Once-a-day oxycodone formulations
The invention is directed to sustained release formulations containing oxycodone or a pharmaceutically acceptable salt thereof which provide a mean C 24 /C max oxycodone ratio of 0.6 to 1.0 or 0.7 to 1 after oral administration at steady state to patients and methods thereof.
1. A sustained-release oral dosage form for once-a-day administration comprising:
a pharmaceutically acceptable matrix comprising an analgesically effective amount of oxycodone or a pharmaceutically acceptable salt thereof and a sustained release material, said dosage form providing an analgesic effect for at least about 24 hours after oral administration at steady state to human patients; and
said dosage form providing a mean C 24 /C max oxycodone ratio of 0.7 to 1.0 and a mean T max of about 6.5 to about 17 hours after steady state oral administration to said patients.
2. The dosage form of claim 1 , wherein the matrix is substantially homogeneous.
3. The dosage form of claim 1 , wherein said matrix is contained within a gelatin capsule.
4. The dosage form of claim 1 , wherein said matrix is formulated into a tablet.
5. The dosage form of claim 1 , wherein said amount is from about 5 to about 640 mg.
6. The dosage form of claim 1 , wherein said pharmaceutically acceptable salt of oxycodone is oxycodone hydrochloride.
7. The dosage form of claim 1 , which provides a mean C 24 /C max ratio of 0.7 to 0.99 after administration at steady state to said patients.
8. The dosage form of claim 1 , which provides a mean C 24 /C max ratio of 0.8 to 0.95 after administration at steady state to said patients.
9. The dosage form of claim 1 , which provides an in-vitro release rate, of oxycodone 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 40% at 1 hour, from about 8% to about 70% at 4 hours, from about 20% to about 80% at 8 hours, from about 30% to about 95% at 12 hours, from about 35% to about 95% at 18 hrs, and greater than about 50% at 24 hours.
10. A sustained-release oral dosage form for once-a-day administration comprising:
a pharmaceutically acceptable matrix comprising an analgesically effective amount of oxycodone or a pharmaceutically acceptable salt thereof and a sustained release material, said dosage form providing an analgesic effect for at least about 24 hours after oral administration at steady state to human patients; and
said dosage form providing a mean C 24 /C max oxycodone ratio of 0.74 to 0.95 and a mean T max at about 6.5 to about 17 hours after oral administration at steady state to said patients.
11. A sustained-release oral dosage form for once-a-day administration comprising:
a pharmaceutically acceptable matrix comprising an analgesically effective amount of oxycodone or a pharmaceutically acceptable salt thereof and a sustained release material, said dosage form providing an analgesic effect for at least about 24 hours after oral administration at steady state to human patients; and
said dosage form providing a mean C 24 /C max oxycodone ratio of 0.72 to 0.99 and a mean T max at about 6.5 to about 17 hours after oral administration at steady state to said patients.
12. A method of preparing a sustained release dosage form comprising incorporating oxycodone or a pharmaceutically acceptable salt thereof and a sustained release material into a pharmaceutically acceptable matrix, and preparing the dosage form comprising the matrix, such that the dosage form provides an analgesic effect for at least about 24 hours, a mean C 24 /C max oxycodone ratio of 0.7 to 1.0 and a mean T max at about 6.5 to about 17 hours after administration at steady state to human patients.
13. The dosage form of any one of claims 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 , or 11 which provides a mean T max of oxycodone at about 10 to about 16 hours after administration at steady state to said patients.
14. The dosage form of any one of claims 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 9 , 10 , or 11 which provides a mean T max of oxycodone at about 12 to about 16 hours after administration at steady state to said patients.
15. The dosage form of claim 1 , wherein said oxycodone is the only active agent in the dosage form.
16. The dosage form of claim 10 , wherein said oxycodone is the only active agent in the dosage form.
17. The dosage form of claim 11 , wherein said oxycodone is the only active agent in the dosage form.