Claims
- 1. Anhydrous crystalline R(-)-N-(4,4-di(3-methylthien-2yl)but-3-enyl)nipecotic acid hydrochloride having substantially the following X-ray powder diffraction peaks obtained with KBr: 6.4, 11.3, 13.0, 13.9, 15.0, 18.7, 19.4, 22.5 and 23.7.
- 2. Anhydrous crystalline R(-)-N-(4,4-di(3-methylthien-2yl)but-3-enyl)nipecotic acid hydrochloride substantially free of bound organic solvent and having substantially the following X-ray powder diffraction peaks obtained with KBr: 6.4, 11.3, 13.0, 13.9, 15.0, 18.7, 19.4, 22.5 and 23.7.
- 3. A process for the preparation of anhydrous crystalline R(-)-N-(4,4-di(3-methylthien-2yl)but-3-enyl)nipecotic acid hydrochloride having substantially the following X-ray powder diffraction peaks obtained with KBr: 6.4, 11.3, 13.0, 13.9, 15.0, 18.7, 19.4, 22.5 and 23.7 which process comprises
- a) dissolving tiagabine hydrochloride in an aqueous hydrochloric acid solution, and
- b) precipitating tiagabine hydrochloride from the aqueous hydrochloric acid solution.
- 4. A pharmaceutical composition comprising a therapeutically effective amount of a crystalline salt according to claim 1 together with a pharmaceutically acceptable carrier or diluent.
- 5. The pharmaceutical composition according to claim 4 in the form of a dosage unit containing about 1.0-1500 mg of the active ingredients.
- 6. A method of inhibiting GABA uptake in a mammal in need of such treatment comprising administering an effective amount of a crystalline salt according to claim 1.
- 7. A method of inhibiting GABA uptake in a mammal in need of such treatment comprising administering a pharmaceutical composition according to claim 4.
Priority Claims (1)
Number |
Date |
Country |
Kind |
0661/96 |
Jun 1996 |
DKX |
|
CROSS-REFERENCE TO RELATED APPLICATIONS
This application claims priority under 35 U.S.C. 119 of Danish application Ser. No. 0661/96 filed Jun. 14, 1996 and U.S. provisional application No. 60/020,978 filed Jun. 24, 1996, the contents of which are fully incorporated herein by reference.
US Referenced Citations (1)
Number |
Name |
Date |
Kind |
5010090 |
Gronvald et al. |
Apr 1991 |
|
Non-Patent Literature Citations (2)
Entry |
McGraw et al. "The identification and characterization of polymorphism in tiagabine HCI bulk drug" Derwent abst 95-05633, 1994. |
Andersen et al., J. Med. Chem., vol. 36, pp. 1716-1725 (1993). |