Polymorphs of bicifadine hydrochloride
A new polymorphic crystalline form of bicifadine hydrochloride, designated form B, which is more thermodynamically stable than the previously known polymorphic form of bicifadine hydrochloride, designated as form A, methods for preparing said crystalline form B and pharmaceutical compositions containing said crystalline form B.
1. A solid composition comprising bicifadine hydrochloride polymorph form B substantially free of bicifadine hydrochloride polymorph form A, said solid composition comprising solid crystals of form B having a distinct infrared profile characterized by one or more of the following infrared spectrum peaks in wavenumbers (cm− 1 ):
3185
1111
2769
1022
2437
963
2276
904
2108
891
1908
856
1804
818
1658
783
1596
719
1518
684
1453
660
1403
637
1343
580
1305
532
1274
475
1209
422
1131
and a distinct x-ray powder diffraction (XRPD) profile characterized by one or more of the following XRPD peaks expressed in terms of “d” spacings and relative intensities I (s =strong, m=medium, w=weak, v=very, d=diffuse)
2θ (deg)
d (Å)
I a
5.08
17.39
Vs
10.07
8.77
S
15.19
5.83
S
16.83
5.27
S
18.64
4.76
Md
18.76
4.73
Md
19.64
4.52
W
20.16
4.40
M
21.96
4.05
M
22.37
3.97
S
23.16
3.84
W
24.00
3.70
W
25.27
3.52
D
27.33
3.26
Md
27.74
3.21
M
29.00
3.08
M
30.43
2.93
Md
31.84
2.80
Wd
32.29
2.77
W
35.27
2.54
Wd
35.64
2.52
W.
s = strong, m = medium, w = weak, v = very, d = diffuse
2. The solid composition of claim 1 , which comprises a tablet.
3. The solid composition of claim 1 , which comprises a capsule.
4. The solid composition of claim 1 , wherein said tablet or capsule comprises said polymorph B crystalline form in a unit dosage amount of between 25 mg to 600 mg.
5. The solid composition of claim 1 , wherein said tablet or capsule comprises said polymorph B crystalline form in a unit dosage amount of between 200 mg to 400 mg.