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Claims for Patent: 7,182,958

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Claims for Patent: 7,182,958

Title:.beta.-carboline pharmaceutical compositions
Abstract:Formulations containing a PDE5 inhibitor, a water-soluble diluent, a lubricant, a hydrophilic binder, a disintegrant, and optional microcrystalline cellulose and/or a wetting agent, and their use in treating sexual dysfunction, are disclosed.
Inventor(s): Oren; Peter L. (Fishers, IN), Anderson; Neil R. (West Lafayette, IN), Kral; Martha A. (Indianapolis, IN)
Assignee: Lilly Icos LLC. (Wilmington, DE)
Application Number:10/031,464
Patent Claims: 1. A pharmaceutical formulation comprising an active compound having the structural formula ##STR00002## wherein said compound is provided as free drug comprising particles wherein at least 90% of the particles of the said compound have a particle size of less than about 40 microns; about 50% to about 85%, by weight, of a water-soluble diluent; a lubricant; a hydrophilic binder selected from the group consisting of a cellulose derivative, povidone, and a mixture thereof; and a disintegrant selected from the group consisting of croscarmellose sodium, crospovidone, and a mixture thereof.

2. The formulation of claim 1 further comprising microcrystalline cellulose.

3. The formulation of claim 1 further comprising a wetting agent.

4. The formulation of claim 1 wherein the active compound is present in an amount of about 0.5% to about 10% by weight.

5. The formulation of claim 1 wherein the water-soluble diluent is selected from the group consisting of a sugar, a polysaccharide, a polyol, a cyclodextrin, and mixtures thereof.

6. The formulation of claim 1 wherein the water-soluble diluent is selected from the group consisting of lactose, sucrose, dextrose, a dextrate, a maltodextrin, mannitol, xylitol, sorbitol, a cyclodextrin, and mixtures thereof.

7. The formulation of claim 1 wherein the lubricant is present in an amount of about 0.25% to about 2% by weight.

8. The formulation of claim 1 wherein the lubricant is selected from the group consisting of talc, magnesium stearate, calcium stearate, stearic acid, colloidal silicon dioxide, calcium silicate, a starch, mineral oil, a wax, glyceryl behenate, a polyethylene glycol, sodium benzoate, sodium acetate, sodium stearyl fumarate, hydrogenated vegetable oils, and mixtures thereof.

9. The formulation of claim 1 wherein the hydrophilic binder is present in an amount of about 1% to about 5% by weight.

10. The formulation of claim 1 wherein the cellulose derivative is selected from the group consisting of hydroxypropylcellulose, hydroxypropyl methylcellulose, and mixtures thereof.

11. The formulation of claim 1 wherein the disintegrant is present in an amount of about 3% to about 10% by weight.

12. The formulation of claim 2 wherein the microcrystalline cellulose is present in an amount of about 5% to about 40% by weight.

13. The formulation of claim 3 wherein the wetting agent is present in an amount of 0.1% to about 5% by weight.

14. The formulation of claim 13 wherein the wetting agent is selected from the group consisting of sodium lauryl sulfate, docusate sodium, ethoxylated castor oil, a polyglycolyzed glyceride, an acetylated monoglyceride, a sorbitan fatty acid ester, a poloxamer, a polyoxyethylene sorbitan fatty acid ester, a polyoxyethylene, a monoglyceride and ethoxylated derivatives thereof, a diglyceride and ethoxylated derivatives thereof, and mixtures thereof.

15. The formulation of claim 14 wherein the wetting agent is selected from the group consisting of sodium lauryl sulfate, polysorbate 80, and a mixture thereof.

16. The formulation of claim 1 wherein the active compound is provided as particles of a free drug wherein at least 90% of the particles have a particle size less than about 10 microns.

17. The formulation of claim 1 comprising: (a) about 1% to about 4% by weight of the active compound; (b) about 50% to about 75% by weight lactose; (c) about 0.25% to about 2% by weight magnesium stearate; (d) about 1% to about 5% by weight hydroxypropyl cellulose; and (e) about 3% to about 10% by weight croscarmellose sodium.

18. The formulation of claim 16 further comprising about 5% to about 40% by weight microcrystalline cellulose.

19. The formulation of claim 16 further comprising about 0.1% to about 5% by weight sodium lauryl sulfate.

20. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 1 to about 20 mg per tablet.

21. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 5 to about 15 mg per tablet.

22. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 5 mg per tablet.

23. A capsule comprising a hard shell encasing the formulation of claim 1 as dry, free-flowing particles, wherein the active compound is present in an amount of about 1 to about 20 mg per capsule.

24. The formulation of claim 1 wherein the active compound is provided as particles of a free drug wherein at least 90% of the particles have a particle size less than about 30 microns.

25. The formulation of claim 1 wherein the active compound is provided as particles of a free drug wherein at least 90% of the particles have a particle size less than about 25 microns.

26. The formulation of claim 1 wherein the active compound is provided as particles of a free drug wherein at least 90% of the particles have a particle size less than about 15 microns.

27. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 10 mg per tablet.

28. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 1 to about 5 mg per tablet.

29. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 2.5 mg per tablet.

30. A tablet comprising the formulation of claim 1 wherein the active compound is present in an amount of about 20 mg per tablet.

31. A method of treating sexual dysfunction in a patient in need thereof comprising administering to the patient an effective amount of a formulation or a tablet according to of any one of claims 1 through 4, 5 through 15, 16 through 23, or 28 through 30.

32. The method of claim 31 wherein the sexual dysfunction is male erectile dysfunction.
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