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Claims for Patent: 8,741,885

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Claims for Patent: 8,741,885

Title:Gastric retentive extended release pharmaceutical compositions
Abstract: The present disclosure provides extended release pharmaceutical compositions comprising an opioid and an additional active pharmaceutical ingredient, wherein the composition exhibits gastric retentive properties which are achieved by a combination of a physical property of the composition and release of the opioid, wherein upon administration to a subject, the composition has at least one pharmacokinetic parameter that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.
Inventor(s): Devarakonda; Krishna (St. Louis, MO), Guiliani; Michael J (Creve Coeur, MO), Gupta; Vishal K (Hillsborough, NJ), Heasley; Ralph A (Webster Groves, MO), Shelby; Susan (Creve Coeur, MO)
Assignee: Mallinckrodt LLC (Hazelwood, MO)
Application Number:13/473,571
Patent Claims: 1. An extended release pharmaceutical composition, comprising: an immediate release portion comprising, by total weight of the immediate release portion, about 0.5% to about 2.5% of oxycodone or a pharmaceutically acceptable salt of oxycodone, and about 65% to about 85% of acetaminophen; and an extended release portion comprising, by total weight of the extended release portion, about 0.3% to about 1.0% of oxycodone or a pharmaceutically acceptable salt of oxycodone and about 15% to about 25% of acetaminophen; wherein the total amount of acetaminophen in the composition is about 200 mg to about 650 mg, and the total amount of oxycodone or salt in the composition is about 5 mg to about 15 mg; wherein when the composition is orally administered to a subject in need thereof the composition delivers the oxycodone or the pharmaceutically acceptable salt thereof and the acetaminophen to the subject's upper gastrointestinal tract for at least about 4 hours to about 12 hours; and wherein either the oxycodone or the acetaminophen produces a plasma profile characterized by at least one pharmacokinetic parameter selected from the group consisting of C.sub.max, C.sub.1hr, C.sub.2h, AUC, partial AUC, T.sub.max, and T.sub.lag that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.

2. The extended release pharmaceutical composition of claim 1, wherein the pharmacokinetic parameter selected from the group consisting of C.sub.max, C.sub.1hr, C.sub.2h, AUC, partial AUC, T.sub.max, and T.sub.lag differs by less than about 20%.

3. The extended release pharmaceutical composition of claim 1, wherein the pharmacokinetic parameter is selected from the group consisting of AUC and C.sub.max.

4. The extended release pharmaceutical composition of claim 1, wherein both the oxycodone and the acetaminophen produce a plasma profile characterized by at least one pharmacokinetic parameter selected from the group consisting of C.sub.max, C.sub.1hr, C.sub.2h, AUC, partial AUC, T.sub.max, and T.sub.lag that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.

5. The extended release pharmaceutical composition of claim 1, wherein the composition releases the oxycodone at a rate that is sufficient to delay gastric emptying but insufficient to cause an adverse gastrointestinal effect.

6. The extended release pharmaceutical composition of claim 1, wherein the extended release portion comprises at least one extended release polymer.

7. The extended release pharmaceutical composition of claim 6, wherein the at least one extended release polymer is a polyethylene oxide.

8. The extended release pharmaceutical composition of claim 7, wherein the polyethylene oxide has a molecular weight from about 500,000 Daltons to about 10,000,000 Daltons.

9. The extended release pharmaceutical composition of claim 6, wherein the at least one extended release polymer absorbs water and swells to a size sufficient for gastric retention.

10. The extended release pharmaceutical composition of claim 1, wherein the total amount of the acetaminophen in the composition is about 325 mg; and the total amount of the oxycodone in the composition is about 7.5 mg.

11. The extended release pharmaceutical composition of claim 1, wherein the composition delivers the oxycodone or the pharmaceutically acceptable salt thereof and the acetaminophen to the subject's upper gastrointestinal tract for at least about 6 hours.

12. The extended release composition of claim 1, wherein the composition comprises (a) two immediate release portions in which one of the immediate release portions contains the oxycodone and the other immediate release portion contains the acetaminophen, and (b) two extended release portions in which one of the extended release portions contains the oxycodone and the other extended release portion contains the acetaminophen.

13. An extended release therapeutically effective pharmaceutical composition, comprising: at least one immediate release portion comprising oxycodone or a pharmaceutically acceptable salt thereof and acetaminophen and at least one extended release portion comprising an extended release component, oxycodone or a pharmaceutically acceptable salt thereof, and acetaminophen; wherein the at least one immediate release portion comprises from about 20% to about 30% (w/w) of the total amount of the oxycodone or a pharmaceutically acceptable salt thereof, and about 40% to about 60% (w/w) of the total amount of the acetaminophen in the composition; wherein the at least one extended release portion comprises from about 70% to about 80% (w/w) of the total amount of the oxycodone or a pharmaceutically acceptable salt thereof, and about 40% to about 60% (w/w) of the total amount of the acetaminophen in the composition; wherein the sum of the amounts of the acetaminophen in the immediate release and the extended release portions is about 325 mg; wherein the sum of the amounts of the oxycodone or pharmaceutically acceptable salt thereof in the immediate release and extended release portions is about 7.5 mg; and wherein the bioavailability of the acetaminophen and the oxycodone or the pharmaceutically acceptable salt thereof is not affected by the absence of food in a subject's gastrointestinal tract.

14. The extended release therapeutically effective pharmaceutical composition of claim 13, wherein when the pharmaceutical composition is administered to a subject under fasted conditions, mean AUC for oxycodone of the subject is about 9.0 nghr/mL/mg to about 18.5 nghr/mL/mg and the mean AUC for acetaminophen of the subject is about 35.0 nghr/mL/mg to about 80.0 nghr/mL/mg.

15. The extended release therapeutically effective pharmaceutical composition of claim 13, wherein the pharmaceutical composition is prepared using a process comprising dual granulation.

16. The extended release therapeutically effective pharmaceutical composition of claim 15, wherein the dual granulation comprises (a) granulating a first mixture comprising the oxycodone or a pharmaceutically acceptable salt thereof and at least one excipient to form a plurality of oxycodone-protected granules; and (b) granulating a second mixture comprising the plurality of oxycodone-protected granules, the acetaminophen, and at least one excipient to form a plurality of tablet granules.

17. The extended release therapeutically effective pharmaceutical composition of claim 16, wherein the plurality of oxycodone-protected granules further comprises at least one excipient selected from the group consisting of a binder, a filler, an antioxidant, and a chelating agent.

18. The extended release therapeutically effective pharmaceutical composition of claim 13, wherein the composition has gastric retentive properties.

19. A method of treating acute pain in a patient in need thereof, comprising administering a therapeutically effective amount of a pharmaceutical composition of claim 13 to the patient.

20. The extended release pharmaceutical composition of claim 1, wherein the composition is gastric retentive.

21. A method of treating acute pain in a patient in need thereof, comprising administering a therapeutically effective amount of a pharmaceutical composition of claim 1 to the patient.

22. An extended release pharmaceutical composition, comprising: an immediate release portion comprising about 20% to about 30% (w/w) of the total amount of the oxycodone or a pharmaceutically acceptable salt thereof in the composition, and about 40% to about 60% (w/w) of the total amount of the acetaminophen in the composition; and an extended release portion comprising about 70% to about 80% (w/w) of the total amount of the oxycodone or a pharmaceutically acceptable salt thereof in the composition, and about 40% to about 60% (w/w) of the total amount of the acetaminophen in the composition; wherein the total amount of acetaminophen in the composition is about 200 mg to about 650 mg, and the total amount of oxycodone or salt in the composition is about 5 mg to about 15 mg; wherein when the composition is orally administered to a subject in need thereof the composition delivers the oxycodone or the pharmaceutically acceptable salt thereof and the acetaminophen to the subject's upper gastrointestinal tract for at least about 4 hours; and wherein either the oxycodone or the acetaminophen produces a plasma profile characterized by at least one pharmacokinetic parameter selected from the group consisting of C.sub.max, C.sub.1hr, C.sub.2h, AUC, partial AUC, T.sub.max, and T.sub.lag that differs by less than about 30% when the subject is in a fasted state as compared to a fed state.

23. The extended release pharmaceutical composition of claim 22, wherein the composition is a bilayer tablet.

24. The extended release pharmaceutical composition of claim 22, wherein the composition comprises about 325 mg of acetaminophen and about 7.5 mg of oxycodone.

25. The extended release pharmaceutical composition of claim 22, wherein the composition further comprises at least one extended release polymer.

26. A method of treating acute pain in a patient in need thereof, comprising administering a therapeutically effective amount of a pharmaceutical composition of claim 22 to the patient.

27. The method of claim 26, wherein the composition is administered to the patient at 8-hour, 12-hour, or 24-hour dosing intervals.

28. The method of claim 26, wherein the composition is administered to the patient every 12 hours without regard to food.

29. A solid oral dosage form, comprising: an immediate release portion comprising about 20% to about 30% (w/w) of the total amount of the oxycodone or a pharmaceutically acceptable salt thereof in the dosage form, and about 40% to about 60% (w/w) of the total amount of the acetaminophen in the dosage form; and an extended release portion comprising about 70% to about 80% (w/w) of the total amount of the oxycodone or a pharmaceutically acceptable salt thereof in the dosage form, and about 40% to about 60% (w/w) of the total amount of the acetaminophen in the dosage form; wherein the total amount of oxycodone or salt in the dosage form is about 7.5 mg and the total amount of acetaminophen in the dosage form is about 325 mg; wherein the dosage form has gastric retentive properties; and wherein the bioavailability of either the acetaminophen or the oxycodone or the pharmaceutically acceptable salt thereof is not affected by the absence of food in a subject's gastrointestinal tract.

30. A method of treating acute pain in a patient in need thereof, comprising administering two solid dosage forms of claim 29 to the patient.
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