Crystalline venlafaxine base and novel polymorphs of venlafaxine hydrochloride, processes for preparing thereof
AssigneeTeva Pharmaceutical USA, Inc.
InventorsBen-Zion Dolitzky, Judith Aronhime, Shlomit Wizel, Gennady A. Nisnevich
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Abstract
The present invention relates to novel essentially pure venlafaxine and the process of preparation thereof. The present invention also relates to novel solvate forms of venlafaxine hydrochloride and the process of preparation thereof. Furthermore, the present invention provides a novel process for preparing venlafaxine hydrochloride from venlafaxine; the process comprises the steps of: i) preparing a mixture of venlafaxine with acetone; and ii) exposing the mixture in gaseous hydrochloric acid.
Claims37
1-27. (canceled)
Venlafaxine hydrochloride Form II, characterized by powder x-ray diffraction peaks at 12.8, 20.5, 21.3±0.2 degrees two-theta.
Venlafaxine hydrochloride Form III characterized by powder x-ray diffraction peaks at 7.4, 14.9, 26.5±0.2 degrees two-theta.
Venlafaxine hydrochloride Form IV characterized by powder x-ray diffraction peaks at 10.3, 13.5, 15.6, 20.3±0.2 degrees two-theta.
A process for preparing venlafaxine hydrochloride Form III comprising dissolving venlafaxine hydrochloride in a protic solvent and crystallizing venlafaxine hydrochloride Form III by the addition of an aprotic solvent.
A process for preparing venlafaxine hydrochloride Form III comprising crystallizing venlafaxine hydrochloride from a protic solvent.
A process for preparing venlafaxine hydrochloride Form IV comprising crystallizing venlafaxine hydrochloride from an aprotic polar solvent.
A process for preparing venlafaxine hydrochloride Form II comprising dissolving venlafaxine hydrochloride in a mixture of a protic solvent and an aprotic solvent, and crystallizing venlafaxine hydrochloride Form II.
A process for preparing venlafaxine hydrochloride Form I, venlafaxine hydrochloride Form II, or a mixture thereof comprising drying venlafaxine hydrochloride Form III for a sufficient time to obtain venlafaxine hydrochloride Form I, venlafaxine hydrochloride Form II, or a mixture thereof.
A process of preparing venlafaxine hydrochloride Form III, venlafaxine hydrochloride Form IV, or a mixture thereof comprising drying venlafaxine hydrochloride Form IV for a sufficient time to obtain venlafaxine hydrochloride Form III, venlafaxine hydrochloride Form IV, or a mixture thereof.
A process for preparing venlafaxine hydrochloride Form III comprising dissolving venlafaxine hydrochloride in chloroform and crystallizing venlafaxine hydrochloride Form III by the addition of any of hexane and toluene.
A process for preparing venlafaxine hydrochloride Form III comprising triturating venlafaxine hydrochloride in an aprotic solvent under a reflux condition for at least 1 hour to obtain venlafaxine hydrochloride Form III.
A process for preparing venlafaxine hydrochloride Form III comprising triturating venlafaxine hydrochloride in an aprotic solvent at room temperature for at least a period of about 20 hours to obtain venlafaxine hydrochloride Form III.
A process for preparing venlafaxine hydrochloride Form II comprising triturating venlafaxine hydrochloride with acetone, and drying to obtain venlafaxine hydrochloride Form II.
Dependencies are inferred from the claim text.