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Claims for Patent: 6,733,783

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Claims for Patent: 6,733,783

Title: Controlled release hydrocodone formulations
Abstract:A solid oral controlled-release dosage form of hydrocodone is disclosed, the dosage form comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material.
Inventor(s): Oshlack; Benjamin (New York, NY), Masselink; John K. (Old Tappan, NJ), Huang; Hua-Pin (Englewood Cliffs, NJ), Tonelli; Alfred P. (Congers, NY)
Assignee: Euro-Celtique S.A. (Luxembourg, LU)
Application Number:10/016,651
Patent Claims: 1. A solid oral controlled-release dosage form suitable for 24 hour dosing in a human patient comprising a pharmaceutically acceptable matrix comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof and controlled release material selected from the group consisting of hydrophobic polymers, hydrophilic polymers, gums, protein derived materials, waxes, shellac, oils and mixtures thereof; said dosage form after administration to a human patient, providing a C.sub.24 /C.sub.max ratio of 0.55 to about 0.85; and said dosage form providing a therapeutic effect for at least about 24 hours.

2. The dosage form of claim 1, which provides a C.sub.24 /C.sub.max ratio of 0.55 to 0.75.

3. The dosage form of claim 1, wherein said matrix is a plurality of multiparticulate matrices.

4. The dosage form of claim 3, wherein said multiparticulates are compressed into a tablet.

5. The dosage form of claim 3, wherein said multiparticulates are disposed in a pharmaceutically acceptable capsule.

6. The dosage form of claim 1 which provides a C.sub.24 /C.sub.max ratio of 0.60 to 0.70.

7. The dosage form of claim 1 which provides a dissolution release rate in-vitro of the hydrocodone when measured by the USP Basket method at 100 rpm in 700 ml aqueous buffer at a pH of 1.2 at 37.degree. C. is at least 10% to about 45% by weight hydrocodone or salt thereof released at 1 hour.

8. The dosage form of claim 1, which provides a dissolution release rate in-vitro of the hydrocodone or salt thereof when measured by the USP Basket Method at 100 rpm in 700 ml Simulated Gastric Fluid (SGF) at 37.degree. C. for 1 hour and thereafter switching to 900 ml with Phosphate Buffer to a pH of 7.5 at 37.degree. C., of at least 20% by weight hydrocodone or salt thereof released at 4 hrs, from about 20% to about 65% by weight hydrocodone or salt thereof released at 8 hrs, from about 45% to about 85% by weight hydrocodone or salt thereof released at 12 hrs, and at least 80% by weight hydrocodone or salt thereof released at 24 hours.

9. The dosage form of claim 1, which provides a time to maximum plasma concentration (T.sub.max) of hydrocodone at about 4 to about 14 hours after oral administration of the dosage form.

10. The dosage form of claim 1, which provides a time to maximum plasma concentration (T.sub.max) of hydrocodone at about 6 to about 12 hours after oral administration of the dosage form.

11. The dosage form of claim 1, which provides a C.sub.max of hydrocodone which is less than 60% of the C.sub.max of an equivalent dose of an immediate release hydrocodone reference formulation.

12. The dosage form of claim 1, wherein said administration is first administration.

13. The dosage form of claim 1, wherein said administration is steady state administration.

14. The dosage form of claim 1, wherein said ratio is provided to a population of patients.

15. A solid oral controlled-release dosage form suitable for 24 hour dosing in a human patient comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof, and controlled release material selected from the group consisting of hydrophobic polymers, hydrophilic polymers, gums, protein derived materials, waxes, shellac, oils and mixtures thereof, said dosage form after oral administration, providing a rate of absorption during the time period from T.sub.max to about 24 hours after oral adminstration of the dosage form which is from about 45% to about 85% of the rate of elimination during the same time period, said dosage form providing a therapeutic effect for at least about 24 hours.

16. A method of providing analgesia in a human patient for at least about 24 hours comprising orally administering a dosage form comprising a pharmaceutically acceptable matrix comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof and controlled release material selected from the group consisting of hydrophobic polymers, hydrophilic polymers, gums, proteins derived materials, waxes, shellac, oils and mixtures thereof, said dosage form after administration to a human patient, providing a C.sub.24 /C.sub.max ratio of 0.55 to about 0.85 and a therapeutic effect for at least about 24 hours.

17. A process for the preparation of a solid oral controlled-release dosage form, comprising incorporating an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof into a controlled release material selected from the group consisting of hydrophobic polymers, hydrophilic polymers, gums, proteins derived materials, waxes, shellac, oils and mixtures thereof, forming a controlled release matrix formulation, said dosage form after administration to a human patient, providing a C.sub.24 /C.sub.max ratio of 0.55 to about 0.85 and a therapeutic effect for at least about 24 hours.

18. A solid oral controlled-release dosage form suitable for 24 hour dosing in a human patient comprising a plurality of pharmaceutically acceptable beads coated with an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof and overcoated with a pH-independent hydrophobic material, said dosage form providing, an in-vitro release rate, of hydrocodone or a pharmaceutically acceptable salt thereof, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37.degree. C. of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours; the in-vitro release rate being substantially independent of pH in that a difference, at any given time, between an amount of opioid released at one pH and an amount released at any other pH, when measured in-vitro using the USP Paddle Method of U.S. Pharmacopeia XXII (1990) at 100 rpm in 900 ml aqueous buffer, is no greater than 10%; said dosage form providing a C.sub.24 /C.sub.max ratio of 0.55 to about 0.85; and a therapeutic effect for at least 24 hours, after oral administration to a human patient.

19. The dosage form of claim 18, which provides a C.sub.24 /C.sub.max ratio of 0.55 to 0.75.

20. The dosage form of claim 18, which provides a time to maximum plasma concentration (T.sub.max) of hydrocodone at about 4 to about 14 hours after oral administration of the dosage form.

21. The dosage form of claim 18, which provides a time to maximum plasma concentration (T.sub.max) of hydrocodone at about 6 to about 12 hours after oral administration of the dosage form.

22. The dosage form of claim 18, which provides a C.sub.max of hydrocodone which is less than 60% of the C.sub.max of an equivalent dose of an immediate release hydrocodone reference formulation.

23. The dosage form of claim 18, wherein said administration is first administration.

24. The dosage form of claim 18, wherein said administration is steady state administration.

25. The dosage form of claim 18, wherein said ratio is provided to a population of patients.

26. A method of providing effective analgesia in a human patient for at least about 24 hours comprising orally administering a dosage form of claim 18 to a human patient.

27. A sustained release oral dosage form comprising: (a) a bilayer core comprising: (i) a drug layer comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof; and (ii) a displacement layer comprising an osmopolymer; and (b) a semipermeable wall surrounding the bilayer core having a passageway disposed therein for the release of said hdyrocodone or pharmaceutically acceptable salt thereof; said dosage form providing a C.sub.24 /C.sub.max ratio of 0.55 to about 0.85; and said dosage form providing a therapeutic effect for at least about 24 hours after oral administration to a human patient.

28. The dosage form of claim 27, which provides a C.sub.24 /C.sub.max ratio of 0.55 to 0.75.

29. The dosage form of claim 27, which provides a time to maximum plasma concentration (T.sub.max) of hydrocodone at about 4 to about 14 hours after oral administration of the dosage form.

30. The dosage form of claim 27, which provides a time to maximum plasma concentration (T.sub.max) of hydrocodone at about 6 to about 12 hours after oral administration of the dosage form.

31. The dosage form of claim 27, which provides a C.sub.max of hydrocodone which is less than 60% of the C.sub.max of an equivalent dose of an immediate release hydrocodone reference formulation.

32. The dosage form of claim 27, wherein said administration is first administration.

33. The dosage form of claim 27, wherein said administration is steady state administration.

34. The dosage form of claim 27, which provides a dissolution release rate in-vitro of the hydrocodone or salt thereof when measured by the USP Basket Method at 100 rpm in 700 ml Simulated Gastric Fluid (SGF) at 37.degree. C. for 1 hour and thereafter switching to 900 ml with Phosphate Buffer to a pH of 7.5 at 37.degree. C., of at least 20% by weight hydrocodone or salt thereof released at 4 hrs, from about 20% to about 65% by weight hydrocodone or salt thereof released at 8 hrs, from about 45% to about 85% by weight hydrocodone or salt thereof released at 12 hrs, and at least 80% by weight hydrocodone or salt thereof released at 24 hours.

35. The dosage form of claim 27, wherein said ratio is provided to a population of patients.

36. A method of providing effective analgesia in a human patient for at least about 24 hours comprising orally administering a dosage form of claim 27 to a human patient.

37. A sustained release oral dosage form comprising: (a) a bilayer core comprising: (i) a drug layer comprising an analgesically effective amount of hydrocodone or a pharmaceutically acceptable salt thereof; and (ii) a displacement layer comprising an osmopolymer; and (b) a semipermeable wall surrounding the bilayer core having a passageway disposed therein for the release of said hydrocodone or pharmaceutically acceptable salt thereof; said dosage form providing an in-vitro release rate, of hydrocodone or a pharmaceutically acceptable salt thereof, when measured by the USP Basket Method at 100 rpm in 900 ml aqueous buffer at a pH of between 1.6 and 7.2 at 37.degree. C. of from 0% to about 35% at 1 hour, from about 10% to about 70% at 4 hours, from about 20% to about 75% at 8 hours, from about 30% to about 80% at 12 hours, from about 40% to about 90% at 18 hours, and greater than about 60% at 24 hours; the in-vitro release rate being substantially independent of pH in that a difference, at any given time, between an amount of opioid released at one pH and an amount released at any other pH, when measured in-vitro using the USP Paddle Method of U.S. Pharmacopeia XXII (1990) at 100 rpm in 900 ml aqueous buffer, is no greater than 10%.

38. A method of providing effective analgesia in a human patient for at least about 24 hours comprising orally administering a dosage form of claim 37 to a human patient.

39. The controlled release dosage form claim 1, wherein said controlled release material is a hydrophobic polymer selected from the group consisting of alkylcelluloses and acrylic resins.

40. The controlled release dosage form of claim 18, wherein said hydrophobic material is selected from the group consisting of a cellulosic polymer, an acrylic polymer, and mixtures thereof.
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