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Claims for Patent: 8,202,537

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Claims for Patent: 8,202,537

Title:Modified release formulations containing drug-ion exchange resin complexes
Abstract: A solid dose composition containing a mixture of a cured, modified release-barrier coated methylphenidate-ion exchange resin complex-matrix and an uncoated methylphenidate-ion exchange resin complex is described. The barrier coated methylphenidate-ion exchange resin complex-matrix comprises methylphenidate complexed with a pharmaceutically acceptable ion-exchange resin to form the complex which is admixed with a polymer to form a methylphenidate-ion exchange resin complex-matrix, which is subsequently coated with a modified release coating. The modified coating contains polyvinyl acetate polymer and a plasticizer and is cured.
Inventor(s): Mehta; Ketan (Cranbury, NJ), Tu; Yu-Hsing (West Windsor, NJ)
Assignee: Tris Pharma Inc (Monmouth Junction, NJ)
Application Number:13/244,748
Patent Claims: 1. A solid modified release methylphenidate tablet which provides at least about a 12 hour release profile and is suitable for oral ingestion which consists of methylphenidate particulates and pharmaceutically acceptable excipients compressed into a tablet, wherein said methylphenidate particulates comprise: (A) a modified release methylphenidate component having a single active drug consisting of a methylphenidate, said component consisting of (i) a particulate matrix comprising a particulate methylphenidate-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 methylphenidate-ion exchange resin complex comprising a pharmaceutically acceptable methylphenidate bound to a pharmaceutically acceptable water insoluble ion exchange resin to form said methylphenidate-ion exchange resin complex, said ion exchange resin being a sulfonated copolymer comprising styrene and divinylbenzene, 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 methylphenidate-ion exchange resin complex, (ii) a cured, high tensile strength, water permeable, water insoluble, non-ionic polymeric diffusion barrier coating over said particulate methylphenidate-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 methylphenidate in said methylphenidate-ion exchange resin complex-matrix and (B) a particulate uncoated methylphenidate-ion exchange resin complex comprising a pharmaceutically acceptable methylphenidate as the sole active drug in the complex bound to a pharmaceutically acceptable water insoluble ion exchange resin to form said methylphenidate-ion exchange resin complex, said ion exchange resin being a sulfonated copolymer comprising styrene and divinylbenzene.

2. The composition according to claim 1, wherein said ion exchange resin which is a sulfonated copolymer comprising styrene and divinylbenzene of (A) and (B) is an irregularly shaped particle.

3. The composition according to claim 1, wherein said methylphenidate is dexmethylphenidate in (A) and/or (B).

4. The composition according to claim 1, wherein said matrix comprises a water insoluble polymer or copolymer, or hydrophilic polymer in an amount of about 5 to about 20% by weight, based on the weight of said methylphenidate-ion exchange resin complex defined in (i).

5. The composition according to claim 1 wherein said cured high tensile strength, water permeable, water insoluble non-ionic polymeric diffusion barrier coating has an elongation factor of between about 125% and about 400%.

6. The composition according to claim 1, wherein said methylphenidate-ion exchange resin complex-matrix includes a hydrophilic polymer.

7. The composition according to claim 6, wherein said hydrophilic polymer comprises a polyvinylpyrrolidone.

8. The composition according to claim 1, wherein said aqueous based coating dispersion comprises about 30% solids comprising polyvinylacetate with polyvinylpyrrolidone in a dry weight ratio about 10:1, respectively, and further includes an effective amount of a surfactant.

9. The composition according to claim 1, wherein said methylphenidate-ion exchange resin complex-matrix comprises a water insoluble polymer or copolymer.

10. The composition according to claim 9, wherein said methylphenidate-ion exchange resin complex-matrix comprises polyvinylacetate with a stabilizer comprising polyvinylpyrrolidone and an effective amount of a surfactant.

11. The composition according to claim 10, wherein said water insoluble polymer is an aqueous dispersion comprising polyvinylacetate in an amount of about 27% w/w of the solids, polyvinylpyrrolidone in an amount of about 2.7% w/w of the solids, and sodium lauryl sulfate in an amount of about 0.3% w/w of the solids in the dispersion which is admixed with said methylphenidate-ion exchange resin complex to form said methylphenidate-ion exchange resin complex-matrix.

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

13. The composition according to claim 12 wherein said plasticizer comprises triacetin.

14. The composition according to claim 1 wherein said barrier coating further comprises a surfactant comprising sodium lauryl sulfate.

15. The composition according to claim 1, wherein said cured, high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating comprises about 5% to about 200% by weight of the matrix defined in (i).

16. The composition according to claim 15, wherein said cured, high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating comprises about 35% to about 50% by weight of the matrix defined in (i).

17. The composition according to claim 15, wherein said cured, high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating comprises about 30% to about 45% by weight of the matrix defined in (i).

18. The composition according to claim 1, wherein said cured, high tensile strength, water permeable, water insoluble, non ionic polymer diffusion barrier coating is cured for about 4 to about 16 hours.

19. The composition according to claim 18, wherein said coating is cured for about 5 hours at about 50.degree. C. to about 65.degree. C.

20. The composition according to claim 19, wherein said coating is cured at about 60.degree. C.

21. The composition according to claim 1, wherein said cured, high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating comprises 50% by weight of the matrix defined in (i).

22. The solid modified release methylphenidate tablet according to claim 1, wherein said tablet further comprises a methylphenidate component which is not in a drug-ion exchange resin complex, in addition to said modified release methylphenidate component (A) and said uncoated methylphenidate-ion exchange resin complex (B).

23. The solid modified release methylphenidate tablet according to claim 1, wherein said cured barrier coating comprises about 70% w/w to about 90% w/w polyvinylacetate, about 5% w/w to about 10% w/w polyvinylpyrrolidone, and about 2.5% to about 20% plasticizer w/w, based on the weight of the cured barrier coating layer.

24. The composition according to claim 11, wherein said cured, high tensile strength, water permeable, water insoluble, non ionic polymeric diffusion barrier coating comprises about 25% to about 35% by weight of the methylphenidate-ion exchange resin complex-matrix defined in (i).
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