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Claims for Patent: 6,228,398

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Claims for Patent: 6,228,398

Title: Multiparticulate modified release composition
Abstract:The invention relates to a multiparticulate modified release composition that in operation delivers an active ingredient in a pulsed or bimodal manner. The multiparticulate modified release composition comprises an immediate release component and a modified release component; the immediate release component comprising a first population of active ingredient containing particles and the modified release component compnsimg a second population of active ingredient containing particles coated with a controlled release coating; wherein the combination of the immediate release and modified release components in operation deliver the active ingredient in a pulsed or a bimodal manner. The invention also relates to a solid oral dosage form containing such a multiparticulate modified release composition. The plasma profile achieved by the multiparticulate modified release composition is advantageous in reducing patient tolerance to the active ingredient and in increasing patient compliance by reducing dosage frequency.
Inventor(s): Devane; John G. (Athlone, IE), Stark; Paul (Athlone, IE), Fanning; Niall M. M. (Athlone, IE)
Assignee: Elan Corporation, PLC (Dublin, IE)
Application Number:09/566,636
Patent Claims: 1. A multiparticulate modified release composition containing at least one active ingredient and having a first component comprising a first population of active ingredient-containing particles and at least one subsequent component, each subsequent component comprising a subsequent population of active ingredient-containing particles, the active ingredient contained in the first and subsequent components being the same or different; wherein the at least one subsequent population of active ingredient containing particles further comprises a modified release coating or, alternatively or additionally, a modified release matrix material, such that the composition following oral delivery to a subject delivers the active ingredient or active ingredients in a pulsatile manner.

2. The multiparticulate modified release composition according to claim 1, wherein the composition comprises a first component and one subsequent component.

3. The multiparticulate modified release composition according to claim 2, wherein the first component comprises an immediate release component and the subsequent component is a modified release component.

4. The multipaiticulate modified release composition according to claim 3, wherein the modified release component comprises particles having a modified release coating.

5. The multiparticulate modified release composition according to claim 3, wherein the modified release component comprises a modified release matrix material.

6. The multiparticulate modified release composition according to claim 1, wherein the first population of active ingredient-containg particles and the at least one subsequent population of active ingredient-containing particles comprise the same active ingredient.

7. The multiparticulate modified release composition according to claim 1, wherein the first population of active ingredient-containing particles contains two or more active ingredients.

8. The multiparticulate modified release composition according to claim 1, wherein the at least one subsequent population of active ingredient-containing particles contains two or more active ingredients.

9. The multiparticulate modified release composition according to claim 1, wherein the active ingredient comprises substantially one optically pure enantiomer or a mixture, racemic or otherwise, of enantiomers.

10. The multiparticulate modified release composition according to claim 1, wherein at least one of the first and subsequent components further comprise an enhancer.

11. The multiparticulate modified release composition according to claim 1, wherein the amount of active ingredient contained in the first and subsequent components is the same or different.

12. The multiparticulate modified release composition according to claim 11, wherein the amount of active ingredient contained in each component is from about 0.1 mg to about 1 g.

13. The multiparticulate modified release composition according to claim 6, wherein the active ingredient is methylphenidate or a pharmaceutically acceptable salt thereof, an enantiomer or mixtures thereof or mixtures thereof.

14. The multipatticulate modified release composition according to claim 1, wherein the first and subsequent populations of active ingredient-containing particles have different in vitro dissolution profiles.

15. The multiparticulate modified release composition according to claim 1, wherein the first component is an immediate release component and the at least one subsequent component is a modified release component.

16. The multiparticulate modified release composition according to claim 15, which in operation releases substantially all of the active ingredient from the first population of active ingredient-containing particles prior to release of the active ingredient from the subsequent population of active ingredient-containing particles.

17. The multiparticulate modified release composition according to claim 1, wherein the in vivo release of the active ingredient in the subject mimics the in vivo release of the same active ingredient administered in the form of two or more doses of immediate release forms of the active ingredient.

18. The multiparticulate modified release composition according to claim 13, wherein the in vivo release of the active ingredient in the subject mimics the in vivo release of the same active ingredient administered in the form of two or more doses of immediate release forms of the active ingredient.

19. The multiparticulate modified release composition according to claim 16, wherein the mean in vitro dissolution profile in an aqueous medium is such that about 50 to 100% of the active ingredient contained in the first population of active ingredient containing particles is released within four hours, and about 25 to 55% of the active ingredient contained in the subsequent population of active ingredient containing particles is released between four and eight hours.

20. The multiparticulate modified release composition according to claim 19, wherein the mean in vitro dissolution profile in an aqueous medium is such that about 80 to 100% of the active ingredient contained in the first population of active ingredient containing particles is released within four hours, and about 28 to 55% of the active ingredient contained in the subsequent population of active ingredient containing particles is released between four and eight hours.

21. A solid oral dosage form comprising a multiparticulate modified release composition according to claim 1.

22. The solid oral dosage form according to claim 21 comprising a blend of first and subsequent active ingredient-containing particles filled into hard gelatin or soft gelatin capsules.

23. The solid oral dosage form according to claim 21, wherein the first and subsequent components are separately and independently compressed into mini-tablets and filled into hard or soft gelatin capsules.

24. The solid oral dosage form according to claim 21, wherein the first component is compressed into the first layer of a multilayer tablet and the at least one subsequent component is compressed into a subsequent layer of the multilayer tablet.

25. The solid oral dosage form according to claim 21, wherein the first and subsequent components are incorporated in a rapidly dissolving dosage form.

26. The solid oral dosage form according to claim 25, wherein the rapidly dissolving dosage form is a fast-melt tablet dosage form.

27. A method, wherein a multiparticulate modified release composition comprising:

a. a first population of active ingredient containing particles and

b. at least one subsequent population of active ingredient containing particles, wherein the subsequent population of active ingredient containing particles further comprises a coating selected from the group consisting of a modified release coating and a modified release matrix material, and wherein oral administration of the composition to a subject in need of the active ingredient releases the active ingredient in a pulsatile manner.

28. The method of claim 27, wherein the in vitro dissolution profile of the multiparticulate modified release composition in an aqueous medium is such that about 50% of the total active ingredient is released within about 30 minutes, about 4% of the total active ingredient is released between about 30 minutes and 4 hours, and about 28% of the active ingredient is released between about four hours and eight hours.

29. The method of claim 27, wherein the active ingredient is an active ingredient for the treatment of attention deficit disorder.

30. A method of treatment of a condition which is characterised by the build up of patient tolerance to an active ingredient administered in the treatment of the condition comprising administering a therapeutically effective amount of a multiparticulate modified release composition according to claim 1.

31. A method of treatment of attention deficit disorder comprising administering a therapeutically effective amount of a multiparticulate modified release composition according to claim 1.

32. A method of treatment of attention deficit disorder comprising administering a therapeutically effective amount of a multiparticulate modified release composition according to claim 13.

33. The composition according to claim 3, wherein the modified release component comprises a pH dependent polymer coating that releases a pulse of active ingredient from the modified release component following a delay time.

34. The composition according to claim 33, wherein the pH dependent polymer coating comprises methacrylate copolymers.

35. The composition according to claim 33, wherein the pH dependent polymer coating comprises a mixture of methacrylate and ammonio methacrylate copolymers in a ratio sufficient to achieve a pulse of active ingredient from the modified release component following a delay time.

36. The composition according to claim 35, where the ratio of methacrylate to ammonio methacryiate copolymers is 1:1.

37. The method of claim 28, wherein the active ingredient is selected from the group consisting of methylphenidate, a pharmaceutically acceptable salt of methylphenidate, an enantiomer of methylphenidate and a mixture of methylphenidate, a pharmaceutically acceptable salt of methylphenidate and an enantiomer of methylphenidate.
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