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Claims for Patent: 5,591,452

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Claims for Patent: 5,591,452

Title: Controlled release formulation
Abstract:A controlled release preparation for oral administration contains tramadol, or a pharmaceutically acceptable salt thereof, as active ingredient.
Inventor(s): Miller; Ronald B. (Basel, CH), Leslie; Stewart T. (Cambridge, GB2), Malkowska; Sandra T. A. (Cambridgeshire, GB2), Smith; Kevin J. (Cambridge, GB2), Wimmer; Walter (Limburg, DE), Winkler; Horst (Linter, DE), Hahn; Udo (Nentershausen, DE), Prater; Derek A. (Cambridge, GB2)
Assignee: Euro-Celtique, S.A. (Luxembourg, LU)
Application Number:08/241,129
Patent Claims: 1. A controlled release oral pharmaceutical preparation suitable for dosing every 24 hours containing from about 50 mg to about 800 mg of tramadol or a pharmaceutically acceptable salt thereof, calculated as hydrochloride salt, in a controlled release matrix, the matrix comprising from about 1 to about 80% w/w of one or more hydrophilic or hydrophobic polymers, and having a dissolution rate in vitro when measured using the Ph. Eur. Paddle Method at 100 rpm in 900 ml 0.1N hydrochloric acid at 37.degree. C. and using UV detection at 270 nm, from about 0 to about 50% tramadol released after 1 hour; from about 0 to about 75% tramadol released after 2 hours; from about 3 to about 95% tramadol released after 4 hours; from about 10 to about 100% after 8 hours; from about 20 to about 100% tramadol released after 12 hours; from about 30 to about 100% tramadol released after 16 hours; from about 50 to about 100% tramadol released after 24 hours; and greater than 80% tramadol released after 36 hours, by weight.

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

3. 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 0.1N 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 0.1N hydrochloric acid at 37.degree. C. and using UV detection at 270 mm) as set forth below:

5. A dosage form according to claim 1, wherein said matrix comprises a cellulose ether.

6. A dosage form according to claim 5, wherein said matrix comprises a controlled release matrix comprising at least one alkylcellulose, at least one C.sub.12 to C.sub.36, aliphatic alcohol and, optionally at least one polyalkylglycol.

7. A dosage form as claimed in claim 6, wherein said polyalkylglycol is polyethylene glycol.

8. A dosage form according to claim 6, wherein said at least one C.sub.12 to C.sub.36 aliphatic alcohol is a C.sub.14 to C.sub.22 aliphatic alcohol.

9. A dosage form according to claim 6, wherein said alkylcellulose is a C.sub.1 -C.sub.6 alkylcellulose.

10. A dosage form according to claim 6, wherein the dosage form contains from about 1 to about 20% w/w of said alkylcellulose.

11. A dosage form according to claim 6, wherein said aliphatic alcohol is selected from the group consisting of lauryl alcohol, myristyl alcohol, stearyl alcohol, cetyl alcohol, cetostearyl alcohol, and mixtures thereof.

12. The dosage form of claim 11, wherein said aliphatic alcohol is cetyl alcohol or cetostearyl alcohol.

13. A dosage form according to claim 6, wherein said dosage form contains from about 5 to about 30% w/w of said aliphatic alcohol.

14. A dosage form according to claim 6, wherein said dosage form contains from about 10 to about 25% w/w of said aliphatic alcohol.

15. A dosage form according to claim 1, in the form of film coated spheroids, wherein said spheroid matrix comprises a spheronizing agent.

16. A dosage form according to claim 1, in the form of multi-particulates wherein said matrix comprises a hydrophobic fusible carrier or diluent having a melting point from 35.degree. to 140.degree. C. and optionally a release control component comprising a water soluble fusible material, or a particulate soluble or insoluble organic or inorganic material.

17. A dosage form according to claims 1, which comprises a tablet formed by compressing a multiparticulate according to claim 16.

18. A dosage form according to claim 5, wherein said cellulose ether is an alkylcellulose.

19. A dosage form according to claim 18, wherein said alkylcellulose is ethylcellulose.

20. A dosage form according to claim 1 which provides a t.sub.max from about 3 to about 6 hours.

21. A dosage form according to claim 1 which provides a W.sub.50 from about 10 to about 33 hours.

22. A controlled release preparation suitable for dosing every twelve hours containing from about 50 to about 400 mg tramadol or pharaceutically acceptable salt thereof, calculated as the hydrochloride salt, in a controlled release matrix containing from about 1 to about 80% w/w of one or more hydrophilic or hydrophobic polymers, said preparation exhibiting an in vitro dissolution rate when measured by the Ph. Eur. Paddle method at 100 rpm in 900 ml 0.1N 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.

23. A dosage form according to claim 22 wherein said controlled release matrix comprises a cellulose ether.

24. A dosage form according to claim 23 wherein said cellulose ether is an alkyl cellulose.

25. A dosage form according to claim 22 wherein said controlled release matrix comprises at least one C.sub.1 to C.sub.6, alkyl cellulose.

26. A dosage form according to claim 25, wherein said controlled release matrix comprises at least one C.sub.12 to C.sub.36, aliphatic alcohol.

27. A dosage form according to claim 26, wherein said controlled release matrix further comprises at least one C.sub.14 to C.sub.22 aliphatic alcohol.

28. A dosage form according to claim 27, wherein said controlled release matrix further comprises at least one polyalkylglycol.

29. A dosage form according to claim 28, wherein said polyalkylglycol is polyethylene glycol.

30. A dosage form according to claim 25, wherein said dosage form contains from about 1 to about 20% w/w of said alkyl cellulose.

31. A dosage form according to claim 29, wherein said dosage form contains from about 2 to 15% w/w of said alkyl cellulose.

32. A dosage form according to claim 26, wherein said aliphatic alcohol is selected from the group consisting of lauryl alcohol, myristyl alcohol, stearyl alcohol, cetyl alcohol cetostearyl alcohol, and mixtures thereof.

33. A dosage form according to claim 32, wherein said dosage form contains from about 5 to about 30% w/w aliphatic alcohol.

34. A dosage form according to claim 32, wherein said dosage form contains from about from 10 to 25% w/w aliphatic alcohol.

35. A dosage form according to claim 25 in the form of multiparticulate spheroid matrices, wherein said spheroid matrix comprises a spheronizing agent.

36. A dosage form according to claim 35, wherein said spheronizing agent comprises microcrystalline cellulose.

37. A dosage form according to claim 22, in the form of multiparticulates wherein said matrix comprises a hydrophobic fusible carrier or diluent having a melting point from 35.degree. to 140.degree. C. and optionally a release control component comprising a water soluble fusible material, or a particulate soluble or insoluble organic or inorganic material.

38. A dosage form according to claim 22, which provides a t.sub.max from about 1.5 to about 8 hours.

39. A dosage form according to claim 22, which provides a W.sub.50 from about 7 to about 16 hours.
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