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Novel crystalline polymorph of venlafaxine hydrochloride and methods for the preparation thereof

a technology of venlafaxine hydrochloride and crystalline polymorphism, which is applied in the field of new crystalline polymorphism of venlafaxine hydrochloride, can solve the problem of no inhibitory activity of monoamine oxidas

Inactive Publication Date: 2006-04-06
WYETH LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0010] The present invention provides a novel anhydrous crystalline polymorph of venlafaxine hydrochloride. This crystalline polymorph is more thermally stable than known forms of venlafaxine hydrochloride. While forms I and II of venlafaxine hydrochloride have melting points of 209 and 211° C. ΔH=125.8 and 130.3 J / g), respectively, the melting point of the crystalline polymorph of the present invention is about 219° C. ΔH=116 J / g). Because of this stability, a mixture of various polymorphs of venlafaxine hydrochloride can be formed into a pure form of this new polymorph. Furthermore, residual solvents used in the preparation of this new polymorph or the precursor venlafaxine hydrochloride can be easily removed.

Problems solved by technology

However, it has no inhibitory activity on monoamine oxidase.

Method used

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  • Novel crystalline polymorph of venlafaxine hydrochloride and methods for the preparation thereof
  • Novel crystalline polymorph of venlafaxine hydrochloride and methods for the preparation thereof
  • Novel crystalline polymorph of venlafaxine hydrochloride and methods for the preparation thereof

Examples

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example 1

Preparation of Anhydrous Venlafaxine Hydrochloride

[0039] About 100 mg of venlafaxine hydrochloride of Form II was put in a glass vial, flushed with nitrogen gas and then sealed by heat. The sealed vial was put in an oil bath at about 200° C. (197° C. to 200° C.) for 1 hour or until the shape of the crystals changed to form cream-white crystals.

example 2

Preparation of Anhydrous Venlafaxine Hydrochloride

[0040] The procedure in Example 1 was repeated with 500 mg of venlafaxine hydrochloride of Form II, except the vial was left in the oil bath for 2.5 hours instead of 1 hour.

example 3

Preparation of Anhydrous Venlafaxine Hydrochloride

[0041] The procedure in Example 1 was repeated, except an aluminum vial was used instead of a glass vial.

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Abstract

This invention relates to a highly thermally stable novel anhydrous crystalline polymorphic form of venlafaxine hydrochloride, methods for the preparation thereof, and its use.

Description

[0001] This application is a divisional of copending U.S. application Ser. No. 10 / 308,480, filed on Dec. 3, 2002, which claims benefit to Provisional Application No. 60 / 335,822, filed on Dec. 5, 2001, the entire disclosure of which is hereby incorporated by reference.FIELD OF THE INVENTION [0002] This invention relates to a novel highly thermally stable anhydrous crystalline polymorphic form of venlafaxine hydrochloride, methods for the preparation thereof, and its use. BACKGROUND OF THE INVENTION [0003] Venlafaxine (1-[2-(dimethylamino)-1-(4-methoxyphenyl)ethyl]cyclohexanol) and its therapeutically acceptable salts (collectively referred to as venlafaxine herein) are inhibitors of monoamine neurotransmitter uptake, a mechanism associated with clinical antidepressant activity. This mechanism has also been associated with reproductive function by affecting indirectly the hypothalamic-pituitary-ovarian axis. It is believed that venlafaxine's mechanism of action is related to potent in...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/137A61P25/22A61P25/00A61P25/24C07C213/10C07C217/64C07C217/74
CPCA61K31/137C07C2101/14C07C217/64C07C2601/14A61P25/00A61P25/22A61P25/24C07C217/74A61K31/135
Inventor ALI, KADUM ABDUL NABIHAN, JUNLEE, YONG JAI
Owner WYETH LLC