Modified release dosage forms

• US 8,545,887 B2
• Filed: 09/28/2002
• Issued: 10/01/2013
• Est. Priority Date: 09/28/2001
• Status: Expired due to Fees

• Current Assignee: Johnson & Johnson Consumer Inc. (Johnson & Johnson)
• Original Assignee: McNeil-PPC Incorporated (Johnson & Johnson)
• Inventors: Sowden, Harry S., Wynn, David, Li, Shun-Por, Lee, Der-Yang, Thomas, Martin
• Primary Examiner(s): Hartley, Michael G
• Assistant Examiner(s): Ebrahim, Nabila G
• Application Number:
  US10/476,530
• Publication Number:
  US 20040213849A1
• Time in Patent Office: 4,021 Days
• Field of Search: 424/472
• US Class Current: 424/472
• CPC Class Codes: A23G 1/54 Composite products, e.g. layered laminated, coated, filled
• CPC Class Codes: A23G 3/0029 Moulding processes for hollow products, e.g. opened shell
• CPC Class Codes: A23G 3/04 Sugar-cookers
• CPC Class Codes: A23G 3/368 containing vitamins, antibiotics
• CPC Class Codes: A23G 3/54 Composite products, e.g. layered, coated, filled
• CPC Class Codes: A23L 29/30 containing carbohydrate syrups; containing sugars; containing sugar alcohols, e.g. xylitol; containing starch hydrolysates, e.g. dextrin products from apiculture A23L21/20; artificial sweetening agents A23L27/30
• CPC Class Codes: A61J 3/005 Coating of tablets or the like coating of sweetmeats or confectionery A23G3/20; coating of granules in general B01J2/006
• CPC Class Codes: A61J 3/06 into the form of pills, lozenges or dragees
• CPC Class Codes: A61J 3/10 into the form of compressed tablets tablet presses B30B11/00
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/2013 Organic compounds, e.g. phospholipids, fats
• CPC Class Codes: A61K 9/2018 Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2031 obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, polyethylene oxide, poloxamers
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2068 Compounds of unknown constitution, e.g. material from plants or animals oils, fats, waxes, shellac A61K9/2013
• 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 9/2081 with microcapsules or coated microparticles according to A61K9/50
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer
• CPC Class Codes: A61K 9/2095 : Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61K 9/282 : Organic compounds, e.g. fats
• CPC Class Codes: A61K 9/2826 : Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
• CPC Class Codes: A61K 9/284 : obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/286 : Polysaccharides, e.g. gums; Cyclodextrin
• CPC Class Codes: A61K 9/2873 : Proteins, e.g. gelatin
• CPC Class Codes: A61K 9/2886 : having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61K 9/2893 : Tablet coating processes mechanical aspects A61J3/06
• CPC Class Codes: A61K 9/5084 : Mixtures of one or more drugs in different galenical forms, at least one of which being granules, microcapsules or (coated) microparticles according to A61K9/16 or A61K9/50, e.g. for obtaining a specific release pattern or for combining different drugs tablets containing such a mixture A61K9/2077
• CPC Class Codes: A61P 11/00 : Drugs for disorders of the respiratory system
• CPC Class Codes: A61P 43/00 : Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: B30B 11/08 : co-operating with moulds carried by a turntable
• CPC Class Codes: B30B 11/34 : for coating articles, e.g. tablets
• CPC Class Codes: B30B 15/302 : Feeding material in particulate or plastic state to moulding presses
• CPC Class Codes: Y10T 428/1352 : Polymer or resin containing [i.e., natural or synthetic]

Abstract

A dosage form comprises: (a) at least one active ingredient: (b) a core having a first surface portion upon which resides a first coating and a second surface portion which is substantially free of the first coating; and (c) a shell which resides upon at least a portion of the second surface portion, wherein the shell comprises a different material from the first coating. In another embodiment, the dosage form comprises: (a) at least one active ingredient; (b) a core comprising a center portion having an exterior surface and an annular portion having an exterior surface and an interior surface, wherein the annular portion interior surface is in contact with at least a portion of the center portion exterior surface, and a coating resides on at least a portion of the annular portion exterior surface; and (c) a shell which resides upon at least a portion of the exterior surface of the center portion, wherein the shell comprises a different material than the impermeable coating. In another embodiment, the dosage form comprises: (a) at least one active ingredient; (b) a core having an outer surface and a cavity which extends at least partially through the core such that the core outer surface has at least a first opening therein; (c) a first coating which resides on at least a portion of the core outer surface, wherein the first shell portion comprises a different material from the first coating; and (d) a first shell portion which is adjacent to the first opening and covers at least the first opening.

Claims

1. A dosage form comprising:

(a) at least one active ingredient;

(b) a core having a first surface portion upon which resides a first coating and a second surface portion which is substantially free of the first coating; and

(c) a shell which resides upon at least part of both the first coating and the second surface portion of the core,

wherein the shell comprises a different material from the first coating,

wherein the core comprises a cavity, wherein the cavity is an aperture which extends entirely through the core,

wherein at least a portion of the second surface portion of the core is located within the cavity, and

wherein the shell resides upon at least a part of the second surface portion of the core which is located within the cavity.

2. The dosage form of claim 1, in which the shell resides over all the first coating and the second surface of the core.

3. The dosage form of claim 1, in which the shell comprises a material selected from water soluble or water swellable thermoplastic film formers, water soluble or water swellable thickeners, crystallizable and non-crystallizable carbohydrates.

4. The dosage form of claim 1, in which the shell comprises a thermal-reversible carrier selected from the group consisting of thermoplastic polyalkylene glycols, thermoplastic polyalkylene oxides, and combinations thereof.

6. The dosage form of claim 1, in which the core comprises at least one active ingredient.

10. The dosage form of claim 1, in which the shell comprises at least one active ingredient.

11. The dosage form of claim 1, in which both the shell and the core each comprise at least one active ingredient.

25. The dosage form of claim 1, in which at least a portion of the active ingredient is released in a sustained manner.

28. The dosage form of claim 1, in which the core functions as an eroding matrix.

29. The dosage form of claim 1, in which the core functions as a diffusional matrix for the release of active ingredient contained therein.

30. The dosage form of claim 1, in which the core comprises a release-modifying excipient selected from the group consisting of swellable erodible hydrophilic materials, insoluble edible materials, pH-dependent polymers, and mixtures thereof.

31. The dosage form of claim 1, in which the first coating comprises at least about 30 weight percent of a thermal reversible carrier, based on the weight of the first coating.

32. The dosage form of claim 1, in which the first coating comprises at lease about 10 weight percent of a film former selected from the group consisting of film-forming water soluble polymers, film-forming proteins, film-forming water insoluble polymers, and film-forming pH-dependent polymers, and combinations thereof.

33. The dosage form of claim 1, in which the shell or shell portion comprises thermoplastic polyalkylene glycols, thermoplastic polyalkylene oxides, and combinations thereof.

34. The dosage form of claim 1, in which the shell portion is breached or dissolved within 30 minutes in 900 ml water or 0.1 N HCl, or phosphate buffer solution at 37°

C. with stirring by a USP type 2 (Paddle method) at 50 or 100 rpm.

35. The dosage form of claim 1, in which the release of at least one active ingredient follows a double pulse profile.

36. The dosage form of claim 1, in which the release of at least one active ingredient follows a delayed then sustained release profile.

37. The dosage form of claim 1, in which the release of one or more active ingredients follows a zero-order, first-order, or square root of time profile.

38. The dosage form of claim 1, in which the shell is substantially free of pores in the diameter range of 0.5 to 5.0 microns.

39. The dosage form of claim 1, in which the first coating comprises up to about 55 weight percent of a release-modifying excipient selected from water-insoluble polymers and low-melting hydrophobic materials and combinations thereof.

40. The dosage form of claim 39, in which the release-modifying excipient is a polycaprolactone.

5. A dosage form comprising:

(a) at least one active ingredient;

(b) a core comprising a center portion having an exterior surface and an annular portion having an exterior surface and an interior surface, wherein the annular portion interior surface is in contact with at least a portion of the center portion exterior surface, and a first coating resides on at least a portion of the annular portion exterior surface, and in which the core annular portion has the shape of a torus; and

(c) a shell which resides upon at least a portion of the exterior surface of the center portion, wherein the shell comprises a different material than the first coating.

7. The dosage form of claim 5, in which the center portion of the core comprises at least one active ingredient.

8. The dosage form of claim 5, in which the annular portion of the core comprises at least one active ingredient.

9. The dosage form of claim 5, in which the center portion of the core comprises a first active ingredient and the annular portion of the core comprises a second active ingredient.

12. The dosage form of claim 5, in which the first coating resides upon the entire annular portion exterior surface.

13. The dosage form of claim 12, in which the shell resides upon the entire first coating and the center portion surface.

14. The dosage form of claim 5, which the shell comprises a material selected from water soluble or water swellable thermoplastic film formers, water soluble or water swellable thickeners, crystallizable and non-crystallizable carbohydrates.

15. The dosage form of claim 5, in which the shell comprises a thermal-reversible carrier selected from the group consisting of thermoplastic polyalkylene glycols, thermoplastic polyalkylene oxides, and combinations thereof.

27. The dosage form of claim 5, in which the center portion of the core provides a time delay to the release of active ingredient from the annular portion of the core.

16. A dosage form comprising:

(a) at least one active ingredient;

(b) a core having an outer surface and a cavity which extends through the core having the shape of a torus such that the core outer surface has at least a first opening therein;

(c) a first coating which resides on at least a portion of the core outer surface, wherein the first shell portion comprises a different material from the first coating; and

(d) a first shell portion which is adjacent to the first opening and covers at least the first opening.

17. The dosage form of claim 16, in which the cavity extends entirely through the core such that the core has first and second openings therein, the first shell portion is adjacent to and covers at least the first opening, and the dosage form additionally comprises a second shell portion which is adjacent to and covers at least the second opening, wherein the first and second shell portions each comprise a material different from the first coating.

18. The dosage form of claim 16, in which the first shell portion comprises at least one water soluble material.

19. The dosage form of claim 16, in which the second shell portion comprises at least one water soluble material.

20. The dosage form of claim 16, in which the first and second shell portions each comprise at least one water soluble material.

21. The dosage form of claim 16, in which the first shell portion or the core or a combination thereof comprises at least one active ingredient.

22. The dosage form of claim 16, in which the first shell portion, second shell portion or the core or a combination thereof comprises at least one active ingredient.

23. The dosage form of claim 16, in which the first shell portion resides upon at least a portion of the first coating.

24. The dosage form of claim 22, in which the shell resides upon the entire outer surface of the first coating.

26. The dosage form of claim 24, in which the dosage form releases at least a portion of the active ingredient at a substantially constant rate.