Claims
- 1. An inclusion complex between cyclodextrin and drospirenone.
- 2. The inclusion complex according to claim 1, wherein the cyclodextrin is selected from the group consisting of α-cyclodextrin, β-cyclodextrin, γ-cyclodextrin and derivatives thereof.
- 3. The inclusion complex according to claim 2, wherein the cyclodextrin is β-cyclodextrin or γ-cyclodextrin.
- 4. The inclusion complex according to claim 3, wherein the cyclodextrin is β-cyclodextrin.
- 5. The inclusion complex according to claim 1, wherein the inclusion complex between drospirenone and the cyclodextrin is in a molar ratio, respectively, selected from the group consisting of 1:1, 2:1, 3:1, 3:2, 1:2, 2:2, 2:3 or 1:3.
- 6. The inclusion complex according to claim 5, wherein the ratio is 1:1, 2:1 or 1:2.
- 7. The inclusion complex according to claim 1 further comprising one or more therapeutically active substances.
- 8. A method for producing an inclusion complex of claim 1 comprising combining cyclodextrin and drospirenone at a molar ratio of, respectively, from 0.3:1 to 20:1.
- 9. The method of claim 8, wherein the ratio is 1:1, 2:1, 3:1, 4:1 or 5:1.
- 10. The method of claim 8, wherein the ratio is 2:1 or 3:1.
- 11. The method according to claim 8, comprising the combining of a solution of drospirenone with a solution of cyclodextrin.
- 12. The method according to claim 8, comprising the combining of solid drospirenone with a solution of cyclodextrin.
- 13. The method according to claim 8, wherein the cyclodextrin is in solution comprising a solvent selected from the group consisting of water, ethanol, acetone, acetonitrile, methanol, DMSO, pyridine or combinations thereof.
- 14. The method of claim 13, wherein the solution comprises water.
- 15. The method according to 8, wherein the drospirenone is in solution comprising a solvent selected from the group consisting of water, ethanol, acetone, acetonitrile, methanol, DMSO, pyridine or combinations thereof.
- 16. The method of claim 15, wherein the solution comprises water, ethanol or both.
- 17. The method according to claim 8 comprising;
dissolving cyclodextrin in water, optionally with heating, to form a cyclodextrin solution; dissolving drospirenone in a solvent selected from the group consisting of water and ethanol or mixtures thereof, optionally with heating, to form a drospirenone solution; combining the cyclodextrin solution and the drospirenone solution to form a combined solution; stirring the combined solution; filtering the resultant precipitate; washing the precipitate with a solvent selected from the group consisting of water, ethanol, ether and acetone, preferably wherein the solvent is cooled to below 25° C.; optionally suspending the resultant solid in a solvent and washing the suspended material with a solvent selected from the group consisting of water, ethanol, ether and acetone; removing substantially all of the solvent from the resultant or suspended material.
- 18. The method according to claim 17, wherein the removing of solvent is by spray drying.
- 19. The method according to claim 17, wherein the removing of solvent is by lyophilization.
- 20. The method according to claim 8 further comprising combining a therapeutically active substance to a combined solution of drospirenone, to a drospirenone solution, or to a cyclodextrin solution.
- 21. A method for improving the solubility of drospirenone in water comprising complexing drospirenone with cyclodextrin to form an inclusion complex.
- 22. A pharmaceutical composition comprising an inclusion complex of drospirenone and cyclodextrin as defined by claim 1 together with one or more pharmaceutically acceptable carriers or excipients.
- 23. The pharmaceutical composition according to claim 22 adapted to be administered by oral, parenteral, mucosal, topical, vaginal, subcutaneous or nasal administration.
- 24. The pharmaceutical composition according to claim 22, wherein the amount of drospirenone is from approximately 0.1 mg to 10 mg.
- 25. The pharmaceutical composition according to claim 22 further comprising one or more therapeutically active substances.
- 26. Use of the inclusion complex as defined by claim 1 as a medicament.
- 27. A method for female contraception comprising administering an inclusion complex as defined by claim 1 to a female.
- 28. A method for treating menopausal symptoms comprising administering an inclusion complex as defined by claim 1 to a female.
Priority Claims (1)
Number |
Date |
Country |
Kind |
00610134.9 |
Dec 2000 |
EP |
|
Parent Case Info
[0001] This application claims priority to U.S. Provisional Application No. 60/256,483, filed Dec. 20, 2000.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60256483 |
Dec 2000 |
US |
Continuations (1)
|
Number |
Date |
Country |
Parent |
10022846 |
Dec 2001 |
US |
Child |
10464453 |
Jun 2003 |
US |