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Claims for Patent: 7,988,998

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Claims for Patent: 7,988,998

Title:Sustained-release tramadol formulations with 24-hour efficacy
Abstract: A sustained-release tramadol formulation oral administration is provided which, upon initial administration of one dose, provides an analgesic effect within 2 hours, which analgesic effect continues for at least 24 hours after administration.
Inventor(s): Lenaerts; Vincent (Beaconsfield, CA), Ouadji-Nijki; Patricia Laure (Montreal, CA), Bacon; Jonathan (Montreal, CA), Ouzerourou; Rachid (Montreal, CA), Gervais; Sonia (Laval, CA), Rahmouni; Miloud (Dollars-des Ormeaux, CA), Smith; Damon (St-Laurent, CA)
Assignee: Labopharm Inc. (Quebec, CA) Labopharm Europe Limited (Dublin, IE) Labopharm (Barbados) Limited (Hastings, Christ Church, BB)
Application Number:11/112,008
Patent Claims: 1. A once daily oral pharmaceutical composition for controlled release of tramadol, comprising: a core comprising tramadol dispersed in a first controlled-release matrix comprising cross-linked high amylose starch, wherein the tramadol is present in the core in an amount from about 10 to about 70 weight-percent of the composition of the core, and a compression coat formed over the core and comprising tramadol dispersed in a mixture of polyvinyl acetate and polyvinylpyrrolidone at a weight ratio of about 8:2 such that the mixture comprises from about 30% to about 65% by weight of the coat, wherein the release of tramadol from the core is slower than the release of tramadol from the coat, wherein the composition, upon initial administration of one dose, provides an onset of analgesic effect within 2 hours, which analgesic effect continues for at least 24 hours after administration, and wherein the composition is a tablet.

2. The composition of claim 1, wherein the composition comprises 200 mg of tramadol and upon initial administration of one dose, provides a mean plasma concentration of at least 100 ng/mL within 2 hours of administration and continues to provide a mean plasma concentration of at least 100 ng/mL for at least 22 hours after administration.

3. The composition of claim 2 which continues to provide a mean plasma concentration of at least 100 ng/mL for at least 23 hours after administration.

4. The composition of claim 2 which continues to provide a mean plasma concentration of at least 100 ng/mL for at least 24 hours after administration.

5. The composition of claim 1, comprising 100 mg of tramadol, wherein the composition, upon initial administration of one dose, provides a mean plasma concentration of at least 50 ng/mL within 2 hours of administration and continues to provide a mean plasma concentration of at least 50 ng/mL for at least 22 hours after administration.

6. The composition of claim 5, which continues to provide a mean plasma concentration of at least 50 ng/mL for at least 23 hours after administration.

7. The composition of claim 1 comprising 300 mg of tramadol, wherein the composition, upon initial administration of one dose, provides a mean plasma concentration of at least 150 ng/mL within 2 hours of administration and continues to provide a mean plasma concentration of at least 150 ng/mL for at least 22 hours after administration.

8. The composition of claim 7, which continues to provide a mean plasma concentration of at least 150 ng/mL for at least 23 hours after administration.

9. The composition of claim 7, which continues to provide a mean plasma concentration of at least 150 ng/mL for at least 24 hours after administration.

10. The composition of claim 1, comprising 200 mg of tramadol, wherein upon initial administration of 400 mg, the composition provides a mean plasma concentration of at least 200 ng/mL for at least 22 hours after administration.

11. The composition of claim 10, which upon said administration provides a mean plasma concentration of at least 190 ng/mL for at least 23 hours after administration.

12. The composition of claim 10, which upon said administration provides a mean plasma concentration of at least 180 ng/mL for at least 24 hours after administration.

13. The composition of claim 5, wherein the mean maximum plasma concentration (C.sub.max) is less than 100 ng/mL.

14. The composition of claim 7, wherein the mean maximum plasma concentration (C.sub.max) is less than 300 ng/mL.

15. The composition of claim 7, wherein the mean maximum plasma concentration (C.sub.max) is less than two times the mean plasma concentration obtained 24 hours after administration (C.sub.24h).

16. The composition of claim 10, wherein the mean maximum plasma concentration (C.sub.max) is less than 2.3 times the mean plasma concentration obtained 24 hours after administration (C.sub.24).

17. The composition of claim 1 comprising 100 mg of tramadol or a salt thereof, wherein the composition, upon initial administration of one dose, provides an O-desmethyltramadol mean plasma concentration of at least 11 ng/mL within 2 hours of administration and continues to provide an O-desmethyltramadol mean plasma concentration of at least 12 ng/mL for at least 24 hours after administration.

18. The composition of claim 17 comprising 200 mg of tramadol or a salt thereof, wherein the composition, upon initial administration of one dose, provides an O-desmethyltramadol mean plasma concentration of at least 24 ng/mL within 2 hours of administration and continues to provide an O-desmethyltramadol mean plasma concentration of at least 25 ng/mL for at least 24 hours after administration.

19. The composition of claim 17 comprising 300 mg of tramadol or a salt thereof, wherein the composition, upon initial administration of one dose, provides an O-desmethyltramadol mean plasma concentration of at least 32 ng/ml within 2 hours of administration and continues to provide an O-desmethyltramadol mean plasma concentration of at least 32 ng/mL for at least 24 hours after administration.

20. The composition of claim 18, wherein upon initial administration of 400 mg, the composition provides an O-desmethyltramadol mean plasma concentration of at least 50 ng/mL within 2 hours of administration and continues to provide an O-desmethyltramadol mean plasma concentration of at least 50 ng/mL for at least 24 hours after administration.

21. The composition of claim 1, wherein between 10% and 40% of the agent is released from the formulation between 0 and about 2 hours of measurement, between about 30% and 60% of the agent is released from the formulation between 2 and about 7 hours of the measurement, between about 50% and 80% of the agent is released from the formulation between 7 and about 12 hours of measurement, and between about 80% and 100% of the agent is released from the formulation after about 20 hours of measurement.

22. The composition of claim 1 having a dissolution rate in vitro when measured with HPLC-USP apparatus Type 1 at 100 rpm in 50 mM sodium phosphate buffer at pH 6.8, from about 5% to about 30% after 1 hour; from about 15% to about 40% after 2 hours; from about 20% to about 50% after 4 hours, from about 30% to about 70% after 8 hours; from about 40% to about 90% after 12 hours; from about 50% to about 100% after 16 hours; from 60% to about 100% after 24 hours.

23. The composition of claim 1 having a dissolution rate in vitro when measured with HPLC-USP apparatus Type 1 at 100 rpm in 50 mM sodium phosphate buffer at pH 6.8, from about 10% to about 25% after 1 hour; from about 15% to about 30% after 2 hours; from about 25% to about 40% after 4 hours, from about 40% to about 55% after 8 hours; from about 60% to about 75% after 12 hours; from about 70% to about 90% after 16 hours; from about 90% to about 100% after 24 hours.

24. The composition of claim 22, wherein the composition comprises 200 mg of tramadol.

25. The composition of claim 23, wherein the composition comprises 200 mg of tramadol.

26. The composition of claim 1, wherein the tramadol is present in the core in an amount from about 20 to about 60 weight-percent of the composition of the core.

27. The composition of claim 1, wherein the tramadol is present in the coat in an amount from about 15 to about 40 weight-percent of the composition of the coat.

28. The composition of claim 1, wherein the polyvinylacetate disposed in the coat has a molecular weight from about 100,000 to about 1,000,000.

29. The composition of claim 1, wherein the polyvinylpyrollidone in the coat has a molecular weight from about 10,000 to about 100,000.
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