Stable micronised monoclin form of asenapine maleate and its synthesis

摘要

A stable micronized monoclinic form of asenapine maleate is described, which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterized by a d90 equal to or below 40 μm. Processes for preparing the stable micronized monoclinic form of asenapine maleate are also described. Formula (I).;

主权项

1. A process for the preparation of a stable micronised monoclinic form of asenapine maleate which comprises 5% by weight or less of orthorhombic form or any other crystalline form of asenapine maleate, wherein the asenapine maleate has a particle size distribution characterised by a d90 equal to or below 40 μm, and which remains polymorphically stable after 3 months of storage, the process comprising the micronisation of monoclinic asenapine maleate wherein the applied micronisation pressure is below 7 bar and the micronisation temperature is 10° C. or below.