Method of treating pain by administering 24 hour oral opioid formulations

• US 5,672,360 A
• Filed: 07/22/1996
• Issued: 09/30/1997
• Est. Priority Date: 11/23/1993
• Status: Expired due to Term

• Current Assignee: Purdue Pharma L.P.
• Original Assignee: Purdue Pharma L.P.
• Inventors: Kaiko, Robert F., Sackler, Richard S., Goldenheim, Paul
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): Benston, Jr., William E.
• Application Number:
  US08/578,688
• Time in Patent Office: 435 Days
• Field of Search: 424/490, 424/494, 424/497, 424/480, 424/468, 514/25, 514/490
• US Class Current: 424/490
• CPC Class Codes: A61K 31/485 Morphinan derivatives, e.g. morphine, codeine
• CPC Class Codes: A61K 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/4808 characterised by the form of the capsule or the structure of the filling; Capsules containing small tablets; Capsules with outer layer for immediate drug release capsules filled with granules or microparticles A61K9/16; filled with microcapsules or coated microparticles A61K9/50; with mixture of different granules, microcapsules, (coated) microparticles A61K9/5084
• CPC Class Codes: A61K 9/5026 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/5073 having two or more different coatings optionally including drug-containing subcoatings
• CPC Class Codes: A61K 9/5078 with drug-free core
• CPC Class Codes: A61P 25/04 Centrally acting analgesics, e.g. opioids
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Patients are treated with 24-hour oral sustained release opioid formulations which, upon administration, provide an initially rapid opioid absorption such that the minimum effective analgesic concentration of the opioid is more quickly achieved. These sustained release opioid formulations include an effective amount of at least one retardant material to cause said opioid analgesic to be released at a such a rate as to provide an analgesic effect after oral administration to a human patient for at least about 24 hours, and are characterized by providing an absorption half-life from 1 to about 8 hours. A method of titrating a human patient utilizing these sustained release opioid formulations is also disclosed.

Claims

1. A method of effectively treating pain in humans, comprising orally administering to a human patient on a once-a-day basis an oral sustained release dosage form containing an opioid analgesic or salt thereof which upon administration provides a time to maximum plasma concentration (T_max) of said opioid in about 2 to about 10 hours and a maximum plasma concentration (C_max) which is more than twice the plasma level of said opioid at about 24 hours after administration of the dosage form, and which dosage form provides effective treatment of pain for about 24 hours or more after administration to the patient.

2. The method of claim 1, wherein the T_max occurs in about 2 to about 8 hours after oral administration of said dosage form.

3. The method of claim 1, wherein the T_max occurs in about 6 to about 8 hours after oral administration of said dosage form.

4. The method of claim 1, wherein said opioid analgesic is morphine sulfate.

5. The method of claim 1, wherein said dosage form contains from about 5 mg to about 800 mg morphine.

6. A method of effectively treating pain in a human patient, comprising orally administering to a human patient on a once-a-day basis an oral sustained release dosage form containing an opioid analgesic or salt thereof which provides a maximum plasma concentration (C_max) which is more than twice the plasma level of said opioid at about 24 hours after administration of the dosage form, and which provides effective treatment of pain for about 24 hours or more after administration to the patient.

7. The method of claim 6, wherein said opioid analgesic is morphine sulfate.

8. The method of claim 6, wherein said dosage form contains from about 5 mg to about 800 mg morphine.

9. A method of effectively treating pain in humans, comprising orally administering to a human patient on a once-a-day basis an oral sustained release dosage form containing an opioid analgesic or salt thereof which at steady-state provides a time to maximum plasma concentration (T_max) of said opioid in about 2 to about 10 hours and a maximum plasma concentration (C_max) which is more than twice the plasma level of said opioid at about 24 hours after administration of the dosage form, and which dosage form provides effective treatment of pain for about 24 hours or more after administration to the patient.

10. The method of claim 9, wherein the T_max occurs from about 6 to about 8 hours after oral administration of said dosage form.

11. The method of claim 9, wherein said opioid analgesic is morphine sulfate.

12. A method of effectively treating pain in a human patient,comprising orally administering to a human patient on a once-a-day basis an oral sustained release dosage containing an opioid analgesic or salt thereof which at steady-state provides a maximum plasma concentration (C_max) which is more than twice the plasma level of said opioid at about 24 hours after administration of the dosage form, and which provides effective treatment of pain for about 24 hours or more after administration to the patient.

13. The method of claim 12, wherein said opioid analgesic is morphine sulfate.

14. The method of claim 12, wherein said dosage form contains from about 5 mg to about 800 mg morphine.