Polymorphs of fexofenadine hydrochloride
OwnerBen-Zion Dolitzky, Shlomit Wizel +3inventors
InventorsBen-Zion Dolitzky, Shlomit Wizel, Barnaba Krochmal, Dov Diller, Irwin Gross
Life of this patent
Estimating the term…
Abstract
The present invention provides novel crystal forms of fexofenadine hydrochloride Forms V, VI and VIII through XV and processes for their preparation and preparation of amorphous form and other crystalline forms of fexofenadine hydrochloride. Forms XIV and XV are solvates of ethyl acetate, while Form IX is a solvate of MTBE or cyclohexane. The forms are useful for administration to humans and animals to alleviate symptoms caused by histamine. The present invention further provides pharmaceutical compositions of the new crystalline forms.
Claims16
Fexofenadine hydrochloride characterized by a PXRD pattern with peaks at about 4.7, 9.3, 17.4, 18.2, 19.4, 19.6, 21.6 and 24.0±0.2 degrees two theta.
Fexofenadine hydrochloride Form IX.
A fexofenadine hydrochloride MTBE solvate.
A fexofenadine hydrochloride Form IX-MTBE solvate.
A fexofenadine hydrochloride MTBE solvate characterized by a DTG profile with endotherms at about 100° C. and about 125° C.
A fexofenadine hydrochloride cyclohexane solvate.
A fexofenadine hydrochloride Form IX-cyclohexane solvate.
A fexofenadine hydrochloride cyclohexane solvate by a DTG profile with endotherms at about 99° C. to about 110° C. and about 140° C. to about 150° C.
A process for preparing fexofenadine hydrochloride Form IX comprising the steps of
- a) preparing a solution of fexofenadine hydrochloride in acetone;
- b) adding the solution to an anti-solvent selected from the group consisting of MTBE and cyclohexane to form a precipitate;
- and
- c) separating the precipitate as a solvate of the anti-solvent used.
A process for preparing fexofenadine hydrochloride Form IX comprising the steps of:
- a) preparing a solution of fexofenadine hydrochloride in ethanol;
- b) adding the solution to an anti-solvent selected from the group consisting of MTBE and cyclohexane to form a precipitate;
- and
- c) separating the precipitate as a solvate of the anti-solvent used.
A pharmaceutical composition comprising:
- a) fexofenadine hydrochloride selected from the group consisting of Form IX-MTBE solvate and Form IX-cyclohexane solvate;
- and
- b) a pharmaceutically acceptable excipient.
Dependencies are inferred from the claim text.