Dosage forms having an inner core and outer shell with different shapes

• US 20040146559A1
• Filed: 12/04/2003
• Published: 07/29/2004
• Est. Priority Date: 09/28/2002
• Status: Abandoned Application

• Current Assignee: McNeil-PPC Incorporated (Johnson & Johnson)
• Original Assignee: McNeil-PPC Incorporated (Johnson & Johnson)
• Inventors: Sowden, Harry S., Bunick, Frank J., Lee, Der-Yang, Thomas, Martin, McNally, Gerard P.
• Application Number:
  US10/432,812
• Publication Number:
  US 20040146559A1
• Time in Patent Office: Days
• US Class Current: 424/471
• CPC Class Codes: A61K 9/2072 characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms A61K9/0004, A61K9/0056, A61K9/0065 take precedence
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/2086 Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• CPC Class Codes: A61K 9/2893 Tablet coating processes mechanical aspects A61J3/06

Abstract

A dosage form comprises an active ingredient, a core having an outer surface and a first shape and a shell having outer and inner surfaces and a second shape, in which the shell surrounds at least a portion of the core, and the first and second shapes are substantially different. In one embodiment the shell comprises at least about 80% of a flowable material selected from the group consisting of film formers, gelling polymers, thermoplastic materials, low melting hydrophobic materials, non-crystallizable sugars, non-crystallizable sugar-alcohols, and mixtures thereof. In another embodiment the shell is substantially free of pores having a diameter of 0.5 to 5.0 microns. In another embodiment, the core and shell each having a different number of planes of symmetry with respect to the same reference axis. In another embodiment, the distance from the core outer surface to the shell outer surface is different at two different points located on the core outer surface and the difference is greater than about 125 microns. Either the core, the shell, or a combination thereof may contain at least one active ingredient. The core and shell may each be molded or compressed. The core may also comprise an insert which may contain at least one active ingredient. The shape of the core may be chosen so as to permit modified release of active material in the core upon breach of the shell or provides a modified release profile for the active material in the core.

Claims

1. A dosage form comprising:

an active ingredient;

a core having an outer surface and a first shape; and

a shell having outer and inner surfaces and a second shape which is substantially different than the first shape, wherein the shell comprises at least about 80% of a flowable material selected from the group consisting of film formers, gelling polymers, thermoplastic materials, low melting hydrophobic materials, non-crystallizable sugars, non-crystallizable sugar alcohols, and mixtures thereof, and the shell surrounds at least a portion of the core.

8. The dosage form of any of claims 1-6, wherein the shell is substantially free of pores having a pore diameter of 0.5-5.0 microns.

9. The dosage form of any of claims 1-7, wherein the core and shell each have a different number of planes of symmetry with respect to the same reference axis.

10. The dosage form of any of claims 1-7, wherein the distance from the core outer surface to the shell outer surface is different at two different points located on the core outer surface, and the difference in distance is greater than about 125 microns.

11. The dosage form of claims 10, wherein the difference in distance is in the range of about 125-30,000 microns.

12. The dosage form of any of claims 1-7, wherein the shell comprises less than 10% by weight of a direct-compression filler-binder.

13. The dosage form of any of claims 1-7, in which the outer surface of the core displays written information, and the shell outer surface is transparent, semi-transparent or translucent.

14. The dosage form of any of claims 1-7, in which the outer surface of the shell displays written information.

15. The dosage form of any of claims 1-7, in which the shell is transparent, semi-transparent or translucent.

16. The dosage form of any of claims 1-7, in which the core and shell have different colors.

17. The dosage form of any of claims 1-7, in which the core is visually observable.

18. The dosage form of any of claims 1-7, in which the core, the shell, or both the core and shell comprise an active ingredient.

19. The dosage form of any claims 1-7, in which only the core comprises an active ingredient.

20. The dosage form of claim 18 or claim 19, in which the active ingredient is capable of dissolution, and dissolution of the active ingredient meets USP specifications for immediate release tablets containing the active ingredient.

21. The dosage form of any of claims 1-7, in which the core comprises a compressed dosage form.

22. The dosage form of any of claims 1-7, in which the core comprises a microelectronic device.

23. The dosage form of any of claims 1-7, in which the core comprises an insert.

24. The dosage form of claim 23, in which the insert is larger than the core in at least one dimension.

25. The dosage form of claim 23, in which at least a portion of the insert protrudes from the core.

26. The dosage form of claim 23, in which the insert comprises an active ingredient.

27. The dosage form of claim 26, in which the active ingredient is capable of dissolution, and dissolution of the active ingredient contained in the insert meets USP specifications for immediate release tablets containing the active ingredient.

28. The dosage form of claim 23, in which the insert comprises a microelectronic device.

29. The dosage form of any of claims 1-7, in which the outer surface of the shell is textured.

30. The dosage form of any of claims 1-7, in which the outer surface of the shell contains a prearranged pattern.

31. The dosage form of any of claims 1-7, in which the shell comprises one or more openings therein.

32. The dosage form of any of claims 1-7, in which the outer surface of the shell is substantially smooth.

33. The dosage form of any of claims 1-7, in which the shape of the core permits controlled release of core upon breach of the shell.

34. The dosage form of any of claims 1-7, in which the outer surface of the shell has a shape selected from the group consisting of spheres, ovoids, ellipses, and flattened derivatives thereof.

35. The dosage form of any of claims 1-7, in which the dosage form comprises a single core.

36. The dosage form of any of claims 1-7, in which the core and shell each have a major plane of symmetry, and the major plane of symmetry of the core is orthogonal to the major plane of symmetry of the shell.

37. The dosage form of any of claims 1-7, in which the core has an aperture therein defining an interior surface.

38. The dosage form of any of claims 1-7, in which the core is in the shape of a torus.

39. The dosage form of any of claims 1-7, in which the shell comprises first and second shell portions having first and second topographies respectively, and the first and second topographies are different.

40. The dosage form of claim 39, in which each of the first and second shell portions have an outer surface, and at least one of the outer surfaces comprises Braille symbols.

41. The dosage form of any of claims 1-7, in which the outer surface of the core contains indentations, intagliations, letters, symbols or a pattern.

42. The dosage form of claim 41, in which the shell covers a portion of the core, but does not substantially cover the indentations, intagliations, letters, symbols or pattern.

43. The dosage form of claim 41, in which a first shell portion coating covers the indentations, intagliations, letters, symbols or pattern but does not substantially cover the remaining portion of the core.

44. The dosage form of claim 43, in which a second shell portion covers the portion of the core which is not covered by the first shell portion.

45. The dosage form of any of claims 1-7, in which the outer surface of the core contains raised protrusions in the form of letters, symbols or a pattern.

46. The dosage form of claim 43, in which the shell covers a portion of the core, but does not substantially cover the raised protrusions.

47. The dosage form of claim 45, in which a first shell portion covers the raised protrusions, but does not substantially cover the remaining portion of the core.

48. The dosage form of claim 47, in which a second shell portion covers the portion of the core which is not covered by the first shell portion.

49. The dosage form of any of claims 1-7, in which the core outer surface is debossed or embossed with visual information and the shell outer surface is transparent, semi-transparent or translucent.

50. The dosage form of any of claims 1-7, wherein the shell contains, based upon the total dry solids weight of the shell composition, from about 25 percent to about 80 percent of a film former;

from about 0.10 percent to about 33 percent of a thickening agent; and

from about 11 percent to about 60 percent of a plasticizer.

51. The dosage form of any of claims 1-7, in which the dosage form further comprises a second core.

52. The dosage form of any of claims 1-7, wherein the shell has a topography which includes indentations or protrusions greater than about 20 microns in width, depth, or height.

53. The dosage form of any of claims 1-7, in which the outer surface of the shell contains a prearranged pattern.

54. The dosage form of claim 53 in which the prearranged pattern comprises Braille symbols.

55. The dosage form of any of claims 1-7, in which at least a portion of the shell comprises one or more openings therein.

56. The dosage form of claim 55 in which the shell comprises a plurality of openings therein.

57. The dosage form of claim 56 in which the openings form a prearranged pattern.

58. The dosage form of any of claims 1-7, in which the shell comprises first and second portions having first and second topographies, respectively, and the first and second topographies are different.

59. The dosage form of any of claims 1-7, in which at least a portion of the shell is transparent, semi-transparent, or translucent.

60. The dosage form of any of claims 1-7, wherein the shell contains, based upon the total dry solids weight of the shell composition, from about 25 percent to about 80 percent of a film former;

from about 0.10 percent to about 33 percent of a thickening agent; and

from about 11 percent to about 60 percent of a plasticizer.

2. A dosage form comprising:

an active ingredient;

a core having an outer surface with a first topography; and

a shell having an inner surface and an outer surface with a second topography which is different than the first topography, wherein at least one of the first or second topographies includes indentations or protrusions greater than about 20 microns in width, depth or height, and the shell surrounds at least a portion of the core.

3. A dosage form comprising:

an active ingredient;

a core having an outer surface having indentations or protrusions greater than about 20 microns in width, depth, or height; and

a shell having an inner surface and an outer surface, wherein the shell resides substantially conformally upon at least a portion of the core outer surface, such that the inner surface of the shell has protrusions and indentations corresponding substantially inversely to the major protrusions and indentations of the outer surface of the core, and the outer surface of the shell does not substantially conform to the major protrusions and indentations of the outer surface of the core.

4. A dosage form comprising:

an active ingredient;

a core having an outer surface having indentations or protrusions; and

a shell which surrounds at least a portion of the core, wherein the shell has an inner surface, an outer surface and a thickness, the ratio of the width of one or more indentations or protrusions in the core surface to the thickness of the shell at one or more locations is at least about 1;

1, the shell resides substantially conformally upon the core outer surface such that the inner surface of the shell has protrusions and indentations correspond substantially inversely to the major indentations and protrusions of the outer surface of the core, and the outer surface of the shell does not substantially conform to the major protrusions and indentations of the outer surface of the core.

5. A dosage form comprising:

an active ingredient;

a first core having an outer surface with a first topography;

a second core having an outer surface with a second topography; and

a shell having an inner surface and outer surface with a third topography which is different than the first topography, wherein at least one of the first, second, or third topographies includes indentations or protrusions greater than about 20 microns in width, depth or height, and the shell surrounds at least a portion of the core.

6. A dosage form comprising:

an active ingredient;

a core comprising a first and second core portion having outer surfaces with a first and second topographies, respectively;

a first shell portion having an outer surface with a third topography; and

a second shell portion having an outer surface with a fourth topography, wherein at least one of the third or fourth shell surface topographies is different from the underlying core portion topography, at lease one of the first, second, third, or fourth topographies includes indentations or protrusions greater than about 20 microns in width, depth or height, and the shell surrounds at least a portion of the core.

7. A dosage form comprising:

an active ingredient;

a core having an outer surface and a first shape; and

a shell having outer and inner surfaces and a second shape which is substantially different than the first shape, wherein the shell is substantially free of pores having a pore diameter of 0.5 to 5.0 microns, and the shell surrounds at least a portion of the core.