USRE47316EExpiredUtility

Oral formulations of ospemifene

38
Assignee: HORMOS MEDICAL LTDPriority: May 4, 2004Filed: Jun 23, 2016Granted: Mar 26, 2019
Est. expiryMay 4, 2024(expired)· nominal 20-yr term from priority
Inventors:Veli-Matti LehtolaMarkku Anttila
A61P 9/10A61P 43/00A61P 35/00A61P 31/04A61P 29/00A61P 15/02A61P 15/08A61P 19/10A61P 15/12A61P 13/02A61K 9/1075A61K 31/085A61K 9/48A61K 9/107A61K 9/10A61K 9/08A61K 9/20A61K 9/4825A61K 31/075A61K 47/10B82Y 5/00
38
PatentIndex Score
0
Cited by
84
References
47
Claims

Abstract

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.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       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, ospemifene 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  1 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  1 wherein the formulation is an emulsion. 
     
     
       6. The drug formulation according to claim  2  1 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  1 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  1 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  1 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  1 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 ospemifene and 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  21 wherein the formulation is packed into a unit dosage form. 
     
     
       24. A method of treating a climacteric disorder in a postmenopausal woman, comprising administering a liquid formulation to the postmenopausal woman, the liquid formulation comprising:
 ospemifene;   and a pharmaceutically acceptable, liquid carrier.   
     
     
       25. The method of claim 24, wherein the formulation is an emulsion. 
     
     
       26. The method of claim 24, wherein the formulation is packed into a unit dosage form. 
     
     
       27. The method of claim 24, wherein the pharmaceutically acceptable liquid carrier is a digestible lipid. 
     
     
       28. The method of claim 27, wherein the digestible lipid is selected from the group consisting of a triglyceride, a diglyceride, a fatty acid, or a phospholipid. 
     
     
       29. The method of claim 24, wherein the liquid formulation further comprises a surfactant. 
     
     
       30. The method of claim 24, wherein the climacteric disorder is selected from the group consisting of vaginal dryness and sexual dysfunction. 
     
     
       31. The method of claim 30, wherein the climacteric disorder is vaginal dryness. 
     
     
       32. The method of claim 30, wherein the climacteric disorder is sexual dysfunction. 
     
     
       33. The method of claim 24, wherein the amount of ospemifene present is between 30 to 90 mg. 
     
     
       34. A liquid, oral drug formulation comprising ospemifene and a pharmaceutically acceptable, liquid carrier. 
     
     
       35. The formulation of claim 34, wherein the pharmaceutically acceptable carrier is a digestible lipid. 
     
     
       36. The formulation of claim 35, wherein the formulation is a suspension. 
     
     
       37. The formulation of claim 34, wherein the formulation is an emulsion. 
     
     
       38. The formulation of claim 34, wherein the formulation is a microemulsion or nanoemulsion. 
     
     
       39. The formulation of claim 35, wherein the digestible lipid is selected from the group consisting of a triglyceride, a diglyceride, a fatty acid, or a phospholipid. 
     
     
       40. The formulation of claim 34, wherein the formulation is packed into a unit dosage form. 
     
     
       41. The formulation of claim 34, wherein the formulation is encapsulated in a soft gel capsule. 
     
     
       42. The formulation of claim 34, wherein the amount ospemifene is from 30 to 90 mg. 
     
     
       43. The formulation of claim 34, wherein the amount of ospemifene is higher than 25 mg. 
     
     
       44. The formulation of claim 35, further comprising a bile flow promoting agent. 
     
     
       45. The formulation of claim 39, wherein the bile flow promoting agent is a cholane derivative. 
     
     
       46. The formulation of claim 34, wherein the pharmaceutically acceptable carrier comprises a mixture of ethanol, polyethylene glycol, and propyleneglycol. 
     
     
       47. The formulation of claim 34, further comprising a surfactant.

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