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Claims for Patent: 6,863,902

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Claims for Patent: 6,863,902

Title: Immediate release eplerenone compositions
Abstract:The invention relates to oral pharmaceutical compositions useful as aldosterone receptor blockers comprising the active agent micronized eplerenone in an amount of about 10 mg to about 1000 mg and one or more carrier materials.
Inventor(s): Thosar; Shilpa S. (Des Plaines, IL), Gokhale; Rajeev D. (Waukegan, IL), Tolbert; Dwain S. (Wadsworth, IL)
Assignee: G. D. Searle & Co. (Skokie, IL)
Application Number:10/289,025
Patent Claims: 1. A pharmaceutical composition comprising (a) particulate eplerenone having a D.sub.90 particle size of about 25 to about 400 microns, in an amount of about 10 mg to about 1000 mg, and (b) one or more pharmaceutically acceptable carrier materials; said composition being an immediate release composition wherein at least about 80% of said eplerenone is dissolved in vitro within about 30 minutes in 0.1N HCl at 37.degree. C.

2. The composition of claim 1 wherein the dissolution of the composition in vitro is determined using U.S.P. Apparatus II at 50 rpm in 1000 ml of 0.1N HCl.

3. The composition of claim 2 wherein the eplerenone is in an amount of about, 20 mg to about 400 mg.

4. The composition of claim 2 wherein the eplerenone is in an amount of about 25 mg to about 150 mg.

5. The composition of claim 2 wherein the eplerenone is in an amount of about 25 mg to about 100 mg.

6. The composition of claim 2 wherein the carrier materials comprise one or more materials selected from the group consisting of purified cellulose, microcrystalline cellulose, and alkylcelluloses and their derivatives and salts.

7. The composition of claim 2 wherein the carrier materials comprise one or more pharmaceutically acceptable binding agents in a total amount of about 0.5% to about 25% by weight of the composition.

8. The composition of claim 7 wherein the binding agents are selected from the group consisting of acacia, tragacanth, sucrose, gelatin, glucose, starch, celluloses, alginic acid and salts thereof, magnesium aluminum silicate, polyethylene glycol, gums, polysaccharide acids, bentonites, polyvinylpyrrolidone, polymethacrylates, hydroxypropylmethylcellulose hydroxypropylcellulose, ethylcellulose, and pregelatinized starch.

9. The composition of claim 2 wherein the carrier materials comprise one or more pharmaceutically acceptable diluents ma total amount of about 5% to about 99% by weight of the composition.

10. The composition of claim 9 wherein the diluents are selected from the group consisting of lactose, starch, mannitol, sorbitol, dextrose, microcrystalline cellulose, dibasic calcium phosphate, sucrose-based diluents, confectioner's sugar, monobasic calcium sulfate monohydrate, calcium sulfate dihydrate, calcium lactate trihydrate, dextrates, inositol, hydrolyzed cereal solids, amylose, powdered cellulose, calcium carbonate, glycine, and bentonite.

11. The composition of claim 2 wherein the carrier materials comprise one or more pharmaceutically acceptable disintegrants in a total amount of about 0.5% to about 30% by weight of the composition.

12. The composition of claim 11 wherein the disintegrants are selected from the group consisting of starches, sodium starch glycolate, clays, celluloses, alginates, pregelatinized corn starches, crospovidone, and gums.

13. The composition of claim 2 wherein the carrier materials comprise one or more pharmaceutically acceptable wetting agents in a total amount of about 0.1% to about 15% by weight of the composition.

14. The composition of claim 13 wherein the wetting agents are selected from the group consisting of oleic acid, glyceryl monostearate, sorbitan monooleate, sorbitan monolaurate, triethanolamine oleate, polyoxyethylene sorbitan monooleate, polyoxyethylene sorbitan monolaurate, sodium oleate, and sodium lauryl sulfate.

15. The composition of claim 2 wherein the carrier materials comprise one or more pharmaceutically acceptable lubricants in a total amount of about 0.1% to about 10% by weight of the composition.

16. The composition of claim 15 wherein the lubricants are selected from the group consisting of glyceryl, behapate, magnesium, calcium and sodium stearates, stearic acid, hydrogenated vegetable oils, talc, waxes, Stearowet, boric acid, sodium benzoate, sodium acetate, sodium chloride, DL-leucine, polyethylene glycols, sodium oleate, sodium lauryl sulfate, and magnesium lauryl sulfate.

17. The composition of claim 2 wherein the carrier materials comprise one or more pharmaceutically acceptable anti-adherents or glidants in a total amount of about 0.25% to about 10% by weight of the composition.

18. The composition of claim 17 wherein the anti-adherents or glidants are selected from the group consisting of talc, corn starch, DL-leucine, sodium lauryl sulfate, and magnesium, calcium and sodium stearates.

19. The composition of claim 2 wherein the eplerenone is present in an amount of about 1% to about 90% by weight of the composition.

20. The composition of claim 2 wherein the carrier materials comprise one or more materials selected from the group consisting of diluents, binding agents, disintegrants, wetting agents, lubricants, anti-adherents and glidants.

21. The composition of claim 2 wherein the carrier materials comprise hydroxypropylmethylcellulose.

22. The composition of claim 2 wherein the carrier materials comprise lactose.

23. The composition of claim 2 wherein the carrier materials comprise microcrystalline cellulose.

24. The composition of claim 2 wherein the carrier materials comprise croscarmellose sodium.

25. The composition of claim 2 wherein the carrier materials comprise (a) lactose in an amount of about 5% to about 90%; (b) microcrystalline cellulose in an amount of about 5% to about 90%; and (c) hydroxypropylmethylcellulose in an amount of about 0.5% to about 10%; all by weight of the composition.

26. The composition of claim 25 wherein the eplerenone is in an amount of about 1% to about 90% by weight of the composition.

27. The composition of claim 26 that comprises: (a) about 19% to about 40% by weight of eplerenone; (b) about 32% to about 52% by weight of lactose; (c) about 8% to about 28% by weight of microcrystalline cellulose; and (d) about 1% to about 8% by weight of hydroxypropylmethylcellulose.

28. The composition of claim 26 that comprises: (a) about 24% to about 35% by weight of eplerenone; (b) about 37% to about 47% by weight of lactose; (c) about 13% to about 23% by weight of microcrystalline cellulose; and (d) about 2% to about 4% by weight of hydroxypropylmethylcellulose; and that further comprises: (e) about 2% to about 6% by weight of croscarmellose sodium.

29. The composition of claim 28 that comprises: (a) about 28% to about 31% by weight of eplerenone; (b) about 41% to about 43% by weight of lactose monohydrate; (c) about 17% to about 19% by weight of microcrystalline cellulose; (d) about 2.5% to about 3.5% by weight of hydroxypropylmethylcellulose; and (e) about 4.5% to about 5.5% by weight of croscarmellose sodium.

30. The composition of claim 29 that is a coated or uncoated unit dosage tablet, and that prior to coating comprises: (a) about 29.4% by weight of eplerenone; (b) about; 42% by weight of lactose; (c) about 18.1% by weight of microcrystalline cellulose; (d) about 3% by weight of hydroxypropylmethylcellulose; (e) about 5% by weight of croscarmellose sodium; (f) about 1% by weight of talc; and (g) about 0.5% by weight of magnesium stearate.

31. The composition of claim 2 wherein the eplerenone is in an amount of about 23 mg to about 27 mg, and wherein the carrier materials comprise: (a) about 34 mg to about 38 mg lactose; (b) about 14 mg to about 17 mg microcrystalline cellulose; (c) about 1 mg to about 4 mg hydroxypropylmethylcellulose; (d) about 3 mg to about 6 mg croscarmellose sodium; (e) about 0.25 mg to about 1.5 mg sodium lauryl sulfate; (f) about 0.25 mg to about 1.5 mg talc; and (g) about 0.1 mg to about 1 mg magnesium stearate.

32. The composition of claim 2 wherein the eplerenone is in an amount of about 48 mg to about 52 mg, and wherein the carrier materials comprise: (a) about 70 mg to about 73 mg lactose; (b) about 29 mg to about 33 mg microcrystalline cellulose; (c) about 4 mg to about 6 mg hydroxypropylmethylcellulose; (d) about 6 mg to about 10 mg croscarmellose sodium; (e) about 1 mg to about 2.5 mg sodium lauryl sulfate; (f) about 1 mg to about 2.5 mg talc; and (g) about 1 mg to about 1.5 mg magnesium stearate.

33. The composition of claim 2 wherein the eplerenone is in an amount of about 98 mg to about 102 mg, and wherein the carrier materials comprise: (a) about 141 mg to about 145 mg lactose; (b) about 60 mg to about 64 mg microcrystalline cellulose; (c) about 9 mg to about 11 mg hydroxypropylmethylcellulose; (d) about 16 mg to about 18 mg croscarmellose sodium; (e) about 3 mg to about 4 mg sodium lauryl sulfate; (f) about 3 mg to about 4 mg talc; and (g) about 1 mg to about 2 mg magnesium stearate.

34. The composition of claim 2 that is in a unit oral dosage form.

35. The composition of claim 2 that is in a form of a unit dosage tablet or capsule.

36. The composition of claim 2 that is in a form of a unit dosage tablet.

37. The composition of claim 36 wherein the tablet is coated.

38. The composition of claim 2 that is in a form of a unit dosage tablet or capsule having a 25 mg dose of eplerenone.

39. The composition of claim 2 that is in a form of a unit dosage tablet or capsule having a 50 mg dose of eplerenone.

40. The composition of claim 2 that is in a form of a unit dosage tablet or capsule having a 100 mg dose of eplerenone.

41. The composition of claim 2 that is suitable for once or twice a day oral administration as an aldosterone receptor blocker.

42. The composition of claim 2 that provides a therapeutic effect as an aldosterone receptor blocker in a human subject over an interval of about 12 to about 24 hours after ingestion of the composition.

43. The composition of claim 2 that provides a therapeutic effect as an aldosterone receptor blocker in a human subject over an interval of about 24 hours after ingestion.

44. The composition of claim 34 wherein said unit dosage form is a capsule prepared by direct encapsulation or a tablet prepared by direct compression.

45. The composition of claim 34 wherein said unit dosage form is prepared by wet granulation followed by encapsulation to form a capsule or compression to form a tablet.

46. The composition of claim 34 wherein said unit dosage form is prepared by dry granulation followed by encapsulation to form a capsule or compression to form a tablet.

47. The composition of claim 2 wherein the eplerenone has a D.sub.90 particle size of about 25 to about 200 microns.

48. The composition of claim 2 wherein the eplerenone has a D.sub.90 particle size of about 25 to about 150 microns.

49. The composition of claim 2 wherein the eplerenone has a D.sub.90 particle size of about 30 to about 110 microns.

50. The composition of claim 2 wherein the eplerenone has a D.sub.90 particle size of about 30 to about 50 microns.

51. The composition of claim 2 wherein the eplerenone has a D.sub.90 particle size of about 50 to about 150 microns.

52. The composition of claim 2 wherein the eplerenone has a D.sub.90 particle size of about 75 to about 125 microns.

53. The composition of claim 2 wherein ingestion of the composition by a human subject causes an average increase of at least about 10% in blood serum renin concentration in the subject over an interval of about 12 to about 24 hours after said ingestion.

54. The composition of claim 2 wherein ingestion of the composition by a human subject causes an average increase of at least about 50% in blood serum aldosterone concentration in the subject over an interval of about 12 to about 24 hours after said ingestion.

55. The composition of claim 2 wherein ingestion of the composition by a human subject causes an average decrease of at least about 5% in diastolic blood pressure in the subject over an interval of about 12 to about 24 hours after said ingestion.

56. A method of treating a condition or disorder where treatment with an aldosterone receptor blocker is indicated, the method comprising orally administering the composition of claim 1 to a patient in need of such treatment.

57. The method of claim 56 wherein the condition or disorder is heart failure.

58. The method of claim 56 wherein the condition or disorder is hypertension.

59. The method of claim 56 wherein the condition or disorder is edema associated with liver insufficiency.

60. The method of claim 56 wherein the condition or disorder is post-myocardial infarction.
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