Forms of 5-azacytidine
View Patent ↗The invention provides novel polymorphic and pseudopolymorphic crystalline forms of 5-azacytidine, along with methods for preparing said forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising said forms.
1. Form IV of 5-azacytidine characterized by a X-Ray Powder Diffraction pattern obtained by irradiation with Cu Kα X-rays which shows main peaks with interplanar spacings at:
d(Å)
15.408
7.642
7.040
6.289
5.555
5.213
4.906
4.355
4.281
4.132
4.073
3.957
3.913
3.760
3.695
3.526
3.511
3.312
3.185
3.126
3.106
2.964
2.912
2.877
2.557
2.354
2.342.
2. A pharmaceutical composition comprising the 5-azacytidine form of claim 1 and a pharmaceutically acceptable excipient, diluent, or carrier.
3. Form V of 5-azacytidine characterized by a X-Ray Powder Diffraction pattern obtained by irradiation with Cu Kα X-rays which shows main peaks with interplanar spacings at:
d(Å)
8.024
7.160
6.714
6.436
6.084
5.697
5.350
4.930
4.780
4.618
4.476
4.365
4.126
4.042
3.948
3.834
3.702
3.620
3.273
3.133
3.072
3.033
2.889
2.870
2.370.
4. A pharmaceutical composition comprising the 5-azacytidine form of claim 3 and a pharmaceutically acceptable excipient, diluent, or carrier.
5. Form VII of 5-azacytidine characterized by a X-Ray Powder Diffraction pattern obtained by irradiation with Cu Kα X-rays which includes diffraction peaks at 5.8, 11.5, 12.8, 22.4 and 26.6° 2θ.
6. A pharmaceutical composition comprising the 5-azacytidine form of claim 5 and a pharmaceutically acceptable excipient, diluent, or carrier.
7. Form VIII of 5-azacytidine characterized by a X-Ray Powder Diffraction pattern obtained by irradiation with Cu Kα X-rays which shows main peaks with interplanar spacings at:
d(Å)
13.384
8.292
7.020
6.623
5.587
5.129
4.383
4.257
4.079
3.923
3.483
3.458
3.046
2.782
2.556
2.348.
8. A pharmaceutical composition comprising the 5-azacytidine form of claim 7 and a pharmaceutically acceptable excipient, diluent, or carrier.