NON-HOMOGENOUS DOSAGE FORM COATINGS

Abstract

The present invention is directed to liquid coating compositions and dosage forms having a continuous shell portion of a first composition and at least one discontinuous shell portion that is compositionally different located within the continuous shell portion. The present invention also provides a process for preparing a dosage form, which comprises coating a core with a continuous shell portion having a first composition and at least one discontinuous shell portion that is compositionally different located within the continuous portion, and then cooling the coated core. The coating compositions are particularly suited for forming shell coatings on solid pharmaceutical dosage forms.

Description

Claims

1. A liquid pharmaceutical dosage coating composition comprising: a) a shell-forming component comprising a dispersion of: i) at least one film-forming polymer in liquid form that is liquid at temperatures of 37° C. or above; andii) at least one particle forming polymer in solid particle form for a discontinuous phase that is dispersed in said polymer in liquid form in (i),

2. A liquid pharmaceutical dosage coating composition according to claim 1 wherein the at least one film-forming polymer is water-insoluble.

3. A liquid pharmaceutical dosage coating composition according to claim 1 wherein the at least one film-forming polymer is a water-soluble or water swellable gelling polymer.

4. A liquid pharmaceutical dosage coating composition according to claim 3 wherein the gelling polymer consists essentially of at least one gelatin.

5. A liquid pharmaceutical dosage coating composition according to claim 2 wherein the water-insoluble film-forming polymer is crosslinked.

6. A liquid pharmaceutical dosage coating composition according to claim 1 wherein the at least one particle forming polymer is water-insoluble.

7. A liquid pharmaceutical dosage coating composition according to claim 6 wherein the water-insoluble particle forming particle is crosslinked.

8. A liquid pharmaceutical dosage coating composition according to claim 1 wherein the particles have a number average particle size less than about 3000 microns.

9. A liquid pharmaceutical dosage coating composition according to claim 8 wherein the particles have a number average particle size less than about 1000 microns.

10. A liquid pharmaceutical dosage coating composition according to claim 8 wherein the particles are spherically shaped and have a number average particle size between about 30 microns to about 3000 microns.

11. The liquid of pharmaceutical dosage coating composition according to claim 1 wherein the solid particles are amorphous.

12. The liquid of pharmaceutical dosage coating composition according to claim 1 wherein the solid particles are water soluble.

13. A solid pharmaceutical dosage form comprising a core and at least one coating layer that comprises a solid continuous film having discrete compositionally different regions dispersed therein.

14. A solid pharmaceutical dosage form according to claim 13 wherein the core comprises a compressed powder tablet.

15. A solid pharmaceutical dosage form according to claim 13 wherein at least one coating layer has a concave dimpled surface area comprising dimpled portions.

16. A solid pharmaceutical dosage form according to claim 13 wherein the diameter of dimpled portions in said raised dimpled surface area is between about 30 microns to about 3000 microns.

17. A solid pharmaceutical dosage form according to claim 15 wherein the diameter of dimpled portions in said concave dimpled surface area is between about 30 microns to about 3000 microns.

18. A solid pharmaceutical dosage form according to claim 15 wherein the thickness of the solid continuous film is, on average, at least 10% greater than the smallest thickness of the solid continuous film and the overlying discrete compositionally different regions in said regions having a concave surface area.

19. A solid pharmaceutical dosage form according to claim 13 wherein at least one coating layer has a raised dimple surface area comprising dimpled portions.

20. A solid pharmaceutical dosage form according to claim 19 wherein the thickness of the solid continuous film is, on average, at least 10% less than the greatest thickness of the solid continuous film and overlying discrete compositionally different region in said regions having raised dimple surface area.

21. A solid pharmaceutical dosage form according to claim 13 wherein the discrete compositionally different regions have greater water solubility than the solid continuous film.

22. A process for preparing a solid dosage form comprising coating a core containing a pharmaceutical active ingredient with the composition according to claim 1.

23. A process for preparing a solid dosage form according to claim 22 wherein the solid particles are sufficiently hydrated to deform in an injection molding system.

24. A process for preparing a core and shell dosage form comprising: a) forming a compressed core containing at least one pharmaceutical active ingredient in compression tableting machine; andb) coating the compressed core with the composition according to claim 0.

25. A process for preparing a core and shell dosage form comprising a) forming a solid, compressed core containing at least one pharmaceutical active ingredient in a tableting machine;b) introducing the compressed core into a mold cavity; andc) injecting the composition according to claim 1 into the mold cavity to coat at least a portion of the compressed core.

26. A process for preparing a core and shell dosage form comprising a) forming a solid, compressed core containing at least one pharmaceutical active ingredient in a tableting machine;b) introducing the compressed core into a mold cavity;c) injecting the composition according to claim 1 into the mold cavity to coat at least a portion of the compressed core;d) rotating the mold cavity; ande) injecting a liquid curable composition into said mold to coat at least a second portion of the compressed core.