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Claims for Patent: 8,747,897

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Claims for Patent: 8,747,897

Title:Osmotic drug delivery system
Abstract: An oral osmotic pharmaceutical delivery system comprises a highly water-soluble drug exhibiting an erratic or an incomplete release profile when formulated in a elementary osmotic pump delivery system and at least one release enhancing agent.
Inventor(s): Kidane; Argaw (Montgomery Village, MD), Bhatt; Padmanabh P. (Rockville, MD)
Assignee: Supernus Pharmaceuticals, Inc. (Rockville, MD)
Application Number:11/412,100
Patent Claims: 1. An oral osmotic pharmaceutical dosage form of treprostinil, comprising an osmotically active drug core surrounded by a semi-permeable membrane, wherein the osmotically active drug core comprises A) at least one release enhancing agent selected from a group consisting of wicking agents, complexing agents, and micelle-forming agents, wherein i) the wicking agents are selected from the group consisting of high HLB surfactants, ionic surfactants, and non-swelling hydrophilic polymers, ii) the complexing agents are selected from the group consisting of polyvinyl pyrrolidone, cyclodextrins, and non-ionic surface active agents, and iii) the micelle-forming agents are selected from the group consisting of poly(ethylene oxide) modified sorbitan monoesters, fatty acid sorbitan esters, sodium lauryl sulfate, and sodium docusate, and B) treprostinil as treprostinil diethanolamine, and wherein the semi-permeable membrane includes at least one opening suitable for providing for the osmotic delivery of the treprostinil from the osmotically active drug core.

2. An oral osmotic pharmaceutical dosage form of claim 1, wherein the treprostinil diethanolamine has water solubility of at least about 30 mg/ml.

3. An oral osmotic pharmaceutical dosage form of claim 1 exhibiting an in-vivo release profile that may be predicted from an in-vitro release profile.

4. An oral osmotic pharmaceutical dosage form of claim 1, wherein said oral osmotic pharmaceutical dosage form is a sustained-release dosage form.

5. An oral osmotic pharmaceutical dosage form of claim 4, wherein the treprostinil diethanolamine has a short half-life.

6. An oral osmotic pharmaceutical dosage form of claim 5, wherein said half-life ranges from several minutes to three hours.

7. An oral osmotic pharmaceutical dosage form of claim 1, wherein the amount of treprostinil diethanolamine is sufficient to produce a therapeutically effective plasma concentration of treprostinil.

8. An oral osmotic pharmaceutical dosage form of claim 7, wherein the therapeutically effective plasma concentration of treprostinil in a human has a C.sub.min of 0.1 ng/ml to 0.2 ng/ml.

9. An oral osmotic pharmaceutical dosage form of claim 7, wherein the therapeutically effective plasma concentration of treprostinil in a human has a C.sub.max of 0.5 ng/ml to 2 ng/ml.

10. An oral osmotic pharmaceutical dosage form of claim 9, wherein the therapeutically effective plasma concentration of treprostinil in a human has a T.sub.max (time to reach C.sub.max) of 2 hours to 8 hours.

11. An oral osmotic pharmaceutical dosage form of claim 7, wherein the therapeutically effective plasma concentration of treprostinil is maintained to allow for a twice-a-day or once-a-day administration.

12. An oral osmotic pharmaceutical dosage form of claim 7, wherein the therapeutically effective plasma concentration of treprostinil results in reduced side effects.

13. An oral osmotic pharmaceutical dosage form of claim 1 wherein said at least one release enhancing agent is present in the dosage form in a concentration of 0.5% to 90% by weight.

14. An oral osmotic pharmaceutical dosage form of claim 1 wherein said release-enhancing agent is selected from the group consisting of wicking agents and micelle-forming agents.

15. An oral osmotic pharmaceutical dosage form of claim 1, wherein said at least one release enhancing agent is a wicking agent selected from the group consisting of ionic surfactants, and non-swelling hydrophilic polymers.

16. An oral osmotic pharmaceutical dosage form of claim 1, wherein said at least one release enhancing agent is a non-swelling hydrophilic polymer selected from the group consisting of polyethylene oxide-polypropylene oxide block copolymers, cellulose ethers, and polyethylene glycols.

17. An oral osmotic pharmaceutical dosage form of claim 1, wherein said at least one release enhancing agent is a complexing agent selected from the group consisting of polyvinyl pyrrolidone, and non-ionic surface active agents.

18. An oral osmotic pharmaceutical dosage form of claim 1, wherein said at least one release enhancing agent is a micelle-forming agent selected from the group consisting of poly(ethylene oxide) modified sorbitan monoesters, fatty acid sorbitan esters, and sodium lauryl sulfate.

19. An oral osmotic pharmaceutical dosage form of claim 1, wherein said dosage form is selected from the group consisting of tablets, capsules, and pellets.

20. A method of oral delivery of treprostinil comprising administering to a human patient in need thereof an oral osmotic pharmaceutical dosage form of claim 1.

21. A method of claim 20, where said at least one release enhancing agent is selected from a group consisting of wicking agents, and micelle-forming agents.

22. A method of claim 21, wherein said at least one release enhancing agent is a wicking agent is selected from the group consisting of ionic surfactants, and non-swelling hydrophilic polymers.

23. A method of claim 22, wherein said at least one release enhancing agent is a non-swelling hydrophilic polymer selected from the group consisting of polyethylene oxide-polypropylene oxide block copolymers, cellulose ethers, and polyethylene glycols.

24. A method of claim 22, where said at least one release enhancing agent is a complexing agent selected from the group consisting of polyvinyl pyrrolidone, and non-ionic surface active agents.

25. A method of claim 21, wherein said at least one release enhancing agent is a micelle-forming agent selected from the group consisting of poly(ethylene oxide) modified sorbitan monoesters, fatty acid sorbitan esters, and sodium lauryl sulfate.

26. A method of claim 20, wherein said treprostinil diethanolamine has a short half-life.

27. A method of claim 26, wherein said treprostinil diethanolamine has a half-life ranging from several minutes up to three hours.

28. A method of claim 20, wherein the amount of treprostinil diethanolamine is sufficient to produce a therapeutically effective plasma concentration of treprostinil.

29. A method of claim 28, wherein the therapeutically effective plasma concentration of treprostinil in a human has a C.sub.min of 0.1 ng/ml to 0.2 ng/ml.

30. A method of claim 28, wherein the therapeutically effective plasma concentration of treprostinil in a human has a C.sub.max of 0.5 ng/ml to 2 ng/ml.

31. A method of claim 30, wherein the therapeutically effective plasma concentration of treprostinil in a human has a T.sub.max (time to reach C.sub.max) of 2 hours to 8 hours.

32. A method of claim 28, wherein the therapeutically effective plasma concentration of treprostinil is maintained to allow for a twice-a-day or once-a-day administration.

33. A method of treating a disease selected from the group consisting of pulmonary hypertension, pulmonary arterial hypertension (PAH), peripheral vascular disease (PVD), ischemic diseases, heart failure, conditions requiring anticoagulation, thrombotic microangiopathy, extracorporeal circulation, central retinal vein occlusion, atherosclerosis, inflammatory diseases, hypertension, cancer and other conditions of unregulated cell growth, comprising administering to a patient in need thereof an oral osmotic pharmaceutical dosage form of claim 1.

34. A method of claim 33, wherein said at least one release enhancing agent is selected from the group consisting of wicking agents, and micelle-forming agents.

35. A method of claim 34, wherein said at least one release enhancing agent is a wicking agent is selected from the group consisting of ionic surfactants, and non-swelling hydrophilic polymers.

36. A method of claim 35, wherein said at least one release enhancing agent is a non-swelling hydrophilic polymer selected from the group consisting of polyethylene oxide-polypropylene oxide block copolymers, cellulose ethers, and polyethylene glycols.

37. A method of claim 33, where said at least one release enhancing agent is a complexing agent selected from the group consisting of polyvinyl pyrrolidone, and non-ionic surface active agents.

38. A method of claim 34, wherein said at least one release enhancing agent is a micelle forming agent selected from the group consisting of poly(ethylene oxide) modified sorbitan monoesters, fatty acid sorbitan esters, and sodium lauryl sulfate.

39. A method of claim 33, wherein said disease is pulmonary arterial hypertension (PAH).

40. An oral osmotic pharmaceutical dosage form of claim 1, which is a tablet comprising treprostinil diethanolamine in an amount equivalent to about 1 mg treprostinil.

41. An oral osmotic pharmaceutical dosage form of claim 1, which is a tablet comprising treprostinil diethanolamine in an amount equivalent to about 1 mg to 5 mg of treprostinil.

42. An oral osmotic pharmaceutical dosage form of claim 1, which is a tablet comprising treprostinil diethanolamine in an amount equivalent to about 1 mg to 10 mg of treprostinil.

43. An oral osmotic pharmaceutical dosage form of claim 7, wherein the therapeutically effective plasma concentration of treprostinil in a human has a C.sub.min of 0.1 ng/ml to 0.2 ng/ml, and a C.sub.max of 0.5 ng/ml to 2 ng/ml, and a T.sub.max (time to reach C.sub.max) of 2 hours to 8 hours.

44. A method of claim 20, wherein the oral osmotic pharmaceutical dosage form is a tablet comprising treprostinil diethanolamine in an amount equivalent to about 1 mg of treprostinil.

45. A method of claim 20, wherein the oral osmotic pharmaceutical dosage form is a tablet comprising treprostinil diethanolamine in an amount equivalent to about 1 mg to 5 mg of treprostinil.

46. A method of claim 20, wherein the oral osmotic pharmaceutical dosage form is a tablet comprising treprostinil diethanolamine in an amount equivalent to about 1 mg to 10 mg of treprostinil.

47. A method of claim 20, wherein the oral osmotic pharmaceutical dosage form is administered in an amount sufficient to produce a plasma concentration of treprostinil having a C.sub.min of 0.1 ng/ml to 0.2 ng/ml, and a C.sub.max of 0.5 ng/ml to 2 ng/ml, and a T.sub.max (time to reach C.sub.max) of 2 hours to 8 hours.

48. An oral osmotic pharmaceutical dosage form of claim 1, wherein the semi-permeable membrane comprises cellulose acetate and at least one component select from the group consisting of triethyl citrate (TEC), propylene glycol(PG), mixtures in ratios of TEC to PG ranging from 25:75 to 75:25, Tween 80, polyethylene glycol (PEG); a polyoxyethylene sorbitan ester, triacetin, diethyl phthalate, mineral oil, tributyl sebacate, and glycerol.

49. An oral osmotic pharmaceutical dosage form of claim 48, wherein the semi-permeable membrane comprises triethyl citrate.

50. An oral osmotic pharmaceutical dosage form of claim 1, which comprises an effective amount of treprostinil diethanolamine up to about 1 mg of treprostinil as treprostinil diethanolamine.

51. An oral osmotic pharmaceutical dosage form of claim 1, which comprises an effective amount of treprostinil diethanolamine up to about 5 mg of treprostinil as treprostinil diethanolamine.

52. An oral osmotic pharmaceutical dosage form of claim 1, which comprises an effective amount of treprostinil diethanolamine up to about 10 mg of treprostinil as treprostinil diethanolamine.

53. An oral osmotic pharmaceutical dosage form of claim 1, wherein the semi-permeable membrane comprises 3% to 10% by weight of the oral osmotic pharmaceutical dosage form.

54. An oral osmotic pharmaceutical dosage form of claim 1, wherein the semi-permeable membrane includes one opening suitable for providing for the osmotic delivery of the treprostinil diethanolamine from the osmotically active drug core.

55. An oral osmotic pharmaceutical dosage form of claim 13, wherein said at least one release enhancing agent is present in the dosage form in a concentration of 1% to 20% by weight.

56. An oral osmotic pharmaceutical dosage form of claim 1, wherein the osmotically active drug core further comprises at least one osmotic agent.

57. An oral osmotic pharmaceutical dosage form of claim 56, wherein the at least one osmotic agent is selected from the group consisting of sucrose, xylitol, glucose, lactose, sodium chloride, potassium chloride, cellulose ethers, maltodextrins, and cyclodextrins.

58. An oral osmotic pharmaceutical dosage form of claim 56, wherein e at least one osmotic agent is present in the dosage form in a concentration of 1% by weight to 90% by weight.

59. An oral osmotic pharmaceutical dosage form of claim 1, wherein the at least one release enhancing agent is sodium lauryl sulfate.

60. An oral osmotic pharmaceutical dosage form of claim 59, wherein the at least one osmotic agent is comprises xylitol.
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