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Last Updated: May 12, 2021

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Claims for Patent: 10,849,857

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Summary for Patent: 10,849,857
Title:Pharmaceutical compositions comprising active drugs, contraceptive kits comprising active drugs, and methods of administering the same
Abstract: The present invention relates to pharmaceutical compositions and kits comprising pharmaceutical compositions, and methods for administering pharmaceutical compositions comprising active contraceptive drugs in a patient. Specifically, the pharmaceutical compositions may comprise progestogen-only contraceptives ("POC"), such as Drospirenone.
Inventor(s): Perrin; Philippe (Paris, FR), Velada; Jose Luis (Amersfoort, NL), Drounin; Dominique (Verrieres, FR)
Assignee: LABORATORIOS LEON FARMA SA (Leon, ES)
Application Number:13/171,410
Patent Claims: 1. A unit dose of a pharmaceutical composition comprising: drospirenone in a particle form that has a d.sub.50 ranging from 10 micrometers (.mu.m) to 60 .mu.m, the drospirenone being present in an amount ranging from 2 milligrams (mg) to 6 mg; microcrystalline cellulose in an amount ranging from 50% to 65%, by weight, of the pharmaceutical composition; anhydrous lactose in an amount ranging from 25% to 35%, by weight, of the pharmaceutical composition; silicon dioxide in an amount ranging from 0.2% to 6%, by weight, of the pharmaceutical composition; and magnesium stearate in an amount ranging from 0.2% to 0.6%, by weight, of the pharmaceutical composition, wherein the pharmaceutical composition does not comprise estrogen, wherein, when subjected to an in vitro dissolution test according to the USP XXIII Paddle Method, no more than 50% of the drospirenone initially present in the pharmaceutical composition is dissolved within 30 minutes.

2. A method for providing contraception, increasing cycle stability, or both, the method comprising administering the unit dose of claim 1 to a subject.

3. The method of claim 2, wherein the unit dose is administered in a 28 day daily dosing regimen.

4. A kit comprising one or more packaging units wherein each packaging unit comprises up to 28 of the unit doses of claim 1.

5. The kit of claim 3, wherein each packaging unit comprises 24 of the unit doses.

6. A unit dose of a pharmaceutical composition comprising: drospirenone in a particle form that has a d.sub.50 ranging from 10 micrometers (.mu.m) to 60 .mu.m, the drospirenone being present in an amount ranging from 2 milligrams (mg) to 6 mg; a binder in an amount ranging from 50% to 65%, by weight, of the pharmaceutical composition, wherein the binder comprises a starch, a gum, microcrystalline cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose, hydroxypropylmethyl cellulose, polyvinyl pyrrolidone, or a combination thereof; a filler in an amount ranging from 25% to 35%, by weight, of the pharmaceutical composition, wherein the filler comprises anhydrous lactose, microcrystalline cellulose, starch, pregelatinized starch, modified starch, dibasic calcium phosphate dihydrate, calcium sulfate trihydrate, calcium sulfate dihydrate, calcium carbonate, lactose, dextrose, sucrose, mannitol, sorbitol, or a combination thereof; a glidant in an amount ranging from 0.2% to 6%, by weight, of the pharmaceutical composition, wherein the glidant comprises silicon dioxide, magnesium trisilicate, powdered cellulose, starch, talc, tribasic calcium phosphate, or a combination thereof; and a lubricant in an amount ranging from 0.2% to 0.6%, by weight, of the pharmaceutical composition, wherein the lubricant comprises magnesium stearate, calcium stearate, zinc stearate, talc, propylene glycol, polyethylene glycol (PEG), stearic acid, vegetable oil, sodium benzoate, sodium lauryl sulfate, magnesium lauryl sulfate, mineral oil polyoxyethylene monostearate, or a combination thereof, wherein the pharmaceutical composition does not comprise estrogens, wherein, when subjected to an in vitro dissolution test according to the USP XXIII Paddle Method, no more than 50% of the drospirenone initially present in the pharmaceutical composition is dissolved within 30 minutes.

7. A kit comprising one or more packaging units wherein each packaging unit comprises 21 to 28 of the unit doses of claim 6.

8. The kit of claim 7, wherein each packaging unit comprises 24 of the unit doses.

9. A method for providing contraception, increasing cycle stability, or both, the method comprising administering the unit dose of claim 6 to a subject.

10. The method of claim 9, wherein the unit dose is administered in a 28 day daily dosing regimen.

11. The unit dose of claim 1, wherein the particle form has a d.sub.90 particle size less than about 100 .mu.m, and a d.sub.10 particle size of more than about 3 .mu.m.

12. The unit dose of claim 11, wherein the particle form has a specific surface area a surface area of the particles is from about 2000 cm.sup.2/g to about 8500 cm.sub.2/g.

13. The unit dose of claim 6, wherein the particle form has a d.sub.90 particle size less than about 100 .mu.m and a d.sub.10 particle size of more than about 3 .mu.m.

14. The unit dose of claim 6, wherein the particle form has a specific surface area from about 2000 cm.sup.2/g to about 8500 cm.sub.2/g.

15. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 2.0 mg to 4.5 mg.

16. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 2.0 mg to 4.0 mg.

17. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 2.5 mg to 4.5 mg.

18. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 2.5 mg to 4.0 mg.

19. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 3.0 mg to 4.5 mg.

20. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 3.0 mg to 4.0 mg.

21. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 3.5 mg to 4.5 mg.

22. The unit dose of claim 1, wherein the amount of drospirenone present ranges from 3.0 mg to 3.5 mg.

23. The unit dose of claim 1, wherein the amount of drospirenone present is about 3.5 mg.

24. The unit dose of claim 1, wherein the amount of drospirenone present is about 4.0 mg.

25. The unit dose of claim 1, wherein the pharmaceutical composition further comprises one or more additional excipients.

26. The unit dose of claim 25, wherein the one or more additional excipients are present in an amount ranging from 0.1% to 10%, by weight, of the pharmaceutical composition.

27. The unit dose of claim 1, wherein the pharmaceutical composition comprises a coating.

28. The unit dose of claim 27, wherein the coating comprises hydroxypropylmethyl cellulose, hydroxypropyl cellulose, ethyl cellulose, or a combination thereof.

29. The unit dose of claim 28, wherein the coating comprises Opadry II.

30. The unit dose of claim 1, wherein the unit dose is a tablet.

31. The unit dose of claim 1, wherein the d.sub.50 ranges from 10 .mu.m to 40 .mu.m.

32. The unit dose of claim 1, wherein the d.sub.50 ranges from 10 .mu.m to 35 .mu.m.

33. The unit dose of claim 1, wherein the d.sub.50 ranges from 10 .mu.m to 30 .mu.m.

34. The unit dose of claim 1, wherein the d.sub.50 ranges from 15 .mu.m to 25 .mu.m.

35. The unit dose of claim 1, wherein the d.sub.10 particle size is more than about 3 .mu.m.

36. The unit dose of claim 1, wherein the d.sub.90 particle size is less than about 100 .mu.m.

37. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 2.0 mg to 4.5 mg.

38. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 2.0 mg to 4.0 mg.

39. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 2.5 mg to 4.5 mg.

40. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 2.5 mg to 4.0 mg.

41. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 3.0 mg to 4.5 mg.

42. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 3.0 mg to 4.0 mg.

43. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 3.5 mg to 4.5 mg.

44. The unit dose of claim 6, wherein the amount of drospirenone present ranges from 3.0 mg to 3.5 mg.

45. The unit dose of claim 6, wherein the amount of drospirenone present is about 3.5 mg.

46. The unit dose of claim 6, wherein the amount of drospirenone present is about 4.0 mg.

47. The unit dose of claim 6, wherein the pharmaceutical composition further comprises one or more additional excipients.

48. The unit dose of claim 47, wherein the one or more additional excipients are present in an amount ranging from 0.1% to 10%, by weight, of the pharmaceutical composition.

49. The unit dose of claim 6, wherein the pharmaceutical composition comprises a coating.

50. The unit dose of claim 49, wherein the coating comprises hydroxypropylmethyl cellulose, hydroxypropyl cellulose, ethyl cellulose, or a combination thereof.

51. The unit dose of claim 49, wherein the coating comprises Opadry II.

52. The unit dose of claim 6, wherein the unit dose is a tablet.

53. The unit dose of claim 6, wherein the d.sub.50 ranges from 10 .mu.m to 40 .mu.m.

54. The unit dose of claim 6, wherein the d.sub.50 ranges from 10.mu.m to 35 .mu.m.

55. The unit dose of claim 6, wherein the d.sub.50 ranges from 10 .mu.m to 30 .mu.m.

56. The unit dose of claim 6, wherein the d.sub.50 ranges from 15 .mu.m to 25 .mu.m.

57. The unit dose of claim 6, wherein the d.sub.10 particle size is more than about 3 .mu.m.

58. The unit dose of claim 6, wherein the d.sub.90 particle size is less than about 100 .mu.m.

59. The unit dose of claim 6, wherein the starch comprises potato starch, wheat starch, corn starch, or a combination thereof.

60. The unit dose of claim 6, wherein the gum comprises gum tragacanth, acacia gum, gelatin, or a combination thereof.

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