Crystalline forms of temozolomide
View Patent ↗Disclosed are novel crystalline forms of Temozolomide, methods of preparation thereof, medicaments including the novel crystalline forms of Temozolomide, and uses thereof in the treatment of medical conditions.
1. Crystalline Temozolomide Form III comprising at least one of the characteristics selected from the group consisting of:
a powder X-ray diffraction pattern exhibiting peaks at diffraction angles 2θ of about 10.8, 13.2, 14.7, 16.2, 16.8, 18, 19.1, 19.6, 21.5, 26.6, 23.8, 28.8, 29.8±0.2°; and
an infrared spectrum with ν max at about 1678, 731 and 712±4 cm −1 .
2. The crystalline Temozolomide of claim 1 , wherein said powder X-ray diffraction pattern is substantially as depicted in FIG. 6 .
3. The crystalline Temozolomide of claim 1 , wherein said infrared spectrum is substantially as depicted in FIG. 7 .
4. A process of preparing crystalline Temozolomide Form III, the process comprising:
contacting Temozolomide with a solvent, said solvent including at least one solvent component selected from the group consisting of dimethylformamide, ethanol, and a mixture of benzyl alcohol and isopropanol, to thereby form a Temozolomide solution;
crystallizing said Temozolomide in said solution, to thereby obtain the crystalline Temozolomide Form III; and
isolating the crystalline Temozolomide Form III.
5. A process of preparing crystalline Temozolomide Form III, the process comprising
heating crystalline Temozolomide Form II to a transubstantiation temperature of about 120° C., to thereby obtain the crystalline Temozolomide Form III, wherein the Form II precursor exhibits a powder X-ray diffraction pattern with peaks at diffraction angles 2θ of about 10.8, 11.3, 14.5, 16.0, 17.9 and 19.1±0.2° or exhibits an infrared spectrum with ν max at about 3451, 1749 and 1736±4 cm −1 , and the Form III product exhibits a powder X-ray diffraction pattern with peaks at diffraction angles 2θ of about 10.8, 13.2, 14.7, 16.2, 16.8, 18, 19.1, 19.6, 21.5, 26.6, 23.8, 28.8, 29.8±0.2° or exhibits an infrared spectrum with ν max at about 1678, 731 and 712±4 cm −1 .