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Details for Patent: 7,687,542

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Details for Patent: 7,687,542

Title:Rapidly bioavailable tablet and capsule formulations of diclofenac
Abstract: The present invention relates to excipients for the production of rapidly bioavailable solid oral dosage forms of diclofenac. In particular, the invention relates to the use of excipients that promote the bioavailability of such formulations, including alkaline buffering agents, gas forming excipients, hygroscopic excipients, water soluble diluents, wetting agents, and particular pharmaceutically acceptable salts.
Inventor(s): Reiner; Giorgio (Como, IT), Reiner; Alberto (Como, IT)
Assignee: Kowa Pharmaeuticals America, Inc. (Montgomery, AL)
Filing Date:Feb 10, 2006
Application Number:11/351,611
Claims:1. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1500 to about 2500 ng/ml, and (iii) an excipient base comprising means for generating a gaseous and alkaline environment for said diclofenac potassium when orally ingested into the stomach, wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients, and said means comprises an alkali metal carbonate or bicarbonate.

2. The method of claim 1 wherein said means and said diclofenac potassium are present in a weight ratio of from about 1:5 to about 4:5.

3. The method of claim 1 wherein said tablet or capsule comprises from about 5 to about 20 wt. % of said means.

4. The method of claim 1 wherein said means yields a pH greater than 7.2 and less than about 8.5 when said tablet or capsule is mixed with 200 ml, water at 25 degrees Celsius.

5. The method of claim 1 wherein said T.sub.max has been characterized as having an inter-subject variability of less than about 49%.

6. The method of claim 1 wherein said dosage form is a tablet comprising about 50 mg, of diclofenac potassium.

7. The method of claim 1 wherein said dosage form is a capsule comprising about 50 mg, of diclofenac potassium.

8. The method of claim 1 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

9. The method of claim 1 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the moisture absorption by the tablet increases.

10. The method of claim 1 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested.

11. The method of claim 1 wherein said means absorbs greater than 1 wt. % moisture when maintained in a humidity chamber at 80% relative humidity and 25 degrees Celsius for 24 hours.

12. The method of claim 1 wherein said tablet or capsule comprises at least 20 wt. % of excipients that are freely soluble in water and from about 30 to about 80 wt. % of a hygroscopic diluent, wherein the weight ratio of hygroscopic diluent to freely soluble diluent is from about 1:20 to about 5:1.

13. The method of claim 1 wherein said tablet comprises a wetting agent having a hydrophilic lipophilic balance (HLB) of greater than 14.

14. The method of claim 1 wherein said tablet comprises from about 30 to about 80 wt. % of a hygroscopic diluent and a freely soluble diluent at a weight ratio of from about 1:20 to about 5:1.

15. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1700 to about 2300 ng/ml, and (iii) an excipient base comprising means for generating a gaseous and alkaline environment for said diclofenac potassium when orally ingested into the stomach wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients, and said means comprises an alkali metal carbonate or bicarbonate.

16. The method of claim 15 wherein said means and said diclofenac potassium are present in a weight ratio of from about 1:5 to about 4:5.

17. The method of claim 15 wherein said tablet or capsule comprises from about 5 to about 20 wt. % of said means.

18. The method of claim 15 wherein said means yields a pH greater than 7.2 and less than about 8.5 when said tablet or capsule is mixed with 200 ml. water at 25 degrees Celsius.

19. The method of claim 15 wherein said T.sub.max has been characterized as having an inter-subject variability of less than about 49%.

20. The method of claim 15 wherein said dosage form is a tablet comprising about 50 mg. of diclofenac potassium.

21. The method of claim 15 wherein said dosage form is a capsule comprising about 50 mg. of diclofenac potassium.

22. The method of claim 15 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

23. The method of claim 15 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested.

24. The method of claim 15 wherein said means absorbs greater than 1 wt. % moisture when maintained in a humidity chamber at 80% relative humidity and 25 degrees Celsius for 24 hours.

25. The method of claim 15 wherein said tablet or capsule comprises at least 20 wt. % of excipients that are freely soluble in water.

26. The method of claim 15 wherein said tablet comprises a wetting agent.

27. The method of claim 15 wherein said tablet comprises from about 30 to about 80 wt. % of a hygroscopic diluent and a freely soluble diluent at a weight ratio of from about 1:20 to about 5:1.

28. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1500 to about 2500 ng/ml, and (iii) from about 7 to about 20 wt. % of a hygroscopic excipient that comprises an alkali metal carbonate or bicarbonate and that absorbs greater than 1 wt. % moisture when maintained in a humidity chamber at 80% relative humidity and 25 degrees Celsius for 24 hours, wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients.

29. The method of claim 28 wherein said hygroscopic excipient is sodium bicarbonate or potassium bicarbonate.

30. The method of claim 28 wherein said T.sub.max has been characterized as having an inter-subject variability of less than about 49%.

31. The method of claim 28 wherein said dosage form is a tablet comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

32. The method of claim 28 wherein said dosage form is a capsule comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

33. The method of claim 28 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

34. The method of claim 28 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested.

35. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1500 to about 2500 ng/ml, and (iii) an alkali metal carbonate or bicarbonate, and (iv) a hygroscopicity of greater than about 1 wt. % water absorption within a twenty four hour period in a humidity chamber maintained at 80% relative humidity, wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients.

36. The method of claim 35 wherein said T.sub.max has been characterized as having an inter-subject variability of less than about 49%.

37. The method of claim 35 wherein said-dosage form is a tablet comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

38. The method of claim 35 wherein said dosage form is a capsule comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

39. The method of claim 35 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

40. The method of claim 35 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested.

41. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1500 to about 2500 ng/ml, and (iii) an alkali metal carbonate or bicarbonate, and (iv) at least 20 wt. % of excipients that are freely soluble in water, wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients.

42. The method of claim 41 wherein said freely soluble excipient is mannitol, lactose, sucrose, or a combination thereof.

43. The method of claim 41 wherein said T.sub.max has been characterized as having an inter-subject variability of less than about 49%.

44. The method of claim 41 wherein said dosage form is a tablet comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

45. The method of claim 41 wherein said dosage form is a capsule comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

46. The method of claim 41 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

47. The method of claim 41 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested.

48. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1500 to about 2500 ng/ml, and (iii) an alkali metal carbonate or bicarbonate, and (iv) a wetting agent, wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients.

49. The method of claim 48 wherein said wetting agent has an hydrophilic lipophilic balance (HLB) of greater than about 14.

50. The method of claim 48 wherein said wetting agent is sodium lauryl sulfate.

51. The method of claim 48 wherein said T.sub.max has been characterized as having an inter-subject variability of less than about 49%.

52. The method of claim 48 wherein said dosage form is a tablet comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

53. The method of claim 48 wherein said dosage form is a capsule comprising about 50 mg. of diclofenac potassium, and said C.sub.max is from about 1700 to about 2300 ng/ml.

54. The method of claim 48 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

55. The method of claim 48 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested.

56. A method of treating acute pain in a host in need thereof comprising orally administering diclofenac potassium in an intact rapidly bioavailable tablet or capsule dosage form comprising (i) a T.sub.max of from about 5 to about 30 minutes, and (ii) a C.sub.max of from about 1500 to about 2500 ng/ml, and (iii) from about 30 to about 80 wt. % of a hygroscopic diluent that comprises an alkali metal carbonate or bicarbonate and a freely soluble diluent at a weight ratio of from about 1:20 to about 5:1, wherein said T.sub.max and C.sub.max are mean values obtained from a plurality of patients.

57. The method of claim 56 wherein said ratio is from about 1:10 to about 3:1.

58. The method of claim 56 wherein said dosage form is a tablet, wherein said tablet has a disintegration time that increases as the hardness of the tablet decreases.

59. The method of claim 56 wherein said dosage form has been characterized as yielding one C.sub.max peak when orally ingested, and said C.sub.max is from about 1700 to about 2300 ng/ml.
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