Details for Patent: 6,797,719

Title:	Benzothiophenes, formulations containing same, and methods
Abstract:	This invention provides compounds of formula I ##STR1## and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.
Inventor(s):	Arbuthnot; Gordon Nelson (Indianapolis, IN), Dalder; Brian Weston (West Lafayette, IN), Hartauer; Kerry John (Indianapolis, IN), Luke; Wayne Douglas (West Lafayette, IN), Stratford, Jr.; Robert Eugene (Carmel, IN)
Assignee:	Eli Lilly and Company (Indianapolis, IN)
Filing Date:	Sep 05, 2002
Application Number:	10/235,617
Claims:	1. A pharmaceutical composition comprising: a) a compound of formula I ##STR8## or a pharmaceutically acceptable salt or solvate thereof, characterized in that the compound of formula I is in particulate form, said particles having a mean particle size of less than about 25 microns, at least about 90% of said particles have a size of less than about 50 microns; b) a surfactant; and c) a water-soluble diluent. 2. The composition of claim 1 wherein the compound is non-solvated crystalline 6-hydroxy-2-(4-hydroxy-phenyl)-3-[4-(-2-piperidinoethoxy)benzoyl]benzo[b]t hiophene hydrochloride. 3. The composition of claim 2 wherein said particles have a mean particle size of between 5 and about 20 microns. 4. The composition of claim 3 wherein at least 90% of said particles have a size of less than about 35 microns. 5. The composition of claim 1 wherein the surfactant is polysorbate 80. 6. The composition of claim 2 wherein the surfactant is polysorbate 80. 7. The composition of claim 3 wherein the surfactant is polysorbate 80. 8. The composition of claim 4 wherein the surfactant is polysorbate 80. 9. The composition of claim 1 wherein the water-soluble diluent is lactose. 10. The composition of claim 2 wherein the water-soluble diluent is lactose. 11. The composition of claim 3 wherein the water-soluble diluent is lactose. 12. The composition of claim 4 wherein the water-soluble diluent is lactose. 13. The composition of claim 5 wherein the water-soluble diluent is lactose. 14. The composition of claim 6 wherein the water-soluble diluent is lactose. 15. The composition of claim 7 wherein the water-soluble diluent is lactose. 16. The composition of claim 8 wherein the water-soluble diluent is lactose. 17. The composition of claim 1 further comprising a hydrophilic binder. 18. The composition of claim 2 further comprising a hydrophilic binder. 19. The composition of claim 3 further comprising a hydrophilic binder. 20. The composition of claim 4 further comprising a hydrophilic binder. 21. The composition of claim 5 further comprising a hydrophilic binder. 22. The composition of claim 6 further comprising a hydrophilic binder. 23. The composition of claim 7 further comprising a hydrophilic binder. 24. The composition of claim 8 further comprising a hydrophilic binder. 25. The composition of claim 9 further comprising a hydrophilic binder. 26. The composition of claim 10 further comprising a hydrophilic binder. 27. The composition of claim 11 further comprising a hydrophilic binder. 28. The composition of claim 12 further comprising a hydrophilic binder. 29. The composition of claim 13 further comprising a hydrophilic binder. 30. The composition of claim 14 further comprising a hydrophilic binder. 31. The composition of claim 15 further comprising a hydrophilic binder. 32. The composition of claim 16 further comprising a hydrophilic binder. 33. The composition of claim 17 wherein the hydrophilic binder is polyvinylpyrrolidone. 34. The composition of claim 18 wherein the hydrophilic binder is polyvinylpyrrolidone. 35. The composition of claim 19 wherein the hydrophilic binder is polyvinylpyrrolidone. 36. The composition of claim 20 wherein the hydrophilic binder is polyvinylpyrrolidone. 37. The composition of claim 21 wherein the hydrophilic binder is polyvinylpyrrolidone. 38. The composition of claim 22 wherein the hydrophilic binder is polyvinylpyrrolidone. 39. The composition of claim 23 wherein the hydrophilic binder is polyvinylpyrrolidone. 40. The composition of claim 24 wherein the hydrophilic binder is polyvinylpyrrolidone. 41. The composition of claim 25 wherein the hydrophilic binder is polyvinylpyrrolidone. 42. The composition of claim 26 wherein the hydrophilic binder is polyvinylpyrrolidone. 43. The composition of claim 27 wherein the hydrophilic binder is polyvinylpyrrolidone. 44. The composition of claim 28 wherein the hydrophilic binder is polyvinylpyrrolidone. 45. The composition of claim 29 wherein the hydrophilic binder is polyvinylpyrrolidone. 46. The composition of claim 30 wherein the hydrophilic binder is polyvinylpyrrolidone. 47. The composition of claim 31 wherein the hydrophilic binder is polyvinylpyrrolidone. 48. The composition of claim 32 wherein the hydrophilic binder is polyvinylpyrrolidone. 49. The composition of claim 1 further comprising a lubricant and a disintegrant. 50. The composition of claim 2 further comprising a lubricant and a disintegrant. 51. The composition of claim 3 further comprising a lubricant and a disintegrant. 52. The composition of claim 4 further comprising a lubricant and a disintegrant. 53. The composition of claim 5 further comprising a lubricant and a disintegrant. 54. The composition of claim 18 further comprising a lubricant and a disintegrant. 55. The composition of claim 32 further comprising a lubricant and a disintegrant. 56. The composition of claim 48 further comprising a lubricant and a disintegrant. 57. The composition of claim 49 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 58. The composition of claim 50 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 59. The composition of claim 51 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 60. The composition of claim 52 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 61. The composition of claim 53 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 62. The composition of claim 54 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 63. The composition of claim 55 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 64. The composition of claim 56 wherein said lubricant is magnesium stearate or stearic acid, and said disintegrant is cross-linked polyvinylpyrrolidone. 65. The composition of claim 57 comprising the hydrochloride salt of a compound of formula I, polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 66. The composition of claim 58 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 67. The composition of claim 59 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 68. The composition of claim 60 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 69. The composition of claim 61 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 70. The composition of claim 62 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 71. The composition of claim 63 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 72. The composition of claim 64 comprising polyvinylpyrrolidone, polysorbate 80, lactose, cross-linked polyvinylpyrrolidone, and magnesium stearate. 73. The composition of claim 72 further comprising a film coating.