| 摘要 |
1. A compound of formula I and pharmaceutically acceptable salts and solvates thereof, characterized in that the compound is in particulate form, said particles having a mean particle size of less than about 25 microns. 2. The compound of claim 1 wherein said particles have a mean particle size of between about 5 and about 20 microns. 3. The compound of claim 1 or 2 wherein at least about 90% of said particles have a size of less than about 50 microns. 4. The compound of claim 3 wherein at least 90% of said particles have a size of less than about 35 microns. 5. The compound of any of claims 1 to 4 wherein the compound of formula I is raloxifene hydrochloride. 6.The compound of claim 5 which is the non-solvated crystalline hydrochloride having substantially the following X-ray diffraction pattern obtained with copper radiation: d-line spacing (Angstroms) I/I o (x100) 13,3864 71,31 9,3598 33,16 8,4625 2,08 7,3888 7,57 6,9907 5,80 6,6346 51,04 6,1717 29,57 5,9975 5,67 5,9135 9,87 5,6467 38,47 5,4773 10,54 5,2994 4,74 4,8680 4,03 4,7910 5,98 4,6614 57,50 4,5052 5,75 4,3701 9,03 4,2516 69,99 4,2059 57,64 4,1740 65,07 4,0819 12,44 3,9673 22,53 3,9318 100,00 3,8775 9,07 3,7096 33,38 3,6561 21,65 3,5576 3,36 3,5037 7,97 3,4522 18,02 3,4138 4,65 3,2738 10,23 3,1857 8,90 3,1333 6,24 3,0831 9,43 3,0025 12,13 2,9437 4,96 2,8642 7,70 2,7904 11,95 2,7246 3,05 2,6652 3,32 2,5882 7,30 13,3864 71,31 9,3598 33,16 8,4625 2,08 7,3888 7,57 6,9907 5,80 6,6346 51,04 6,1717 29,57 5,9975 5,67 5,9135 9,87 5,6467 38,47 5,4773 10,54 5,2994 4,74 4,8680 4,03 4,7910 5,98 4,6614 57,50 4,5052 5,75 4,3701 9,03 4,2516 69,99 4,2059 57,64 4,1740 65,07 4,0819 12,44 3,9673 22,53 3,9318 100,00 3,8775 9,07 3,7096 33,38 3,6561 21,65 3,5576 3,36 3,5037 7,97 3,4522 18,02 3,4138 4,65 3,2738 10,23 3,1857 8,90 3,1333 6,24 3,0831 9,43 3,0025 12,13 2,9437 4,96 2,8642 7,70 2,7904 11,95 2,7246 3,05 2,6652 3,32 2,5882 7,30 7. A pharmaceutical composition comprising or formulated using a compound as claimed in any one of claims 1 to 5 and one or more pharmaceutically acceptable carriers, diluents, or excipients. 8. A method of enhancing bioavailability in the treatment of osteoporosis with raloxifene comprising administering an effective amount of a compound of formula I as claimed in any one of claims 1 to 6, or a pharmaceutical composition as claimed in claims 7, to a person in need thereof. 9. A method of enhancing bioavailability in lowering serum lipid levels with raloxifene comprising administering an effective amount of a compound of formula I as claimed in any one of claims 1 to 6, or a pharmaceutical composition as claimed in claims 7, to a person in need thereof. 10. A method for enhancing bioavailability in preventing breast cancer with raloxifene comprising administering an effective amount of a compound of formula I as claimed in any one of claims 1 to 6, or a pharmaceutical composition as claimed in claims 7, to a person in need thereof. 11. An article of manufacture comprising packaging material containing a pharmaceutical composition, said packaging material further containing labeling indicating said pharmaceutical composition is useful for inhibiting a human pathology, said pharmaceutical composition comprising or formulated using a compound as claimed in any of claims 1-6. |
