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 - 32 . (canceled)
33 . An oral sustained release pharmaceutical formulation comprising:
10 to 80 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 a weight ratio of 2:1.
34 . The pharmaceutical formulation of claim 33 , wherein the oxycodone is present in the form of a pharmaceutically acceptable salt thereof.
35 . The pharmaceutical formulation of claim 34 , wherein the oxycodone is present in the form of oxycodone hydrochloride.
36 . The pharmaceutical formulation of claim 33 , wherein the naloxone is present in the form of a pharmaceutically acceptable salt thereof.
37 . The pharmaceutical formulation of claim 36 , wherein the naloxone is present in the form of naloxone hydrochloride.
38 . The pharmaceutical formulation of claim 33 , wherein the oxycodone is present in the form of oxycodone hydrochloride, and the naloxone is present in the form of naloxone hydrochloride.
39 . The pharmaceutical formulation of claim 33 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount ranging from 10 to 40 mg.
40 . The pharmaceutical formulation of claim 39 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 10 mg.
41 . The pharmaceutical formulation of claim 39 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 20 mg.
42 . The pharmaceutical formulation of claim 39 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 30 mg.
43 . The pharmaceutical formulation of claim 39 , wherein the oxycodone or pharmaceutically acceptable salt thereof is present in an amount of 40 mg.
44 . The pharmaceutical formulation of claim 33 , wherein the formulation is a tablet.
45 . The pharmaceutical formulation of claim 33 , 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.
46 . The pharmaceutical formulation of claim 45 , 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.
47 . The pharmaceutical formulation of claim 46 , 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.
48 . The pharmaceutical formulation of claim 33 , wherein the formulation is formulated to release 1% to 40% of the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof by 15 minutes.
49 . The pharmaceutical formulation of claim 33 , 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.
50 . The pharmaceutical formulation of claim 33 , 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.
51 . The pharmaceutical formulation of claim 33 , 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.
52 . The pharmaceutical formulation of claim 33 , 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.
53 . The pharmaceutical formulation of claim 33 , wherein the formulation comprises a sustained release matrix that contains the oxycodone or pharmaceutically acceptable salt thereof and the naloxone or pharmaceutically acceptable salt thereof.
54 . The pharmaceutical formulation of claim 53 , wherein the matrix is substantially non-swellable.
55 . The pharmaceutical formulation of claim 53 , wherein the matrix is non-erosive.
56 . The pharmaceutical formulation of claim 53 , wherein the matrix provides release of the oxycodone or pharmaceutically acceptable salt thereof and of the naloxone or pharmaceutically acceptable salt thereof in an invariant manner.
57 . The pharmaceutical formulation of claim 56 , wherein the matrix provides release of the oxycodone or pharmaceutically acceptable salt thereof and of the naloxone or pharmaceutically acceptable salt thereof in an independent manner.
58 . The pharmaceutical formulation of claim 33 , 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.
59 . The pharmaceutical formulation of claim 58 , wherein
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%.
60 . The pharmaceutical formulation of claim 53 , wherein
the oxycodone or pharmaceutically acceptable salt thereof is present in an amount ranging from 10 to 40 mg;
the oxycodone is present in the form of oxycodone hydrochloride, and the naloxone is present in the form of naloxone hydrochloride; and
the matrix is formulated to release the oxycodone hydrochloride and the naloxone hydrochloride in equal percent amounts per unit time.
61 . A method of treating pain comprising administering to a subject in need thereof the pharmaceutical composition of claim 33 .
62 . A method of reducing oxycodone-induced side effects comprising administering to a subject in need thereof the pharmaceutical composition of claim 33 .