Crystalline forms of gatifloxacin
AssigneeTeva Pharmaceuticals USA, Inc.
InventorsValerie Niddam-Hildesheim, Shlomit Wizel, Greta Sterimbaum
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Abstract
Provided are novel crystalline forms of gatifloxacin, denominated forms L, M, P, Q, S, and T1, and methods for making them. Also provided are methods of transforming the novel crystalline forms of gatifloxacin of the present invention to other crystalline forms of gatifloxacin.
Claims36
A crystalline form of gatifloxacin characterized by an x-ray diffraction diagram consisting essentially of a major reflection at about 17.2°±0.2° 2θ.
A crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 8.8°, 14.1°, 17.6°, 18.2°, 22.0°, and 22.6°±0.2° 2θ.
A crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 11.1°, 11.7°, 12.5° and 23.0°±0.2° θ.
A crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 6.8°, 7.1°, 11.1°, 15.5°, and 17.4°±0.2° 2θ.
A crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 9.3°, 11.0°, 12.0°, 14.5°, 18.6° and 21.2°±0.2° 2θ.
A crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 7.4°, 8.9°, 9.6°, 11.4°, 12.2°, 12.9°, 14.1°, 16.7°, 21.2°, 21.8°, 24.1°, and 26.0°±0.2° 2θ.
A method of making gatifloxacin sesquihydrate comprising the step of maintaining a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 11.1°, 11.7°, 12.5° and 23.0°±0.2° 2θ at ambient temperature for a time sufficient to effect conversion to the sesquihydrate.
A method of making a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 13.5°, 19.6°, 20.4°, 23.6°, 25.8°, and 28.5°±0.2° 2θ comprising the step of drying gatifloxacin form K at about 50° C. and a pressure of about 10 mm Hg.
A method of making a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 6.7°, 11.3°, 13.8°, and 16.4°±0.2° 2θ comprising the step of drying gatifloxacin form K at about 50° C. and atmospheric pressure.
A method of making a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 13.5°, 19.6°, 20.4°, 23.6°, 25.8°, and 28.5°±0.2° 2θ comprising the step of maintaining a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram consisting essentially of a major reflection at about 17.2°±0.2° 2θ at ambient temperature for a time sufficient to effect conversion to the crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 13.5°, 19.6°, 20.4°, 23.6°, 25.8°, and 28.5°±0.2° 2θ.
A method of making gatifloxacin hemihydrate comprising the step of maintaining a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 8.8°, 14.1°, 17.6°, 18.2°, 22.0°, and 22.6°±0.2° 2θ at room temperature for a time sufficient to effect conversion to the hemihydrate.
A pharmaceutical composition comprising at least one pharmaceutically acceptable excipient and at least one of
- i) a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram consisting essentially of a major reflection at about 17.2°±0.2° 2θ,
- ii) a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 8.8°, 14.1°, 17.6°, 18.2°, 22.0°, and 22.6°±0.2° 2θ,
- iii) a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 11.1°, 11.7°, 12.5° and 23.0° 2θ,
- iv) a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 6.8°, 7.1°, 11.1°, 15.5°, and 17.4°±0.2° 2θ,
- v) a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 9.3°, 11.0°, 12.0°, 14.5°, 18.6° and 21.2°±0.2° 2θ, or
- vi) a crystalline form of gatifloxacin characterized by an x-ray diffraction diagram having reflections at about 7.4°, 8.9°, 9.6°11.4°, 12.2°, 12.9°, 14.1°, 16.7°, 21.2°, 21.8°, 24.1°, and 26.0°±0.2° 2θ.
Dependencies are inferred from the claim text.