Crystalline form IV of linezolid
OwnerJudith Aronhime, Tamas Koltai +3inventors
InventorsJudith Aronhime, Tamas Koltai, Viviana Braude, Serguei Fine, Tamar Niddam
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Abstract
The present invention provides a novel crystalline form of linezolid referred to herein as Form IV as well as methods for the preparation and use of Form IV. The present invention provides pharmaceutical compositions that comprise therapeutically effective amounts of Form IV that can be used to treat patients suffering from gram-positive bacterial infections. Various processes for making crystalline linezolid Form IV are disclosed.
Claims16
1-7. (canceled)
Crystalline linezolid characterized by data selected from the group consisting of:
- a) a powder X-ray diffraction pattern with peaks at about 13.5. 18.0, 21.1, 22.2, and 25.4±0.2 degrees 2 theta:
- b) an FTIR spectrum with peaks at about 2817 1335, 1229, 1200. and 662 cm−1;
- and
- c) an FTRaman spectrum with peaks at about 2975, 2930, 2865, 1083, and 750 cm−1;
- and having a content of less than 0.5% (w/w) of the R-enantiomer of linezolid.
Crystalline linezolid characterized by data selected from the group consisting of:
- a) a powder X-ray diffraction pattern with peaks at about 13.5. 18.0, 21.1, 22.2. and 25.4±0.2 degrees 2 theta;
- b) an FTIR spectrum with peaks at about 2817, 1335, 1229, 1200, and 662 cm−1;
- and
- c) an FTRaman spectrum with peaks at about 2975, 2930, 2865, 1083. and 750 cm−1;
- and containing less than about 10% of crystalline Form II.
Crystalline linezolid characterized by data selected from the group consisting of:
- a) a powder X-ray diffraction pattern with peaks at about 13.5, 18.0. 21.1, 22.2, and 25.4±0.2 degrees 2 theta;
- b) an FTIR spectrum with peaks at about 2817, 1335, 1229, 1200, and 662 cm−1;
- and
- c) an FTRaman spectrum with peaks at about 2975, 2930, 2865, 1083, and 750 cm−1;
- and which is stable against transformation into Form II upon storage at a relative humidity of about 0% to about 100% at room temperature for at least 10 days.
A method of preparing crystalline linezolid characterized by data selected from the group consisting of:
- a) a powder X-ray diffraction pattern with peaks at about 13.5, 18.0, 21.1, 22.2, and 25.4±0.2 degrees 2 theta;
- b) an FTIR spectrum with peaks at about 2817, 1335, 1229, 1200, and 662 cm−1;
- and
- c) an FTRaman spectrum with peaks at about 2975, 2930, 2865, 1083, and 750 cm−1 comprising:
- d) dissolving linezolid in a polar organic solvent to form a linezolid solution;
- e) spray-drying the linezolid solution at a temperature of at least 50° C.
A process for preparing crystalline linezolid characterized by data selected from the group consisting of:
- a) a powder X-ray diffraction pattern with peaks at about 13.5, 18.0, 21.1, 22.2, and 25.4±0.2 degrees 2 theta;
- b) an FTIR spectrum with peaks at about 2817, 1335, 1229, 1200, and 662 cm−1;
- and
- c) an FTRaman spectrum with peaks at about 2975, 2930, 2865, 1083, and 750 cm−1 comprising heating crystalline Linezolid Form II to a temperature of at least 85° C. for at least one hour.
A process for preparing crystalline linezolid Form II comprising:
- a) combining crystalline linezolid Form IV with a solvent at room temperature to form a slurry;
- b) stirring the slurry for 1 to 24 hours to obtain crystalline material;
- c) filtering and drying the crystalline material to obtain crystalline linezolid Form II.
A process for preparing crystalline linezolid Form IV comprising:
- a) combining crystalline linezolid Form II with a solvent at room temperature to form a slurry;
- b) heating the slurry;
- c) filtering the heated slurry to obtain crystalline linezolid Form IV.
22-23. (canceled)
Dependencies are inferred from the claim text.