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Claims for Patent: 7,157,101

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Claims for Patent: 7,157,101

Title:Micronized 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, LLC (New York, NY)
Application Number:10/817,577
Patent Claims: 1. A pharmaceutical composition comprising: (a) about 25 mg to about 100 mg of particulate eplerenone having a D.sub.90 particle size of about 25 microns to about 400 microns, (b) about 0.5 to about 30 weight percent of one or more pharmaceutically acceptable disintegrants, (c) about 5 to about 99 weight percent of one or more pharmaceutically acceptable diluents, and (d) about 0.5 to about 25 weight percent of one or more pharmaceutically acceptable binding agents, wherein the composition is an immediate release composition wherein at least about 80% of the eplerenone is dissolved in vitro within about 30 minutes in 0.1N HCl at 37.degree. C., and wherein the composition substantially disintegrates within about 30 minutes when placed in a water bath maintained at a temperature of 37.degree. C..+-.2.degree. C.

2. The pharmaceutical composition according to claim 1 wherein said composition comprises eplerenone in an amount of about 25 mg.

3. The pharmaceutical composition according to claim 1 wherein said composition comprises eplerenone in an amount of about 50 mg.

4. The pharmaceutical composition according to claim 1 wherein said composition comprises eplerenone in an amount of about 100 mg.

5. The pharmaceutical composition according to claim 1 wherein at least one of the one or more diluents is selected from the group consisting of purified cellulose, microcrystalline cellulose, and alkyl celluloses and their derivatives and salts.

6. The pharmaceutical composition according to claim 1 wherein at least one of the one or more binding agents is selected from the group consisting of acacia, tragacanth, sucrose, gelatin, glucose, starch, celluloses, alginic acid, salts of alginic acid, magnesium aluminum silicate, polyethylene glycol, gums, polysaccharide acids, bentonites, polyvinylpyrrolidone, polymethacrylates, hydroxypropyl methylcellulose, hydroxypropyl cellulose, ethyl cellulose, and pregelatinized starch.

7. The pharmaceutical composition according to claim 1 wherein at least one of the one or more diluents is 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.

8. The pharmaceutical composition according to claim 1 wherein at least one of the one or more disintegrants is selected from the group consisting of starches, sodium starch glycolate, clays, celluloses, alginates, pregelatinized corn starches, crospovidone, and gums.

9. The pharmaceutical composition according to claim 1 further comprising one or more pharmaceutically acceptable wetting agents, wherein said wetting agente or wetting agents are present at about 0.1% to about 15% of the total weight of the composition.

10. The pharmaceutical composition according to claim 9 wherein said wetting agents are selected from the group consisting of oleic acid, glyceryl monostearate, sorbitan mono-oleate, sorbitan monolaurate, triethanolamine oleate, polyoxyethylene sorbitan mono-oleate, polyoxyethylene sorbitan monolaurate, sodium oleate, and sodium lauryl sulfate.

11. The pharmaceutical composition according to claim 1 further comprising one or more pharmaceutically acceptable lubricants, wherein said lubricant or lubricants are present at about 0.1% to about 10% of the total weight of the composition.

12. The pharmaceutical composition according to claim 11 wherein said lubricants are selected from the group consisting of glyceryl behenate, magnesium stearate, calcium stearate, sodium stearatee, 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, sodium stearyl fumarate and magnesium lauryl sulfate.

13. The pharmaceutical composition according to claim 1 comprising one or more pharmaceutically acceptable anti-adherents or glidants, wherein said anti-adherent or anti-adherents or glidants are present at about 0.25% to about 10% of the total weight of the composition.

14. The pharmaceutical composition according to claim 13 wherein said anti-adherents or glidants are selected from the group consisting of talc, cornstarch, DL-Leucine, sodium lauryl sulfate, and magnesium, calcium and sodium stearates.

15. The pharmaceutical composition according to claim 1 wherein at least one of the one or more binding agents is hydroxypropyl methylcellulose.

16. The pharmaceutical composition according to claim 1 wherein at least one of the one or more diluents is lactose.

17. The pharmaceutical composition according to claim 1 wherein at least one of the one or more diluents is microcrystalline cellulose.

18. The pharmaceutical composition according to claim 1 wherein at least one of the one or more disintegrants is croscarmellose sodium.

19. The pharmaceutical composition according to claim 7 comprising: lactose at about 5% to about 90% of the total weight of the composition; and microcrystalline cellulose at about 5% to about 90% of the total weight of the composition; and wherein at least one of the one or more binding agents is hydroxypropyl methylcellulose at about 0.5% to about 10% of the total weight of the composition.

20. The pharmaceutical composition according to claim 19 comprising: about 19 to about 40 weight percent of eplerenone; about 32 to about 52 weight percent of lactose; about 8 to about 28 weight percent of microcrystalline cellulose; and about 1 to about 8 weight percent of hydroxypropyl methylcellulose.

21. The pharmaceutical composition according to claim 19 comprising: about 24 to about 35 weight percent of eplerenone; about 37 to about 47 weight percent of lactose; about 13 to about 23 weight percent of microcrystalline cellulose; and about 2 to about 4 weight percent of hydroxypropyl methylcellulose; and wherein at least one of the one or more disintegrants is croscarmellose sodium at about 2% to about 6% of the total weight of the composition.

22. The pharmaceutical composition according to claim 21 comprising: about 28 to about 31 weight percent of eplerenone; about 41 to about 43 weight percent of lactose monohydrate; about 17 to about 19 weight percent of microcrystalline cellulose; about 4.5 to about 5.5 weight percent of croscarmellose sodium; and about 2.5 to about 3.5 weight percent of hydroxypropyl methylcellulose.

23. The pharmaceutical composition according to claim 22 in the form of a coated or uncoated unit dosage tablet wherein the uncoated tablet or the coated tablet prior to coating comprises: about 29.4 weight percent of eplerenone; about 42 weight percent of lactose; about 18.1 weight percent of microcrystalline cellulose; about 5 weight percent of croscarmellose sodium; about 3 weight percent of hydroxypropyl methylcellulose; about 1 weight percent of sodium lauryl sulfate; about 1 weight percent of talc; and about 0.5 weight percent of magnesium stearate.

24. The pharmaceutical composition according to claim 22 comprising: about 25 mg of eplerenone; about 34 mg to about 38 mg of lactose; about 14 mg to about 17 mg of microcrystalline cellulose; about 3 mg to about 6 mg of croscarmellose sodium; about 1 mg to about 4 mg of hydroxypropyl methylcellulose; about 0.25 mg to about 1.5 mg of sodium lauryl sulfate; about 0.25 mg to about 1.5 mg of talc; and about 0.1 mg to about 1 mg of magnesium stearate.

25. The pharmaceutical composition according to claim 22 comprising: about 50 mg of eplerenone; about 70 mg to about 73 mg of lactose; about 29 mg to about 33 mg of microcrystalline cellulose; about 6 mg to about 10 mg of croscarmellose sodium; about 4 mg to about 6 mg of hydroxypropyl methylcellulose; about 1 to about 2.5 mg of sodium lauryl sulfate; about 1 to about 2.5 mg of talc; and about 1 mg to about 1.5 mg of magnesium stearate.

26. The pharmaceutical composition according to claim 22 comprising: about 100 mg of eplerenone; about 141 mg to about 145 mg of lactose; about 60 mg to about 64 mg of microcrystalline cellulose; about 16 mg to about 18 mg of croscarmellose sodium; about 9 mg to about 11 mg of hydroxypropyl methylcellulose; about 3 mg to about 4 mg of sodium lauryl sulfate; about 3 mg to about 4 mg of talc; and about 1 mg to about 2 mg of magnesium stearate.

27. The pharmaceutical composition according to claim 1 in a unit oral dosage form.

28. The pharmaceutical composition according to claim 1, wherein said composition is in the form of a unit dosage tablet or capsule.

29. The pharmaceutical composition according to claim 1, wherein said composition is in the form of a unit dosage tablet.

30. The pharmaceutical composition according to claim 29 wherein the unit dosage tablet is a coated unit dosage tablet.

31. The pharmaceutical composition according to claim 1 in the form of an oral unit dosage tablet or capsule having a 25 mg, 50 mg or 100 mg dose of eplerenone.

32. The unit oral dosage form of the pharmaceutical composition of claim 27 wherein the composition is directly encapsulated or directly compressed into tablets.

33. The unit oral dosage form of the pharmaceutical composition of claim 27 wherein the composition is wet granulated and encapsulated or compressed into tablets.

34. The unit oral dosage form of the pharmaceutical composition of claim 27 wherein the composition is dry granulated and encapsulated or compressed into tablets.

35. A method of treating a condition or disorder where treatment with an aldosterone receptor blocker is indicated, comprising orally administering a composition according to claim 1 to a patient in need of such treatment and wherein the said condition or disorder is selected from the group consisting of heart failure, hypertension, edema associated with liver insufficiency and post-myocardial infarction.

36. The pharmaceutical composition according to claim 1, wherein said composition disintegrates within 6 minutes 16 second to 10 minutes 30 seconds when placed in a water bath maintained at a temperature of 37.degree. C. .+-.2.degree. C.

37. The pharmaceutical composition according to claim 1, wherein said composition disintegrates within about 20 minutes.

38. The pharmaceutical composition according to claim 1, wherein said composition disintegrates within about 14 minutes.
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