,000 Daltons to about 12,000,000 Daltons.

6. The dosage form of claim 1, wherein the polymer is present in an amount ranging from about 35 weight percent to about 50 weight percent of the extended release portion.

7. The dosage form of claim 1, further comprising an immediate release portion comprising a second dose of acetaminophen and a second dose of phenylephrine, both of the second doses dispersed in the immediate release portion, said immediate release portion in contact with said extended release portion.

8. A method of making a dosage form for the extended release of acetaminophen and phenylephrine comprising, dry-blending the acetaminophen and the phenylephrine with at least one excipient to make a dry-blend mixture.

9. The method of claim 8, further comprising compressing the dry-blend mixture into a tablet and coating the tablet with an outer layer comprising a second drug, wherein the second drug is release immediately after ingestion or immersion in fluid.

10. The method of claim 9, wherein the second drug is phenylephrine.