Oral formulations of ospemifene
View Patent ↗This invention relates to a liquid or semisolid oral drug formulation comprising 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, in combination with a pharmaceutically acceptable carrier.
1. A liquid, oral drug formulation comprising 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, in combination with a pharmaceutically acceptable carrier comprising a mixture of ethanol, polyethylene glycol, and propyleneglycol.
2. The formulation of claim 1 , wherein the compound is ospemifene.
3. The formulation according to claim 2 further comprising a bile-flow promoting agent selected from the group consisting of (a) a pharmaceutically acceptable carrier comprising a digestible lipid selected from the group consisting of a triglyceride, a diglyceride, a fatty acid, or a phospholipid; and (b) a cholane derivative and a pharmaceutically acceptable carrier.
4. The drug formulation according to claim 3 wherein the formulation is a suspension.
5. The drug formulation according to claim 2 wherein the formulation is an emulsion.
6. The drug formulation according to claim 2 wherein the formulation is a microemulsion or nanoemulsion.
7. The drug formulation according to claim 3 wherein the formulation is a syrup.
8. The drug formulation according to claim 2 wherein the formulation is packed into a unit dosage form.
9. The drug formulation according to claim 8 wherein the dosage form is the formulation encapsulated in a soft gel capsule.
10. The drug formulation according to claim 2 wherein the formulation is a solution.
11. The drug formulation according to claim 10 wherein the formulation is packed into a unit dosage form.
12. The drug formulation according to claim 11 wherein the dosage form is the formulation encapsulated in a soft capsule.
13. The drug formulation according to claim 10 wherein the dosage amount is from 30 to 90 mg/day.
14. The drug formulation according to claim 11 wherein the dosage amount is 60 mg.
15. The drug formulation according to claim 2 wherein the dosage amount is from 30 to 90 mg/day.
16. The drug formulation according to claim 15 wherein the dosage amount is 60 mg.
17. The drug formulation according to claim 3 wherein the bile flow promoting agent is a cholane derivative.
18. The drug formulation according to claim 3 wherein the bile flow promoting agent is a digestible lipid.
19. The drug formulation according to claim 2 further comprising ethanol.
20. The drug formulation according to claim 10 further comprising ethanol.
21. A liquid, oral drug formulation consisting essentially 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, in combination with a pharmaceutically acceptable carrier comprising a mixture of ethanol, polyethylene glycol, and propyleneglycol.
22. The formulation of claim 21 wherein the compound is ospemifene.
23. The drug formulation according to claim 22 wherein the formulation is packed into a unit dosage form.