Rapamycin polymorphs and uses thereof
AssigneeWyeth
InventorsTianmin Zhu, Mahdi Fawzi
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Abstract
The present invention provides rapamycin polymorph Form II. This invention also provides processes for preparing rapamycin polymorph Form II and pharmaceutical compositions including rapamycin polymorph Form II.
Claims22
A rapamycin polymorph Form II having:
- (a) a differential scanning calorimetry thermogram lacking an endotherm peak of about 194°;
- and
- (b) an X-ray diffraction peak pattern lacking peaks at 2θ of 7.2°, 9.9°, 10.2°, 11.1°, 12.5°, 14.5°, 15.3°, 15.5°, 16.2°, 20.0°, 20.4°, and 21.8°.
A rapamycin polymorph Form II having the following characteristics:
- (a) X-ray diffraction peak pattern comprising peaks at 2θ of about 7°, 9.7°, 10.1°, 11.0°, 12.4°, 13.1°, 14.1°, 14.6°, 15.0°, 15.2°, 15.8°, 16.3°, 16.6°, 17.6°, 18.1°, 18.3°, 19.7°, 20.2°, and 21.2°;
- and
- (b) a differential scanning calorimetry thermogram having an endotherm peak of about 188°.
A rapamycin polymorph Form II obtained by recrystallizing rapamycin from t-butyl methyl ether.
A process for preparing rapamycin polymorph Form II comprising the steps of:
- dissolving amorphous rapamycin in t-butyl methyl ether and recrystallizing rapamycin to afford rapamycin form II.
A process for preparing rapamycin polymorph Form I comprising desolvating rapamycin polymorph Form II.
A pharmaceutical composition comprising rapamycin polymorph Form II and a pharmaceutically acceptable carrier.
A kit comprising (i) rapamycin polymorph Form II;
- and (ii) a carrier suitable for administration to a mammalian subject.
Dependencies are inferred from the claim text.