Pharmaceutical preparation containing oxycodone and naloxone
The invention concerns a storage stable pharmaceutical preparation comprising oxycodone and naloxone for use in pain therapy, with the active compounds being released from the preparation in a sustained, invariant and independent manner.
1. An oral sustained release pharmaceutical formulation comprising:
10 to 30 mg of oxycodone or a pharmaceutically acceptable salt thereof; and
naloxone or a pharmaceutically acceptable salt thereof;
wherein the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof are present in the pharmaceutical formulation in a weight ratio of 2:1 and are released from the pharmaceutical formulation in a sustained manner;
wherein the formulation is a tablet.
2. The pharmaceutical formulation of claim 1 , wherein the oxycodone is present in the form of a pharmaceutically acceptable salt thereof.
3. The pharmaceutical formulation of claim 1 , wherein the oxycodone is present in the form of oxycodone hydrochloride.
4. The pharmaceutical formulation of claim 1 , wherein the naloxone is present in the form of a pharmaceutically acceptable salt thereof.
5. The pharmaceutical formulation of claim 1 , wherein the naloxone is present in the form of naloxone hydrochloride.
6. The pharmaceutical formulation of claim 1 , wherein the oxycodone is present in the form of oxycodone hydrochloride, and the naloxone is present in the form of naloxone hydrochloride.
7. The pharmaceutical formulation of claim 1 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 10 mg.
8. The pharmaceutical formulation of claim 1 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 12 mg.
9. The pharmaceutical formulation of claim 1 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 20 mg.
10. The pharmaceutical formulation of claim 1 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 30 mg.
11. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof over 2 to 24 hours.
12. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof over 2 to 16 hours.
13. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof over 2 to 12 hours.
14. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release 40% to 80% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 2 hours.
15. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release 70% to 100% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 4 hours.
16. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release 70% to 100% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 7 hours.
17. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release 85% to 100% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 12 hours.
18. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof in equal percent amounts per unit time.
19. The pharmaceutical formulation of claim 1 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof such that
the percent released of the oxycodone or pharmaceutically acceptable salt thereof deviates from the percent released of the naloxone or pharmaceutically acceptable salt by not more than 20%, and
the percent released of the naloxone or pharmaceutically acceptable salt thereof deviates from the percent released of the oxycodone or pharmaceutically acceptable salt by not more than 20%.
20. The pharmaceutical formulation of claim 1 , wherein the formulation comprises a sustained release matrix that contains and releases the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof.
21. The pharmaceutical formulation of claim 20 , wherein
the oxycodone is present in the form of oxycodone hydrochloride, and the naloxone is present in the form of naloxone hydrochloride;
the matrix is formulated to release 85% to 100% of the oxycodone hydrochloride and the naloxone hydrochloride by 12 hours; and
the matrix is formulated to release the oxycodone hydrochloride and the naloxone hydrochloride in equal percent amounts per unit time.
22. A method of treating pain comprising administering to a subject in need thereof the pharmaceutical composition of claim 1 .
23. An oral sustained release pharmaceutical formulation comprising:
oxycodone or a pharmaceutically acceptable salt thereof; and
1 to 10 mg of naloxone or a pharmaceutically acceptable salt thereof;
wherein the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof are present in the pharmaceutical formulation in a weight ratio of 2:1 and are released from the pharmaceutical formulation in a sustained manner,
wherein the formulation is a tablet.
24. The pharmaceutical formulation of claim 23 , wherein the oxycodone is present in the form of a pharmaceutically acceptable salt thereof.
25. The pharmaceutical formulation of claim 23 , wherein the oxycodone is present in the form of oxycodone hydrochloride.
26. The pharmaceutical formulation of claim 23 , wherein the naloxone is present in the form of a pharmaceutically acceptable salt thereof.
27. The pharmaceutical formulation of claim 23 , wherein the naloxone is present in the form of naloxone hydrochloride.
28. The pharmaceutical formulation of claim 23 , wherein the oxycodone is present in the form of oxycodone hydrochloride, and the naloxone is present in the form of naloxone hydrochloride.
29. The pharmaceutical formulation of claim 23 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 5 mg.
30. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof over 2 to 24 hours.
31. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof over 2 to 16 hours.
32. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof over 2 to 12 hours.
33. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release 40% to 80% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 2 hours.
34. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release 70% to 100% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 4 hours.
35. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release 70% to 100% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 7 hours.
36. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release 85% to 100% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 12 hours.
37. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof in equal percent amounts per unit time.
38. The pharmaceutical formulation of claim 23 , wherein the formulation is formulated to release the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof such that
the percent released of the oxycodone or pharmaceutically acceptable salt thereof deviates from the percent released of the naloxone or pharmaceutically acceptable salt by not more than 20%, and
the percent released of the naloxone or pharmaceutically acceptable salt thereof deviates from the percent released of the oxycodone or pharmaceutically acceptable salt by not more than 20%.
39. The pharmaceutical formulation of claim 23 , wherein the formulation comprises a sustained release matrix that contains and releases the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof.
40. The pharmaceutical formulation of claim 39 , wherein
the oxycodone is present in the form of oxycodone hydrochloride, and the naloxone is present in the form of naloxone hydrochloride;
the matrix is formulated to release 85% to 100% of the oxycodone hydrochloride and the naloxone hydrochloride by 12 hours; and
the matrix is formulated to release the oxycodone hydrochloride and the naloxone hydrochloride in equal percent amounts per unit time.
41. A method of treating pain comprising administering to a subject in need thereof the pharmaceutical composition of claim 23 .