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Claims for Patent: 8,062,667

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Claims for Patent: 8,062,667

Title:Modified release formulations containing drug-ion exchange resin complexes
Abstract: A coated drug-ion exchange resin complex comprising a core composed of a drug complexed with a pharmaceutically acceptable ion-exchange resin is provided. The drug-ion exchange resin complex is in admixture with a release retardant. The coating is a polyvinyl acetate polymer and a plasticizer. Methods of making and products containing this coated complex are described.
Inventor(s): Mehta; Ketan (Cranbury, NJ), Tu; Yu-Hsing (West Windsor, NJ)
Assignee: Tris Pharma, Inc. (Monmouth Junction, NJ)
Application Number:11/724,966
Patent Claims: 1. An aqueous pharmaceutical suspension composition suitable for oral ingestion comprising: (i) a particulate matrix comprising a particulate drug-ion exchange resin complex and a water insoluble polymer or copolymer, or hydrophilic polymer, said particulate matrix capable of passing through a number 40 mesh screen, said drug-ion exchange resin complex comprising a pharmaceutically acceptable drug bound to a pharmaceutically acceptable water insoluble ion exchange resin to form said drug-ion exchange resin complex, said ion exchange resin being selected from (A) a sulfonated copolymer comprising styrene and divinylbenzene, and (B) a copolymer comprising styrene and divinylbenzene having quaternary ammonium functional groups, wherein said water insoluble polymer or copolymer, or hydrophilic polymer is present in an amount of about 3% to about 30% by weight, based on the weight of said drug-ion exchange resin complex (ii) a cured, high tensile strength, water permeable, water insoluble, non-ionic polymeric diffusion barrier coating over said particulate drug-ion exchange resin complex--water insoluble polymer or copolymer, or hydrophilic polymer matrix defined in (i), said cured barrier coating applied as an aqueous dispersion and comprising (a) a polyvinylacetate polymer (b) a stabilizer, and (c) at least an amount of plasticizer effective to enhance the tensile strength of said cured barrier coating, whereby said barrier coating provides a modified release profile to said pharmaceutically acceptable drug in said drug-ion exchange resin complex in said matrix and (iii) a pharmaceutically acceptable aqueous suspension base wherein said particulate drug-ion exchange resin complex and said water insoluble polymer or copolymer, or hydrophilic polymer covered with said cured barrier coating as defined in (ii) is suspended in said aqueous suspension base.

2. The aqueous suspension composition according to claim 1, wherein said water insoluble polymer or copolymer or the hydrophilic polymer-matrix is present in an amount of about 5 to about 20% by weight, based on the weight of said drug-ion exchange resin complex defined in (i).

3. The aqueous suspension composition according to claim 1 wherein said cured barrier coating has an elongation factor of between about 125% and about 400% when measured by a texture analyzer.

4. The aqueous suspension composition according to claim 1, wherein said ion exchange resin is a sulfonated copolymer comprising styrene and divinylbenzene.

5. The aqueous suspension composition according to claim 1, wherein said ion exchange resin is a copolymer comprising styrene and divinylbenzene having quaternary ammonium functional groups.

6. The aqueous suspension composition according to claim 1, further comprising an orally ingestible drug bound to a pharmaceutically acceptable, water insoluble ion exchange resin to form an uncoated particulate drug-ion exchange resin complex, said ion exchange resin in the uncoated complex being a sulfonated copolymer comprising styrene and divinylbenzene, and wherein said drug in said uncoated complex is either the same as or different from the pharmaceutically acceptable drug in (i) and said uncoated complex being of a size capable of passing through a number 40 mesh screen.

7. The aqueous suspension composition according to claim 6, wherein said drug in said uncoated drug-ion exchange resin complex is different from said pharmaceutically acceptable drug in (i).

8. The aqueous suspension composition according to claim 6, wherein said drug in said uncoated drug-ion exchange resin complex is the same as the pharmaceutically acceptable drug in (i).

9. The aqueous suspension composition according to claim 8, wherein said drug in said uncoated drug-ion exchange resin complex is a methylphenidate.

10. The aqueous suspension composition according to claim 1, further comprising a pharmaceutically acceptable drug in said pharmaceutically acceptable aqueous suspension base defined in (iii) being the same as or different from said pharmaceutically acceptable drug in (i).

11. The aqueous suspension composition according to claim 10, wherein said pharmaceutically acceptable drug in said suspension base is an antihistamine and is a different drug from said pharmaceutically acceptable drug in (i).

12. The aqueous suspension composition according to claim 11, wherein said antihistamine is fexofenadine or a pharmaceutically acceptable salt thereof.

13. The aqueous suspension composition according to claim 1, wherein said particulate matrix comprises said particulate drug-ion exchange resin complex and said hydrophilic polymer.

14. The aqueous suspension composition according to claim 13, wherein said hydrophilic polymer comprises a polyvinylpyrrolidone.

15. The aqueous suspension composition according to claim 1, wherein said cured barrier coating comprises polyvinyl acetate, polyvinylpyrrolidone and an effective amount of a surfactant, said polyvinylacetate and polyvinylpyrrolidone being in a dry weight ratio about 10:1.

16. The aqueous suspension composition according to claim 1, wherein said particulate matrix comprises said particulate drug-ion exchange resin complex and said water insoluble polymer or copolymer.

17. The aqueous suspension composition according to claim 16, wherein said water insoluble polymer in said particulate matrix comprises polyvinylacetate, wherein said particulate matrix comprises said particulate drug-ion exchange resin complex, a stabilizer comprising polyvinylpyrrolidone and an effective amount of a surfactant.

18. The aqueous suspension composition according to claim 17, said surfactant in said particulate matrix being sodium lauryl sulfate, wherein said particulate matrix is prepared by a process comprising mixing said particulate drug-ion exchange resin complex with an aqueous dispersion comprising said polyvinylacetate, said polyvinylpyrrolidone and said sodium lauryl sulfate to form a mass, drying said mass and milling through a 40 mesh screen, and wherein said polyvinylacetate is present in an amount of about 27% by weights of the said aqueous dispersion, said polyvinylpyrrolidone is present in an amount of about 2.7% by weight of said aqueous dispersion, and said sodium lauryl sulfate is present in an amount of about 0.3% by weight of the said aqueous dispersion which comprises 30% w/w solids.

19. The aqueous suspension composition according to claim 16, wherein said water insoluble polymer or copolymer comprises an acrylate polymer or copolymer.

20. The aqueous suspension composition according to claim 19, wherein said water insoluble copolymer comprises ethyl acrylate and methyl methacrylate.

21. The aqueous suspension composition according to claim 1 , wherein said plasticizer comprises about 5% to about 10% w/w of solids in said cured barrier coating.

22. The aqueous suspension composition according to claim 20 wherein said plasticizer comprises triacetin.

23. The aqueous suspension composition according to claim 1 wherein said cured barrier coating further comprises a surfactant comprising sodium lauryl sulfate.

24. The aqueous suspension composition according to claim 1, wherein said cured barrier coating comprises about 5% to about 200% by weight of the particulate drug-ion exchange resin complex defined in (i).

25. The aqueous suspension composition according to claim 24, wherein said cured barrier coating comprises about 35% to about 50% by weight of the particulate drug-ion exchange resin complex defined in (i).

26. The aqueous suspension composition according to claim 24, wherein said cured barrier coating comprises about 30% to about 45% by weight of the composition particulate drug-ion exchange resin complex defined in (i).

27. The aqueous suspension composition according to claim 1, wherein said cured barrier coating comprises 50% by weight of the particulate drug-ion exchange resin complex defined in (i).

28. The aqueous suspension composition according to claim 1, wherein said pharmaceutically acceptable drug in said particulate drug-ion exchange resin complex defined in (i) is selected from the group consisting of morphine, oxycodone, albuterol, methylphenidate, dexmethylphenidate, dextromethorphan, codeine, tramadol, pseudoephedrine, phenylephrine, hydrocodone, venlafaxine, ibuprofen, oxybutynin, clonidine, dexchlorpheniramine, fexofenadine, diphenhydramine, carbemazepine, oxymorphone, carbinoxamine, dicylomine, chlorpheniramine, amphetamine, naproxene, diclofenac, paroxetine, amoxicillin and pharmaceutically acceptable salts thereof.

29. The aqueous suspension composition according to claim 28, wherein said pharmaceutically acceptable drug in (i) is hydrocodone.

30. The aqueous suspension composition according to claim 28, wherein said pharmaceutically acceptable drug in (i) is clonidine.

31. The aqueous suspension composition according to claim 28, wherein said pharmaceutically acceptable drug in (i) is pseudoephedrine.

32. The aqueous suspension composition according to claim 1, wherein said pharmaceutically acceptable drug in (i) is selected from methylphenidate and dexmethylphenidate.

33. The aqueous suspension composition according to claim 1, wherein said pharmaceutically acceptable drug in (i) is carbinoxamine.

34. The aqueous suspension composition according to claim 28, wherein said pharmaceutically acceptable drug in (i) is diphenhydramine.

35. The aqueous suspension composition according to claim 28, wherein said pharmaceutically acceptable drug in (i) is ibuprofen.

36. The aqueous suspension composition according to claim 28, wherein said pharmaceutically acceptable drug in (i) is morphine.

37. An orally ingestible aqueous pharmaceutical suspension composition, comprising: (i) a particulate matrix comprising a particulate dextromethorphan-ion exchange resin complex, said dextromethorphan-ion exchange resin complex comprising dextromethorphan bound to a pharmaceutically acceptable water insoluble ion exchange resin, wherein said ion exchange resin is a sulfonated copolymer of styrene and divinylbenzene and wherein said matrix further comprises about 5% to about 20%, based on the weight of said dextromethorphan-ion exchange resin complex, of a water insoluble polymer or copolymer or a hydrophilic polymer, said particulate matrix comprising granules having a size capable of passing through a number 40 mesh screen; (ii) a cured high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating over said dextromethorphan-ion exchange resin complex and said water insoluble polymer or said hydrophilic polymer defined in (i), said cured barrier coating applied as an aqueous dispersion, and wherein said cured barrier coating comprises polyvinylacetate with a stabilizer comprising polyvinylpyrrolidone in a weight ratio of about 10:1, respectively, and said cured barrier coating further comprising from about 5% to about 10% by weight of a plasticizer based on the dry weight of said cured barrier coating, (iii) an uncoated particulate dextromethorphan-ion exchange resin complex wherein said ion exchange resin comprises a sulfonated copolymer of styrene and divinylbenzene and wherein said uncoated dextromethorphan-ion exchange resin complex comprises particles of a size capable of passing through a number 40 mesh screen; and (iv) a pharmaceutically acceptable aqueous suspension base, wherein said coated particulate dextromethorphan-ion exchange resin complex and said water insoluble polymer or said hydrophilic polymer defined in (ii) and said uncoated particulate dextromethorphan-ion exchange resin complex defined in (iii) are suspended in said base.

38. The aqueous pharmaceutical suspension composition according to claim 37, wherein said aqueous dispersion further comprises an effective amount of surfactant.

39. The aqueous pharmaceutical suspension composition according to claim 37, wherein said aqueous dispersion comprises polyvinylacetate in an amount of about 27% by weight polyvinylpyrrolidone in an amount of about 2.7% by weight, and sodium lauryl sulfate in an amount of about 0.3% by weight of the the aqueous dispersion which comprises 30% w/w solids.

40. The aqueous pharmaceutical suspension composition according to claim 37, wherein said plasticizer is triacetin.

41. The aqueous suspension composition according to claim 1, wherein said particulate matrix (i) comprises about 10% by weight to about 15% by weight of water insoluble polymer or copolymer.

42. The aqueous suspension composition according to claim 1, further comprising a second modified release diffusion barrier coated drug-ion exchange resin complex-matrix , wherein said second modified release diffusion barrier coated drug-in exchange resin complex-matrix contains a pharmaceutically acceptable drug which differs from the drug of said drug-ion exchange resin complex-matrix of (ii).

43. The aqueous suspension composition according to claim 1, wherein the cured barrier coating layer comprises at least about 75% w/w polyvinylacetate.

44. The aqueous suspension composition according to claim 1, wherein the cured barrier coating layer comprises about 75% to about 90% w/w polyvinylacetate.

45. The aqueous suspension composition according to claim 43, wherein the cured barrier coating layer comprises about 2.5% to about 20% by weight plasticizer.

46. The aqueous suspension composition according to claim 1, wherein the stabilizer is present in an amount of about 5 to about 10% w/w of the cured barrier coating layer.

47. The aqueous suspension composition according to claim 46, wherein the cured barrier coating further comprises a surfactant.

48. The aqueous pharmaceutical suspension composition suitable for oral ingestion according to claim 1, wherein said cured barrier coating comprises at least about 75% w/w polyvinylacetate, a stabilizer, and about 2.5% to about 20% w/w plasticizer based on the weight of said cured barrier coating.

49. The aqueous pharmaceutical suspension according to claim 48, wherein said barrier coating provides about 25% w/w to about 50% w/w weight gain to the particulate drug-ion exchange resin complex-matrix.

50. The aqueous pharmaceutical suspension according to claim 49, wherein said barrier coating provides about 30% w/w to about 45% w/w weight gain to the drug-ion exchange resin complex-matrix.

51. The aqueous pharmaceutical suspension according to claim 48, wherein the water insoluble polymer or copolymer, or hydrophilic polymer of said particulate matrix is present in an amount of about 5% w/w to about 20% w/w of the drug-ion exchange resin complex-matrix particles.

52. The aqueous pharmaceutical suspension according to claim 51, wherein the water insoluble polymer or copolymer, or hydrophilic polymer of said particulate matrix is present in an amount of about 10% w/w to about 15% w/w of the drug-ion exchange resin complex-matrix particles.

53. The aqueous pharmaceutical suspension according to claim 51, wherein the water insoluble polymer or copolymer, or hydrophilic polymer of said particulate matrix is present in an amount of about 10% w/w to about 15% w/w of the drug-ion exchange resin complex particles.

54. The aqueous pharmaceutical oral suspension according to claim 48, wherein the hydrophilic polymer of said particulate matrix is polyvinylpyrrolidone.

55. The aqueous pharmaceutical oral suspension according to claim 48, wherein said particulate matrix comprises polyvinylacetate, polyvinylpyrrolidone, and a surfactant.
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