New stable polymorphic forms of olanzapine, useful for treating psychotic conditions, mild anxiety and gastrointestinal conditions

摘要

Process for producing a polymorph of olanzapine comprises dissolving an initial polymorph of olanzapine (2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine) in aqueous acid solution and precipitating a different polymorph of olanzapine by neutralization with an aqueous or alcoholic solution of base. Independent claims are also included for: (1) a form III olanzapine polymorph with defined x-ray diffraction pattern interplanar d-spacings; (2) a form IV olanzapine polymorph with defined x-ray diffraction pattern interplanar d-spacings; (3) a form V olanzapine polymorph with defined x-ray diffraction pattern interplanar d-spacings; and (4) a pharmaceutical formulation containing at least 1 form III, form IV or form V olanzapine polymorph (all with defined x-ray diffraction patterns) or their salts or mixtures. ACTIVITY : Gastrointestinal; tranquilizer; anxiolytic; neuroleptic. MECHANISM OF ACTION : None given.