Claims
- 1. Bicifadine hydrochloride as solid crystals having polymorph form B.
- 2. Bicifadine hydrochloride polymorph form B wherein solid crystals of said polymorph have the following major infrared spectrum peaks in wavenumbers (cm−1):
2108; 891; 856; 719; and 660.
- 3. A bicifadine hydrochloride of polymorph form B of claim 2, wherein the crystals are characterized by an infrared spectrum as solid crystals having the following peaks in wavenumbers (cm−1)
- 4. Bicifadine hydrochloride polymorph form B wherein solid crystals of said polymorph are characterized by having major peaks as measured by x-ray powder diffraction radiation using Cu Ka radiation at the following 2θ (deg)
5.08; 10.07; 20.16; 25.17; and 30.43.
- 5. The bicifadine hydrochloride polymorph form B of claim 4 having the following x-ray diffraction expressed in terms of “d” spacings and relative intensities I (s=strong, m=medium, w=weak, v=very, d=diffuse)
- 6. A method of producing bicifadine hydrochloride as solid polymorph B crystals comprising providing a slurry of bicifadine hydrochloride in an organic solvent, having a boiling point of at least about 50° C., heating said slurry to a temperature at which said slurry is a clear solution, allowing said solution to cool to a temperature of at most about 35° C., maintaining said cooled solution at said temperature of at most 35° C. for a period of time sufficient to allow said polymorph B to crystallize out in the form of crystals from said solution.
- 7. The process of claim 6 wherein said cooling is carried out while said solution in agitated.
- 8. The process of claim 6 wherein said cooled solution is maintained at a temperature of at most 35° C. while subject to agitation.
- 9. The process of claim 6 wherein the heated solution is allowed to cool to a temperature of from about −200° C. to 0° C.
- 10. A method of producing bicifadine as solid polymorph B crystals comprising providing solid polymorph A crystals of bicifadine hydrochloride, agitating said crystals at a temperature of from about −200° C. to 50° C. to convert said polymorph A crystals to polymorph B crystals.
- 11. The process of claim 10 wherein said agitation is carried out by grinding.
- 12. The process of claim 10 wherein said agitation is carried out at a temperature of from about −200° C. to about 35° C.
- 13. The method of claim 12 wherein said agitation is carried out at a temperature of from about −200° C. to 0° C.
- 14. The pharmaceutical composition in oral unit dosage form comprising solid polymorph B crystals of bicifadine hydrochloride and an inert pharmaceutically acceptable carrier or diluent.
- 15. The oral unit dosage form of claim 14 wherein said bicifadine hydrochloride in polymorph B crystalline form is present in said oral unit dosage form in the amount of 25 mg to about 600 mg.
- 16. The pharmaceutical composition of claim 15 wherein the oral unit dosage form contains from about 25 to 600 mg of said crystalline polymorph form B.
- 17. The composition of claim 15 wherein said oral unit dosage form is a tablet or capsule.
- 18. A method for reducing pain in a patient in need of said treatment comprising administering to said patient a composition containing bicifadine hydrochloride having the crystalline structure of polymorph B and an inert carrier or diluent, said composition being administered in an effective amount to alleviate said pain.
- 19. The composition of claim 18 wherein said bicifadine hydrochloride having crystalline form of polymorph B is administered in an amount of from 0.5 mg/kg to about 20 mg/kg per day.
- 20. The method of claim 19 where said bicifadine is administered in all unit dosage forms containing from about 25 to 600 mg.
- 21. A method of producing pure polymorph B crystals from bicifadine hydrochloride in either polymorph form A or a mixture of polymorph from A and B comprising adding bicifadine hydrochloride in either polymorph form A or a mixture of polymorph from A and B to an organic solvent to form a slurry and applying kinetic energy to said slurry at a temperature of at most of about 35° C. or for at least a period of time sufficient to form polymorph B crystals of bicifadine hydrochloride.
- 22. The method of claim 21 wherein said kinetic energy is applied by agitation.
- 23. The method of claim 22 wherein agitation is carried out by stirring.
RELATED APPLICATIONS
[0001] This application is based upon and claims the benefits of U.S. Provisional Patent Application 60/424,982, filed on Nov. 8, 2002 entitled “Polymorphs of Bicifadine Hydrochloride”.
Provisional Applications (1)
|
Number |
Date |
Country |
|
60424982 |
Nov 2002 |
US |