Sustained release oxycodone formulations with no fed/fast effect

• US 20010031278A1
• Filed: 04/05/2001
• Published: 10/18/2001
• Est. Priority Date: 05/31/1996
• Status: Abandoned Application

• Current Assignee: Benjamin Oshlack, Mark Chasin
• Original Assignee: Benjamin Oshlack, Mark Chasin
• Inventors: Oshlack, Benjamin, Chasin, Mark
• Application Number:
  US09/826,441
• Publication Number:
  US 20010031278A1
• Time in Patent Office: Days
• US Class Current: 424/457
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/1617 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/1635 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates

Abstract

A solid controlled release, oral dosage form, the dosage form comprising a therapeutically effective amount of oxycodone or a salt thereof together with a sustained release carrier which causes the formulation to preferentially release the drug in low pH (e.g., gastric fluid) is bioavailable and does not exhibit a fed/fast effect.

Claims

1. An oral solid sustained-release oral dosage form containing oxycodone which is bioavailable and does not exhibit a fed/fast effect, comprising

an analgesically effective amount of oxycodone or a salt thereof;

an effective amount of a sustained release carrier which preferentially causes said oxycodone to be released faster in simulated gastric fluid than in simulated intestinal fluid to provide analgesia for a time period from about 8 to about 24 hours when said dosage form is orally administered to a patient; and

optional pharmaceutical excipients.

2. A dosage form according to

claim 1

wherein said therapeutically effective amount of oxycodone is from about 2 mg to about 500 mg, calculated based on the hydrochloride salt.

3. A dosage form according to composition of

claim 1

, wherein said susteined-release carrier comprises an acrylic resin.

4. A dosage form according to

claim 1

which provides effective blood levels of oxycodone when administered to human patients for about 12 hours for about 24 hours.

5. A method for the preparation of an oral sustained release oxycodone formulation, the improvement comprising utilizing a sustained release carrier which preferentially releases oxycodone or a pharmaceutically acceptable salt thereof faster in simulated gastric fluid than in simulated intestinal fluid, such that the formulation is bioavailable and does not exhibit a fed/fast effect.

6. A method of treating patients having moderate to severe pain, comprising administering an oral sustained-release formulation comprising effective amount of oxycodone or a pharmaceutically acceptable salt thereof in a sustained release carrier which preferentially releases oxycodone or a pharmaceutically acceptable salt thereof faster in simulated gastric fluid than in simulated intestinal fluid, such that the formulation is bioavailable and does not exhibit a fed/fast effect.

7. A method of preparing an oral sustained-release oxycodone formulation which is bioavailable and which does not exhibit a fed/fast effect, comprising,

preparing a solid dosage form comprising an effective amount of oxycodone or a pharmaceutically acceptable salt thereof in a sustained release carrier which preferentially releases oxycodone or a pharmaceutically acceptable salt thereof faster in simulated gastric fluid than in simulated intestinal fluid, and optional pharmaceutical excipients, such that the formulation is bioavailable and does not exhibit a fed/fast effect.