Method for enhancing the bioavailability of ospemifene
View Patent ↗This invention relates to a method for enhancing the bioavailability of a therapeutically active compound of the formula (I) 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.
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.