Tamper resistant dosage forms
The present invention relates to pharmaceutical dosage forms, for example to a tamper resistant dosage form including an opioid analgesic, and processes of manufacture, uses, and methods of treatment thereof.
1. A cured shaped extended release tablet comprising:
(1) at least one high molecular weight polyethylene oxide having, based on rheological measurements, an approximate molecular weight selected from 4,000,000 and 7,000,000; and
(2) oxycodone or a pharmaceutically acceptable salt;
wherein said tablet is prepared by a process comprising the steps of:
(a) forming a tablet-shaped pharmaceutical preparation comprising said oxycodone or pharmaceutically acceptable salt thereof and said high molecular weight polyethylene oxide;
(b) curing said tablet-shaped pharmaceutical preparation by subjecting said preparation to a temperature from about 60° C. to about 90° C. for a time of from about 15 minutes to about 10 hours; and
(c) optionally applying at least one coating to said tablet-shaped pharmaceutical preparation, before, during or after curing;
wherein said tablet comprises:
(i) 5, 7.5, 10, 15, 20, or 30 mg of said oxycodone or pharmaceutically acceptable salt thereof, and at least 79% by weight of said high molecular weight polyethylene oxide;
(ii) 40 mg of said oxycodone or pharmaceutically acceptable salt thereof, and at least 72% by weight of said high molecular weight polyethylene oxide;
(iii) 60 mg of said oxycodone or pharmaceutically acceptable salt thereof, and at least 57% by weight of said high molecular weight polyethylene oxide; or
(iv) 80 mg of said oxycodone or pharmaceutically acceptable salt thereof, and at least 54% by weight of said high molecular weight polyethylene oxide; and
wherein percent by weight is based upon the total weight of said tablet-shaped pharmaceutical preparation, not including the combined weight of said applied coatings.
2. A tablet as defined in claim 1 , wherein said oxycodone or pharmaceutically acceptable salt thereof is oxycodone hydrochloride.
3. A tablet as defined in claim 1 , wherein said time in said curing step is from about 30 minutes to about 90 minutes.
4. A tablet as defined in claim 1 , wherein said temperature in said curing step is from about 62° C. to about 90° C.
5. A tablet as defined in claim 1 , wherein at least one coating is applied to said tablet-shaped pharmaceutical preparation, before, during or after said curing step.
6. A tablet as defined in claim 1 , wherein said tablet comprises 5, 7.5, 10, 15, 20, or 30 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 79%.
7. A tablet as defined in claim 1 , wherein said tablet comprises 40 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 72%.
8. A tablet as defined in claim 1 , wherein said tablet comprises 60 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 57%.
9. A tablet as defined in claim 1 , wherein said tablet comprises 80 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 54%.
10. A tablet as defined in claim 1 , wherein said curing comprises convection curing in a convection curing device.
11. A tablet as defined in claim 1 , wherein said cured tablet-shaped pharmaceutical preparation has a density that is at least about 1% lower than the density of said preparation prior to curing.
12. A tablet as defined in claim 1 , wherein said tablet-shaped pharmaceutical preparation is formed by direct compression.
13. A tablet as defined in claim 12 , wherein said tablet comprises 5, 7.5, 10, 15, 20, or 30 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 79%.
14. A tablet as defined in claim 12 , wherein said tablet comprises 40 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 72%.
15. A tablet as defined in claim 12 , wherein said tablet comprises 60 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 57%.
16. A tablet as defined in claim 12 , wherein said tablet comprises 80 mg of said oxycodone or pharmaceutically acceptable salt thereof; said high molecular weight polyethylene oxide has an approximate molecular weight of 4,000,000; and the percent by weight of said high molecular weight polyethylene oxide is at least 54%.
17. A tablet as defined in claim 12 , wherein said curing comprises curing in a convection curing device.
18. A tablet as defined in claim 12 , wherein said cured tablet-shaped pharmaceutical preparation has a density that is at least about 1% lower than the density of said preparation prior to curing.
19. A tablet as defined in claim 12 , wherein said cured tablet-shaped pharmaceutical preparation has a density that is at least about 2% lower than the density of said preparation prior to curing.
20. A cured shaped extended release tablet comprising:
(1) at least one high molecular weight polyethylene oxide having, based on rheological measurements, an approximate molecular weight selected from 4,000,000 and 7,000,000; and
(2) an opioid analgesic or a pharmaceutically acceptable salt thereof;
wherein said tablet is prepared by a process comprising the steps of:
(a) forming a tablet-shaped pharmaceutical preparation comprising said opioid or pharmaceutically acceptable salt thereof and said high molecular weight polyethylene oxide;
(b) curing said tablet-shaped pharmaceutical preparation by subjecting said preparation to a temperature from about 60° C. to about 90° C. for a time of from about 15 minutes to about 10 hours; and
(c) optionally applying at least one coating to said tablet-shaped pharmaceutical preparation, before, during or after curing;
wherein said high molecular weight polyethylene oxide is in an amount of at least 54%, by weight, based upon the total weight of said tablet-shaped pharmaceutical preparation, not including the combined weight of said applied coatings.
21. A tablet as defined in claim 20 , wherein, said temperature in said curing step is from about 62° C. to about 90° C.
22. A tablet as defined in claim 20 , wherein at least one coating is applied to said tablet-shaped pharmaceutical preparation, before, during or after said curing step.
23. A tablet as defined in claim 20 , wherein the percent by weight of said high molecular weight polyethylene oxide is at least 80%, and said opioid analgesic or pharmaceutically acceptable salt comprises hydrocodone or a pharmaceutically acceptable salt thereof.
24. A tablet as defined in claim 20 , wherein the percent by weight of said high molecular weight polyethylene oxide is at least 80%, and said opioid analgesic or pharmaceutically acceptable salt thereof comprises hydromorphone or a pharmaceutically acceptable salt thereof.
25. A tablet as defined in claim 24 , wherein said hydromorphone or pharmaceutically acceptable salt thereof comprises hydromorphone hydrochloride.
26. A tablet as defined in claim 20 , wherein the percent by weight of said high molecular weight polyethylene oxide is at least 80%, and said opioid analgesic or pharmaceutically acceptable salt comprises oxymorphone or a pharmaceutically acceptable salt thereof.
27. A tablet as defined in claim 26 , wherein the percent by weight of said high molecular weight polyethylene oxide is at least 80%, and said oxymorphone or pharmaceutically acceptable salt thereof comprises oxymorphone hydrochloride.
28. A tablet as defined in claim 20 , wherein the percent by weight of said high molecular weight polyethylene oxide is at least 80%, and said opioid analgesic or pharmaceutically acceptable salt comprises morphine or a pharmaceutically acceptable salt thereof.
29. A tablet as defined in claim 20 , wherein said curing comprises convection curing in a convection curing device.
30. A tablet as defined in claim 20 , wherein said cured tablet-shaped pharmaceutical preparation has a density that is at least about 1% lower than the density of said preparation prior to curing.