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AMORPHOUS FORM OF ASENAPINE MALEATE

IP.com Disclosure Number: IPCOM000179473D
Publication Date: 2009-Feb-13
Document File: 3 page(s) / 88K

Publishing Venue

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Abstract

Amorphous form of asenapine maleate and pharmaceutical compositions comprising the novel amorphous form of asenapine maleate are reported.

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AMORPHOUS FORM OF ASENAPINE MALEATE

Abstract

Amorphous form of asenapine maleate and pharmaceutical compositions comprising the novel amorphous form of asenapine maleate are reported.

Formula I

Asenapine maleate (ORG 5222) chemically is trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole maleate of Formula I and disclosed in U.S. Patent No. 4,145,434 (hereinafter referred to as U.S. ‘434 patent).  

The present disclosure provides amorphous asenapine maleate and process for preparation thereof.

The X-ray powder diffractograms (XRPD) were recorded on a PANalytical X’pert Pro instrument.  The measurements were done using CuKα radiation at 45kV/40mA X-Ray tube settings.

The Infra-red (IR) spectra were recorded on a Perkin Elmer Spectrum One FT-IR instrument using KBr pellets.

Figure 1 depicts the XRPD of amorphous asenapine maleate.

Figure 2 depicts the IR of amorphous asenapine maleate.

The amorphous form of asenapine maleate can be prepared by using a process that comprises the recovery of solvent from a solution having asenapine maleate. The asenapine maleate used herein above in this aspect as starting material can be prepared by following any reported method, for example, the method described in US ‘434. Crystalline asenapine maleate can be used for the purpose.

The solvent used herein is any solvent which is capable to dissolve asenapine maleate. The solvent comprises organic solvent or mixtures thereof.  By way to define this aspect of the disclosure, present authors like to specify some of the organic solvents, mentioned below, but these are not intended to limit the scope of the disclosure.  These includes alkanols such as methanol, ethanol, n-propanol, isopropanol, n-butanol, isobutanol, tert-butanol, 2-pentanol, d...