Controlled release hydrocodone
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.
1. A once-a-day oral controlled-release dosage form comprising hydrocodone or a pharmaceutically acceptable salt thereof and a controlled release material comprising a hydrophobic and/or hydrophilic material,
wherein the controlled release material is included in an effective amount such that the dosage form provides a rate of absorption during the time period from T max to about 24 hours after oral administration of the dosage form to an individual patient which is from about 45% to about 85% of the rate of elimination during the same time period, and
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° 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.
2. The dosage form of claim 1 , which provides a W 50 for the hydrocodone of between 4 and 22 hours.
3. The dosage form of claim 2 , wherein the W 50 is at least 4 hours.
4. The dosage form of claim 2 , wherein the W 50 is at least 12 hours.
5. The dosage form of claim 1 , wherein the W 50 is at least 18 hours.
6. The dosage form of claim 1 , which provides a time to peak plasma concentration of hydrocodone at about 6 to about 12 hours after said administration.
7. The dosage form of claim 1 , which provides a time to peak plasma concentration of hydrocodone at about 8 to about 10 hours after said administration.
8. The dosage form of claim 1 , which provides a time to peak plasma concentration of hydrocodone at about 4 to about 10 hours after said administration.
9. The dosage form of claim 1 , which provides a time to peak plasma concentration of hydrocodone at about 8 to about 14 hours after said administration.
10. The dosage form of claim 1 , wherein the hydrophobic material is selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.
11. The dosage form of claim 1 , wherein the controlled release material is incorporated into a matrix along with the hydrocodone.
12. The dosage form of claim 1 , wherein the controlled release material is applied as a sustained release coating over a substrate comprising the hydrocodone, and the substrate is selected from the group consisting of beads, pellets, spheroids, tablets and tablet cores.
13. The dosage form of claim 1 , wherein said administration is first administration.
14. The dosage form of claim 1 , which comprises a core and a coating.
15. The dosage form of claim 14 , which is a compressed tablet.
16. A once-a-day oral controlled-release dosage form comprising hydrocodone or a pharmaceutically acceptable salt thereof and a controlled release material comprising a hydrophobic and/or hydrophilic material,
wherein the controlled release material is included in an effective amount such that the dosage form provides a mean rate of absorption during the time period from T max to about 24 hours after oral administration of the dosage form to a group of patients which is from about 45% to about 85% of the mean rate of elimination during the same time period, and
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° 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.
17. The dosage form of claim 16 , which provides a mean W 50 for the hydrocodone of between 4 and 22 hours.
18. The dosage form of claim 17 , wherein the mean W 50 is at least 4 hours.
19. The dosage form of claim 17 , wherein the mean W 50 is at least 12 hours.
20. The dosage form of claim 17 , wherein the mean W 50 is at least 18 hours.
21. The dosage form of claim 17 , which provides a mean time to peak plasma concentration of hydrocodone at about 6 to about 12 hours after said administration.
22. The dosage form of claim 16 , which provides a mean time to peak plasma concentration of hydrocodone at about 8 to about 10 hours after said administration.
23. The dosage form of claim 16 , which provides a mean time to peak plasma concentration of hydrocodone at about 4 to about 10 hours after said administration.
24. The dosage form of claim 16 , which provides a mean time to peak plasma concentration of hydrocodone at about 8 to about 14 hours after said administration.
25. The dosage form of claim 16 , wherein the hydrophobic material is selected from the group consisting of gums, cellulose ethers, acrylic resins, waxes, shellac and oils.
26. The dosage form of claim 16 , wherein the controlled release material is incorporated into a matrix along with the hydrocodone.
27. The dosage form of claim 16 , wherein the controlled release material is applied as a sustained release coating over a substrate comprising the hydrocodone, and the substrate is selected from the group consisting of beads, pellets, spheroids, tablets and tablet cores.
28. The dosage form of claim 16 , wherein said administration is first administration.
29. The dosage form of claim 16 , which comprises a core and a coating.
30. The dosage form of claim 29 , which is a compressed tablet.
31. The dosage form of claim 1 , wherein said hydrocodone or pharmaceutically acceptable salt thereof is the only active agent in the dosage form.
32. The dosage form of claim 31 , wherein the dosage form comprises said pharmaceutically acceptable salt of hydrocodone, and said pharmaceutically acceptable salt of hydrocodone is a bitartrate salt of hydrocodone.
33. The dosage form of claim 16 , wherein said hydrocodone or pharmaceutically acceptable salt thereof is the only active agent in the dosage form.
34. The dosage form of claim 33 , wherein the dosage form comprises said pharmaceutically acceptable salt of hydrocodone, and said pharmaceutically acceptable salt of hydrocodone is a bitartrate salt of hydrocodone.