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Claims for Patent: 8,323,692

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Claims for Patent: 8,323,692

Title:Controlled release dosage forms
Abstract: The invention provides stable controlled release monolithic coating compositions for use in coating pharmaceutical oral dosage forms comprising a polyglycol having a melting point greater than 55.degree. C. and an aqueous dispersion of a neutral ester copolymer lacking functional groups.
Inventor(s): Frisbee; Steven (Reston, VA)
Assignee: Valeant International Bermuda (Hamilton, BM)
Application Number:12/328,828
Patent Claims: 1. A controlled release oral dosage form comprising: a) a core, wherein said core comprises: i) an effective amount of metformin hydrochloride, and ii) at least one first pharmaceutically acceptable excipients, and b) a stable controlled release monolithic coating surrounding the core, wherein said dosage form provides a T.sub.max of said metformin hydrochloride of from about 6 hours to about 12 hours after administration to a patient; and/or provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid and at about 37.degree. C., such that not more than 37% of the metformin hydrochloride is released after about 2 hours and not more than 61% of the metformin hydrochloride is released after about 4 hours, wherein the stable controlled release coating hydrates when placed into water, and wherein the at least one first pharmaceutically acceptable excipient comprises cross-linked polyvinylpyrrolidone, and wherein the stable controlled release coating is formed by a process comprising: coating the core with a coating composition to form a coated core, and curing the coated core to form the stable controlled release coating, wherein the coating composition comprises i) an aqueous dispersion of a neutral ester copolymer without any functional groups; ii) a poly glycol having a melting point of at least about 55.degree. C., and iii) one or more second pharmaceutically acceptable excipients; and wherein the curing is conducted at a temperature at least equal to or greater than the melting point of the poly glycol.

2. The controlled release oral dosage form of claim 1 wherein the effective amount of the metformin hydrochloride is about 1000 mg.

3. The controlled release oral dosage form of claim 1 wherein the dosage form floats when placed in an aqueous environment.

4. The controlled release oral dosage form of claim 1 wherein the dosage form expands when placed in an aqueous environment.

5. The controlled release oral dosage form of claim 1 wherein upon oral administration to a patient, an effective amount of the metformin hydrochloride is released into a region of the patient's upper gastrointestinal tract.

6. The controlled release oral dosage form of claim 1 wherein upon oral administration to a patient, the dosage form remains substantially intact until substantially all of the metformin hydrochloride is released.

7. The controlled release oral dosage form of claim 1 wherein the stable controlled release monolithic coating is formed by a process that excludes usage of an organic solvent.

8. The controlled release oral dosage form of claim 1, wherein the core further comprises at least one of colloidal silicon dioxide, polyvinyl alcohol, and glyceryl behenate.

9. The controlled release oral dosage form of claim 1, wherein the at least one second pharmaceutically acceptable excipient comprises at least one of hypromellose, talc, titanium dioxide, simethicone, and polysorbate 80.

10. The controlled release oral dosage form of claim 1, wherein the at least one second pharmaceutically acceptable excipient comprises at least one of an anti-tacking agent agent, an emulsifying agent agent, a hydrophilic agent, an antifoaming agent, a flavorant, a colorant, and a sweetener.

11. The controlled release oral dosage form of claim 1 wherein the aqueous dispersion of neutral ester copolymer without any functional groups comprises at least one of a 30% aqueous dispersion of a neutral copolymer based on ethyl acrylate and methacrylate, and a 40% aqueous dispersion of a neutral copolymer based on ethyl acrylate and methacrylate.

12. The controlled release oral dosage form of claim 1 wherein the poly glycol comprises at least one of polyethylene glycol 4000, polyethylene glycol 4600, polyethylene glycol 6000, polyethylene glycol 8000, polyethylene glycol 10000, polyethylene glycol 12000, polyethylene glycol 20000, polyethylene glycol 35000, poloxamer 188, poloxamer 338, poloxamer 407, polyethylene oxides, polyoxyethylene alkyl ethers, polyoxyethylene sorbitan fatty acid esters, and polyoxyethylene stearates.

13. The controlled release oral dosage form of claim 1 wherein the curing is conducted for a time period of from about 1 to about 24 hours.

14. The controlled release oral dosage form of claim 1 wherein the curing is conducted for a time period of from about 1 to about 16 hours.

15. The controlled release oral dosage form of claim 1 wherein the curing is conducted for a time period of from about 2 to about 7 hours.

16. The controlled release oral dosage form of claim 1 wherein the curing is conducted for a time period of from about 4 to about 7 hours.

17. The controlled release oral dosage form of claim 1 wherein the curing is conducted for a time period of from about 2 to about 4 hours.

18. The controlled release oral dosage form of claim 1 wherein the curing is conducted for a time period of from about 1 to about 3 hours.

19. The controlled release oral dosage form of claim 1 wherein the curing is conducted at a temperature at least equal to or greater than about 60 degrees C.

20. A controlled release oral dosage form comprising: a) a core, wherein said core comprises: i) metformin hydrochloride, and ii) at least one first pharmaceutically acceptable excipient excipients, and b) a stable controlled release monolithic coating surrounding the core, wherein said dosage form provides a T.sub.max of said metformin hydrochloride of from about 6 hours to about 12 hours after administration to a patient; and/or provides an in-vitro release rate of the metformin hydrochloride when tested by the USP Apparatus I (Basket Apparatus) method at 100 rpm, in 900 mL simulated gastric fluid and at about 37.degree. C., such that nor more than 37% of the metformin hydrochloride is released after about 2 hours and not more than 61% of the metformin hydrochloride is released after about 4 hours, wherein the stable controlled release coating hydrates when placed into water, and wherein the at least one first pharmaceutically acceptable excipient comprises cross-linked polyvinylpyrrolidone, wherein the stable controlled release monolithic coating is formed by a process comprising: coating the core with a coating composition to form a coated core, and curing the coated core to form the stable controlled release coating, wherein the coating composition comprises i) an ethyl acrylate and methyl methacrylate copolymer dispersion; ii) a poly glycol comprising at least one of polyethylene glycol 4000, polyethylene glycol 4600, polyethylene glycol 6000, polyethylene glycol 8000, polyethylene glycol 10000, polyethylene glycol 12000, polyethylene glycol 20000, and polyethylene glycol 35000, and iii) at least one second pharmaceutically acceptable excipient; and wherein the curing is conducted at a temperature at least equal to or greater than the melting point of the poly glycol, wherein the polyglycol has a melting point of at least about 55.degree. C.

21. The controlled release oral dosage form of claim 20, wherein the effective amount of the metformin hydrochloride is about 1000mg.

22. The controlled release oral dosage form of claim 20, wherein the dosage form floats when placed in an aqueous environment.

23. The controlled release oral dosage form of claim 20, wherein the dosage form expands when placed in an aqueous environment.

24. The controlled release oral dosage form of claim 20, wherein upon oral administration to a patient, an effective amount of the metformin hydrochloride is released into a region of the patient's upper gastrointestinal tract.

25. The controlled release oral dosage form of claim 20, wherein upon oral administration to a patient, the dosage form remains substantially intact until substantially all of the metformin hydrochloride is released.

26. The controlled release oral dosage form of claim 20, wherein the stable controlled release monolithic coating is formed by a process that excludes usage of an organic solvent.

27. The controlled release oral dosage form of claim 20, wherein the core further comprises at least one of colloidal silicon dioxide, polyvinyl alcohol, and glyceryl behenate.

28. The controlled release oral dosage form of claim 20, wherein the one or more second pharmaceutically acceptable excipients comprises at least one of hypromellose, talc, titanium dioxide, simethicone, polysorbate 80, and a mixture thereof.

29. The controlled release oral dosage form of claim 20, wherein the one or more second pharmaceutically acceptable excipients comprises at least one of an anti-tacking agent agent, an emulsifying agent agent, a hydrophilic agent, an antifoaming agent, a flavorant, a colorant, a sweetener and a mixture thereof.

30. The controlled release oral dosage form of claim 20, wherein the ethyl acrylate and methyl methacrylate copolymer dispersion comprises at least one of a 30% aqueous dispersion of a neutral copolymer based on ethyl acrylate and methacrylate, and a 40% aqueous dispersion of a neutral copolymer based on ethyl acrylate and methacrylate.

31. The controlled release oral dosage form of claim 20, wherein the curing is conducted for a time period of from about 1 to about 24 hours.

32. The controlled release oral dosage form of claim 20, wherein the curing is conducted for a time period of from about 1 to about 16 hours.

33. The controlled release oral dosage form of claim 20, wherein the curing is conducted for a time period of from about 2 to about 7 hours.

34. The controlled release oral dosage form of claim 20, wherein the curing is conducted for a time period of from about 4 to about 7 hours.

35. The controlled release oral dosage form of claim 20, wherein the curing is conducted for a time period of from about 2 to about 4 hours.

36. The controlled release oral dosage form of claim 20, wherein the curing is conducted for a time period of from about 1 to about 3 hours.

37. The controlled release oral dosage form of claim 20, wherein the curing is conducted at a temperature at least equal to or greater than about 60 degrees C.
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