Pharmaceutical compositions
The invention provides (+)-α-dihydrotetrabenazine succinate salt. Also provided are (+)-α-dihydrotetrabenazine succinate salt for use in medicine, pharmaceutical compositions comprising (+)-α-dihydrotetrabenazine succinate salt and a pharmaceutically acceptable excipient and the uses of (+)-α-dihydrotetrabenazine succinate salt as a VMAT2 receptor antagonist and in the treatment of a movement disorder such as Tourette's syndrome. The invention further provides a method for preparing the (+)-α-dihydrotetrabenazine succinate salt.
1. (+)-α-Dihydrotetrabenazine succinate salt.
2. A pharmaceutical composition comprising (+)-α-dihydrotetrabenazine succinate salt and a pharmaceutically acceptable excipient.
3. A pharmaceutical composition according to claim 2 , which is a unit dosage form comprising between 1 mg and 30 mg of (+)-α-dihydrotetrabenazine succinate salt and a pharmaceutically acceptable excipient.
4. The unit dosage form according to claim 3 , wherein the unit dosage form is a capsule or a tablet.
5. (+)-α-Dihydrotetrabenazine succinate salt according to claim 1 in a crystalline form.
6. A pharmaceutical composition according to claim 2 wherein the (+)-α-dihydrotetrabenazine succinate salt is in a crystalline form.
7. (+)-α-Dihydrotetrabenazine succinate salt according to claim 1 having a salt ratio of approximately 1:1.
8. A pharmaceutical composition according to claim 2 wherein the (+)-α-dihydrotetrabenazine succinate salt has a salt ratio of approximately 1:1.
9. (+)-α-Dihydrotetrabenazine succinate salt according to claim 1 in a substantially crystalline form having an X-ray powder diffraction pattern characterized by the presence of major peaks at the diffraction angles of approximately 9.2° and/or 10.0° and/or 18.5° and/or 22.4°.
10. A pharmaceutical composition according to claim 2 wherein the (+)-α-dihydrotetrabenazine succinate salt is in a substantially crystalline form having an X-ray powder diffraction pattern characterized by the presence of major peaks at the diffraction angles of approximately 9.2° and/or 10.0° and/or 18, and/or 22.5°.
11. (+)-α-Dihydrotetrabenazine succinate salt according to claim 1 in a substantially crystalline form having an X-ray powder diffraction pattern substantially as shown in any of plots ZEN-E-6-7b, LYO-F-4(3), SUN-AJ-163(2) or SUN-AJ-163(2) AD in FIG. 1 .
12. A pharmaceutical composition according to claim 2 wherein the (+)-α-dihydrotetrabenazine succinate salt is in a substantially crystalline form having an X-ray powder diffraction pattern substantially as shown in any of plots ZEN-E-6-7b, LYO-F-4(3), SUN-AJ-163(2) or SUN-AJ-163(2) AD in FIG. 1 .
13. (+)-α-Dihydrotetrabenazine succinate salt according to claim 1 in a substantially crystalline form having an X-ray powder diffraction pattern substantially as shown in plot SUN-AJ-163(2) in FIG. 1 .
14. A pharmaceutical composition according to claim 2 wherein the (+)-α-dihydrotetrabenazine succinate salt is in a substantially crystalline form having an X-ray powder diffraction pattern substantially as shown in plot SUN-AJ-163(2) in FIG. 1 .
15. (+)-α-Dihydrotetrabenazine succinate salt according to claim 1 which exhibits an endothermic event having a peak at approximately 150° C. when subjected to differential scanning calorimetry.
16. A pharmaceutical composition according to claim 2 wherein the (+)-α-dihydrotetrabenazine succinate salt exhibits an endothermic event having a peak at approximately 150° C. when subjected to differential scanning calorimetry.