Polymorphic forms of lubiprostone
AssigneeApotex Pharmachem Inc.
InventorsAlfredo Paul Ceccarelli, Kiran Kumar Kothakonda
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Abstract
There is provided a crystalline form of Lubiprostone, termed APO-II and methods for making APO-II. APO-II is a polymorphic form of Lubiprostone.
Claims114
APO-II polymorphic form of Lubiprostone.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at approximately 8.98.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at approximately 13.53.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at approximately 18.06.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at approximately 20.57.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at approximately 20.80.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern comprising a peak, in terms of 2-theta, at approximately 22.74.
A crystalline form of Lubiprostone having an X-ray powder diffraction pattern substantially as shown in FIG. 1.
A process to prepare APO-II comprising:
- distilling a Lubiprostone filtrate to near dryness thereby forming a residue;
- dissolving the residue in a first organic solvent thereby forming a residue solution;
- adding a second organic solvent to the residue solution thereby forming a mixture;
- stirring the mixture until precipitation occurs thereby forming a precipitate;
- filtering the precipitate thereby isolating APO-II.
A process to prepare APO-II comprising:
- dissolving Lubiprostone in a third organic solvent thereby forming a Lubiprostone solution;
- adding a fourth organic solvent to the Lubiprostone solution thereby forming a mixture;
- stirring the mixture until precipitation occurs thereby forming a precipitate;
- filtering the precipitate thereby isolating APO-II.
A process to prepare APO-II comprising:
- dissolving Lubiprostone in a third organic solvent thereby forming a Lubiprostone solution;
- adding the Lubiprostone solution to a fourth organic solvent thereby forming a mixture;
- stirring the mixture until precipitation occurs thereby forming a precipitate;
- filtering the precipitate thereby isolating APO-II.
A pharmaceutical formulation comprising APO-II.
Dependencies are inferred from the claim text.