Compositions and Formulations of 9-Nitrocamptothecin Polymorphs and Methods of Use Therefor
A polymorphic form of 9-nitrocamptothecin is provided, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
1 . A polymorphic form of 9-nitrocamptothecin, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
2 . A polymorphic form of 9-nitrocamptothecin according to claim 1 , the polymorph being further characterizable as having, by differential scanning calorimetry, an endotherm at between 274.4 to 275.3° C., and an exotherm at between 279.8 and 280.8° C.
3 . A polymorphic form of 9-nitrocamptothecin according to claim 1 , the polymorph being further characterizable as having, by differential scanning calorimetry, an endotherm at between 274.7 to 275.1° C., and an exotherm at between 280.1 and 280.5° C.
4 . A polymorphic form of 9-nitrocamptothecin according to claim 1 , the polymorph being further characterizable as having, by differential scanning calorimetry, an endotherm at between 274.8 to 275.0° C., and an exotherm at between 280.2 and 280.4° C.
5 . A polymorphic form of 9-nitrocamptothecin, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
6 . A polymorphic form of 9-nitrocamptothecin, the polymorph being characterizable as having, for Cu Kα radiation of wavelength of 1.5406 Angstrom, an X-ray powder diffraction pattern with diffraction lines at °2θ values 4.8, 14.2, 19.1 and 26.8.
7 . 9-nitrocamptothecin in a form crystallized from acetonitrile.
8 . A polymorphic form of 9-nitrocamptothecin according to claim 7 , the polymorph being characterizable as having, differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
9 . A polymorphic form of 9-nitrocamptothecin according to claim 7 , the polymorph being characterizable as having an X-ray powder diffraction pattern with diffraction lines at °2θ values 4.8, 14.2, 19.1 and 26.8 for Cu Kα radiation wavelength 1.5406 Angstrom.
10 . A polymorphic form of 9-nitrocamptothecin according to claim 7 , the polymorph being characterizable as having, for Cu Kα radiation of wavelength 1.5406 Angstrom, an X-ray powder diffraction pattern with diffraction lines at °2θ values 4.8, 14.2, 19.1 and 26.8.
11 . A pharmaceutical composition comprising:
a pharmaceutical carrier; and
a polymorphic form of 9-nitrocamptothecin, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
12 . A pharmaceutical formulation according to claim 11 , the polymorph being further characterizable as having, by differential scanning calorimetry, an endotherm at between 274.4 to 275.3° C., and an exotherm at between 279.8 and 280.8° C.
13 . A pharmaceutical formulation according to claim 11 , the polymorph being further characterizable as having, by differential scanning calorimetry, an endotherm at between 274.7 to 275.1° C., and an exotherm at between 280.1 and 280.5° C.
14 . A pharmaceutical formulation according to claim 11 , the polymorph being further characterizable as having, by differential scanning calorimetry, an endotherm at between 274.8 to 275.0° C., and an exotherm at between 280.2 and 280.4° C.
15 . A pharmaceutical composition comprising:
a pharmaceutical carrier; and
a polymorphic form of 9-nitrocamptothecin, the polymorph being characterizable as having, by differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
16 . A pharmaceutical composition comprising:
a pharmaceutical carrier; and
a polymorphic form of 9-nitrocamptothecin, the polymorph being characterizable as having, for Cu Kα radiation of wavelength of 1.5406 Angstrom, an X-ray powder diffraction pattern with diffraction lines at °2θ values 4.8, 14.2, 19.1 and 26.8.
17 . A pharmaceutical composition comprising:
a pharmaceutical carrier; and
a polymorphic form of 9-nitrocamptothecin crystallized from acetonitrile.
18 . A pharmaceutical formulation according to claim 17 , the polymorph being characterizable as having, differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
19 . A pharmaceutical formulation according to claim 17 , the polymorph being characterizable as having an X-ray powder diffraction pattern with diffraction lines at °2θ values 4.8, 14.2, 19.1 and 26.8 for Cu Kα radiation of wavelength 1.5406 Angstrom.
20 . A method of preparing a polymorphic form of 9-nitrocamptothecin, the method comprising:
crystallizing 9-nitrocamptothecin from acetonitrile.
21 . A method according to claim 20 , the polymorph being characterizable as having, differential scanning calorimetry, an endotherm at between 273.9 to 275.9° C., and an exotherm at between 279.3 and 281.3° C.
22 . A method according to claim 20 , the polymorph being characterizable as having an X-ray powder diffraction pattern with diffraction lines at °2θ values 4.8, 14.2, 19.1 and 26.8 for Cu Kα radiation of wavelength 1.5406 Angstrom.