Cocrystallization
View Patent ↗The present disclosure relates to novel cocrystals and novel methods for cocrystallization. In particular, the disclosure includes cocrystals comprising a salt of an active agent, such as a chloride salt of an active pharmaceutical ingredient. The present disclosure also relates to methods of preparing cocrystals and methods for screening for solid state phases.
1. A cocrystal of fluoxetine hydrochloride and a guest,
wherein the guest is selected from benzoic acid, succinic acid, and fumaric acid.
2. The cocrystal of claim 1 wherein the guest is benzoic acid.
3. The cocrystal of claim 2 wherein the cocrystal is a 1:1 cocrystal of fluoxetine hydrochloride to benzoic acid.
4. The cocrystal of claim 3 having a melting point of about 134° C.
5. The cocrystal of claim 1 wherein the guest is succinic acid.
6. The cocrystal of claim 5 wherein the cocrystal is a 2:1 cocrystal of fluoxetine hydrochloride to succinic add.
7. The cocrystal of claim 6 having a melting point of about 137° C.
8. The cocrystal of claim 1 wherein the guest is fumaric acid.
9. The cocrystal of claim 8 wherein the cocrystal is a 2:1 cocrystal of fluoxetine hydrochloride to fumaric acid.
10. The cocrystal of claim 6 having a melting point of about 164° C.
11. The cocrystal of claim 6 wherein the crystal system is orthorhombic.
12. The cocrystal of claim 11 wherein the space group is Pbcn.
13. The cocrystal of claim 11 wherein the unit cell volume is about 4000 Å 3 at about 100 K.
14. The cocrystal of claim 12 wherein the unit cell volume is about 4000 Å 3 at about 100 K.
15. The cocrystal of claim 11 wherein the unit cell dimensions are: a is about 26.6 Å at about 100 K; b is about 7.2 Å at about 100 K; and c is about 20.8 Å at about 100 K.