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1. WO2004101561 - SELS DE PIOGLITAZONE TELS QUE LE SULFATE DE PIOGLITAZONE, ET LEURS COMPOSITIONS PHARMACEUTIQUES ET LEURS PROCEDES D'UTILISATION

Note: Texte fondé sur des processus automatiques de reconnaissance optique de caractères. Seule la version PDF a une valeur juridique

[ EN ]

WHAT IS CLAIMED IS:

1. A pioglitazone sulfate.
2. The pioglitazone sulfate according to claim 1, in a solid state.
3. The pioglitazone sulfate according to claims 1 or 2, in a crystalline state.
4. The pioglitazone sulfate according to any of the claims 1-3, having a molar ratio of pioglitazone moiety to sulfuric acid moiety of about 1:1.
5. A pharmaceutical composition, comprising a pioglitazone sulfate according to any of the preceding claims and at least one pharmaceutically acceptable excipient.
6. The composition according to claim 5, wherein said pharmaceutically acceptable excipient is a liquid carrier.
7. The composition according to claim 6, wherein said pioglitazone sulfate is dissolved in said liquid carrier.
8. The composition according to claims 6 or 7, wherein said liquid carrier is comprised of at least 50% water.
9. The composition according to claims 7 or 8, wherein said composition is an aqueous solution of pioglitazone sulfate.
10. The composition according to claim 9, which further comprises a solution stabilizer.

11. The composition according to claim 10, wherein said solution stabilizer is a polymer.

12. The composition according to claim 11, wherein said polymer is dissolved in said solution.
13. The composition according to claims 11 or 12, wherein said polymer is selected from the group consisting of hydroxypropylmethylcellulose, polyvinylpyrrolidone, and cyclodextrins.

14. The composition according to claim 13, wherein said polymer is
hydroxypropylmethylcellulose.
15. The composition according to claim 10, wherein said solution stabilizer is a crown- ether.
16. The composition according to any of the claims 10 to 15, wherein said solution
stabilizer is contained in a concentration within the range from 1 to 500 mg/ml of said composition.
17. The composition according to any of the claims 5-16, wherein said pioglitazone
sulfate is contained in a concentration within the range from 1 to 10 mg/ml of said composition.
18. The composition according to claim 5, wherein said pharmaceutically acceptable excipient is a solid binder, carrier, or diluent.
19. The composition according to claim 18, wherein said composition is a solid oral dosage form.
20. A process of treating a hypoglycemia disorder, which comprises:
administering an effective amount of said pharmaceutical composition according to any of the claims 5-19 to a patient in need of such treatment.
21. A process, which comprises reacting pioglitazone or a salt thereof, other than a
pioglitazone sulfate, with sulfuric acid in a solvent to form pioglitazone sulfate.
22. The process according to claims 21 or 22, wherein said solvent comprises methanol.

23. The process according to claim 21, which further comprises precipitating said
pioglitazone sulfate.
24. The process according to claims 23, wherein said precipitating comprises contacting said solvent containing pioglitazone sulfate with a contrasolvent.

25. The process according to claim 24, wherein said contrasolvent is an ether, an aliphatic hydrocarbon, or a combination thereof.
26. A process, which comprises contacting a pioglitazone salt with sufficient water for a sufficient time to precipitate solid pioglitazone base therefrom.
27. The process according to claim 26, wherein said water does not contain a neutralizing agent.
28. The process according to claim 26 or 27 wherein said pioglitazone salt is dissolved in a solvent when subjected to said contacting step.
29. A pioglitazone compound obtainable according to any of the preceding claims 21-28.

30. Use of a substance according to any of the claims 1-4, 29 for the production of a
medicament for a therapeutic application, particularly a hypoglycemia disorder.
31. Use of a composition according to any of the claims 5- 19 for the production of a
medicament for a therapeutic application, particularly a hypoglycemia disorder.