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Claims for Patent: 6,254,887

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Claims for Patent: 6,254,887

Title: Controlled release tramadol
Abstract:A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.
Inventor(s): Miller; Ronald Brown (Basel, CH), Leslie; Stewart Thomas (Cambridge, GB), Malkowska; Sandra Therese Antoinette (Cambridgeshire, GB), Smith; Kevin John (Cambridge, GB), Wimmer; Walter (Limburg, DE), Winkler; Horst (Linter, DE), Hahn; Udo (Nentershausen, DE), Prater; Derek Allan (Cambridge, GB)
Assignee: Euro-Celtique S.A. (Luxembourg, LU)
Application Number:08/677,798
Patent Claims: 1. A controlled release oral pharmaceutical preparation suitable for dosing every 24 hours comprising

a substrate comprising a pharmaceutically effective amount of tramadol or a salt thereof;

said substrate coated with a controlled release coating;

said preparation having a dissolution rate in vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0,1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 nm, between 0 and 50% tramadol released after 1 hour; between 0 and 75% tramadol released after 2 hours; between 3 and 95% tramadol released after 4 hours; between 10 and 100% tramadol released after 8 hours; between 20 and 100% tramadol released after 12 hours; between 30 and 100% tramadol released after 16 hours; between 50 and 100% tramadol released after 24 hours; and greater than 80% tramadol released after 36 hours, by weight, said preparation providing a therapeutic effect for about 24 hours after oral administration.

2. A controlled release preparation as claimed in claim 1, having an in vitro dissolution rate (measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. And using UV detection at 270 mm) as set forth below:

3. A controlled release preparation as claimed as claim 1, having an in vitro dissolution rate (measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 mm) as set forth below:

4. A controlled release preparation as claimed in claim 1, having an in vitro dissolution rate (measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 mm) as set forth below:

5. A controlled release preparation according to claim 1, wherein said substrate comprises a plurality of spheroids.

6. A controlled release preparation according to claim 5, wherein said spheroids comprise a spheronizing agent.

7. A controlled release preparation suitable for dosing every twelve hours comprising

a substrate comprising an effective amount of tramadol or pharmaceutically acceptable salt thereof and said substrate coated wit a controlled release coating;

said preparation exhibiting an in vitro dissolution rate when measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 mm, such that between 5 and 50% (by weight) tramadol is released after 1 hour, between 10 and 75% by weight) tramadol is released after 2 hours, between 20 and 95% (by weight) tramadol is released after 4 hours, between 40 and 100% (by weight) tramadol is released after 8 hours, more than 50% (by weight) tramadol is released after 12 hours, more than 70% (by weight) tramadol is released after 18 hours and more than 80% (by weight) tramadol is released after 24 hours said preparation providing a therapeutic effect for at least about 12 hours after oral administration.

8. A controlled release preparation according to claim 7, wherein said substrate comprises a plurality of spheroids.

9. A controlled release preparation according to claim 7 which provides a t.sub.max at 2 to 7 hours after oral administration.

10. A controlled release preparation according to claim 7, which provides a t.sub.max at 1.5 to 8 hours after oral administration.

11. A controlled release preparation according to claim 7, which provides a W.sub.50 from about 7 to about 16 hours after oral administration.

12. A controlled release preparation according to claim 7, wherein said substrate is a tablet.

13. A controlled release oral pharmaceutical tablet suitable for dosing every 24 hours comprising

a tablet containing a pharmaceutically effective amount of tramadol or a salt thereof;

said tablet coated with a controlled release coating;

said coated tablet having a dissolution rate in vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 nm, between 0 and 50% tramadol released after 1 hour; between 0 and 75% tramadol released after 2 hours; between 3 and 95% tramadol released after 4 hours; between 10 and 100% tramadol released after 8 hours; between 20 and 100% tramadol released after 12 hours; between 30 and 100% tramadol released after 16 hours; between 50 and 100% tramadol released after 24 hours; and greater than 80% tramadol released after 36 hours, by weight, and providing a W.sub.50 in the range of 10 to 33 hours when orally administered, said coated tablet providing a therapeutic effect for about 24 hours after oral administration.

14. A controlled release oral pharmaceutical tablet suitable for dosing every 24 hours comprising

a tablet containing a pharmaceutically effective amount of tramadol or a salt thereof;

said tablet coated with a controlled release coating;

said coated tablet providing a therapeutic effect for about 24 hours after oral administration and having an in vitro dissolution rate (measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 mm) as set forth below:

15. A controlled release oral pharmaceutical tablet in accordance with claim 15 which has

an in vitro dissolution rate (measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. using UV detection at 27 mm) as set forth below:

16. A controlled release preparation according to claim 1, which when orally administered provides a W.sub.50 value in the range of 10 to 33 hours.

17. A controlled release preparation according to claim 1, having an in vitro dissolution rate (measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 mm) as set forth below:

18. A controlled release preparation according to claim 1, which when orally administered provides a t.sub.max at 4-5 hours after oral administration.

19. A controlled release oral pharmaceutical preparation suitable for dosing every 24 hours comprising

a substrate comprising a pharmaceutically effective amount of an opioid analgesic consisting essentially of tramadol or a salt thereof;

said substrate coated with a controlled release coating;

said preparation having a dissolution rate in vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0.1 N hydrochloric acid at 37.degree. C. and using UV detection at 270 nm, between 0 and 50% tramadol released after 1 hour; between 0 and 75% tramadol released after 2 hours; between 3 and 95% tramadol released after 4 hours; between 10 and 100% tramadol released after 8 hours; between 20 and 100% tramadol released after 12 hours; between 30 and 100% tramadol released after 16 hours; between 50 and 100% tramadol released after 24 hours; and greater than 80% tramadol released after 36 hours, by weight, said preparation providing a therapeutic effect for about 24 hour, after oral administration.

20. A controlled release preparation according to claim 1, wherein said substrate comprises inert non-pareil beads coated with said tramadol.

21. A controlled release preparation according to claim 7, wherein said substrate comprises inert nonpareil beads coated with said tramadol.

22. A controlled release preparation according to claim 19, wherein said substrate comprises inert non-pareil beads coated with said tramadol.

23. A controlled release preparation according to claim 19, wherein said substrate is a tablet.

24. A controlled release preparation according to claim 19, wherein said substrate comprises spheroids.

25. A controlled release preparation according to claim 19, which provides a t.sub.max from 3 to 6 hours after orally administered to a human patient,

26. A controlled release preparation according to claim 25, which provides a W.sub.50 value in the range from 10 to 33 hours.

27. A controlled release preparation in accordance with claim 1, wherein said controlled release coating comprises a material selected from the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.

28. A controlled release preparation in accordance with claim 7, wherein said controlled release coating comprises a material selected from the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.

29. A controlled release preparation in accordance with claim 13, wherein said controlled release coating comprises a material selected from the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.

30. A controlled release preparation in accordance with claim 14, wherein said controlled release coating comprises a material selected tom the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.

31. A controlled release preparation in accordance with claim 19, wherein said controlled release coating comprises a material selected from the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.

32. A controlled release preparation in accordance with claim 26, wherein said controlled release coating comprises a material selected from the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.

33. A controlled release preparation in accordance with claim 11, wherein said controlled release coating comprises a material selected from the group consisting of a water insoluble wax, a water insoluble polymer, a water insoluble cellulose and mixtures of any of the foregoing.
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