Claims for Patent: 9,855,224

Summary for Patent: 9,855,224

Title:	Method for enhancing the bioavailability of ospemifene
Abstract:	This invention relates to a method for enhancing the bioavailability of a therapeutically active compound of the formula (I) ##STR00001## or a geometric isomer, a stereoisomer, a pharmaceutically acceptable salt, an ester thereof or a metabolite thereof, wherein said compound is administered orally to the individual in connection with the intake of food.
Inventor(s):	Anttila; Markku (Turku, FI)
Assignee:	HORMOS MEDICAL CORPORATION (FI)
Application Number:	14/971,252
Patent Claims:	1. A method for treating one or more vaginal symptoms of urogenital atrophy due to menopause with ospemifene, the improvement comprising increasing ospemifene absorption by about 2-3 fold by orally administering the ospemifene in connection with the intake of a meal, wherein the increase is as compared to the administration of ospemifene in a fasted state. 2. The method of claim 1, wherein the meal comprises a high-fat, high-calorie meal. 3. The method of claim 1, wherein the meal comprises a low-fat, low-calorie meal. 4. The method of claim 1, wherein peak ospemifene mean serum concentration is reached in about 2-3 hours after administration. 5. The method of claim 4, wherein the increase in peak mean serum concentration is between 1 and 4 times greater as compared to said administration in a fasted state. 6. The method of claim 1, wherein the improvement further comprises instructing a patient that ospemifene should be taken with food. 7. A method for treating one or more vaginal symptoms of urogenital atrophy due to menopause, comprising increasing the peak mean serum concentration of ospemifene by orally administering ospemifene in connection with a meal, wherein the increase in peak mean serum concentration of ospemifene is as compared to the administration in a fasted state. 8. The method of claim 7, wherein the increase is between 1 and 4 times greater. 9. The method of claim 7, wherein the meal comprises a high-fat, high-calorie meal. 10. The method of claim 7, wherein the meal comprises a low-fat, low-calorie meal. 11. The method of claim 7, wherein the peak ospemifene mean serum concentration is reached in about 2-3 hours after administration. 12. The method of claim 11, wherein ospemifene absorption increases by about 2-3 fold. 13. The method of claim 7, further comprising instructing a patient that ospemifene should be taken with food. 14. A method of treating one or more vaginal symptoms of urogenital atrophy due to menopause, comprising orally administering a therapeutically effective amount of ospemifene in connection with a meal wherein the absorption of ospemifene is increased by about 2-3 fold, wherein the increase is as compared to the administration of ospemifene in a fasted state. 15. The method of claim 14, wherein the meal comprises a high-fat, high-calorie meal. 16. The method of claim 14, wherein the meal comprises a low-fat, low-calorie meal. 17. The method of claim 14, wherein the peak ospemifene mean serum concentration is reached in about 2-3 hours after administration. 18. The method of claim 17, wherein the increase in peak mean serum concentration is about 1-4 times greater. 19. The method of claim 14, further comprising instructing a patient that ospemifene should be taken with food. 20. A method for enhancing the absorption of orally administered ospemifene for the treatment of one or more symptoms of menopause, comprising administering said ospemifene in connection with the intake of a meal, thereby increasing the absorption of ospemifene by about 2-3 fold, wherein the increase is as compared to the administration of ospemifene in a fasted state. 21. The method of claim 20, wherein the meal comprises a high-fat, high-calorie meal. 22. The method of claim 20, wherein the meal comprises a low-fat, low-calorie meal. 23. The method of claim 20, wherein the peak ospemifene mean serum concentration is reached in about 2-3 hours after administration. 24. The method of claim 23, wherein the increase in peak mean serum concentration is about 1-4 times greater. 25. The method of claim 20, further comprising instructing a patient that ospemifene should be taken with food. 26. A method for increasing the bioavailability of orally administered ospemifene, comprising orally administering ospemifene in connection with a meal, thereby increasing the peak mean serum concentration of ospemifene as compared to administration in a fasted state. 27. The method of claim 26, wherein the increase is between 1 and 4 times greater. 28. The method of claim 26, wherein the meal comprises a high-fat, high-calorie meal. 29. The method of claim 26, wherein the meal comprises a low-fat, low-calorie meal. 30. The method of claim 26, wherein the peak mean serum concentration is reached in about 2-3 hours after administration. 31. The method of claim 30, wherein ospemifene absorption increases by about 2-3 fold. 32. The method of claim 26, further comprising instructing a patient that ospemifene should be taken with food.