Aqueous suspensions of submicron 9-hydroxyrisperidone fatty...

A - Human Necessities – 61 – K

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Details

A61K 31/519 (2006.01) A61K 9/10 (2006.01) A61K 9/14 (2006.01) A61P 25/00 (2006.01)

Patent

CA 2309629

The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramus-cular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxy-risperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof in submicron form and (2) a pharmaceuticall acceptable carrier, wherein the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein: and with a process of preparing such a composition. The invention further concerns such a pharmaceutical composition for use as a medicament in the treatment of psy-chosis, schizophrenia, schizoaffective disorders, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, Tourette's syndrome, bipolar mania, depression, anxiety.

Cette invention se rapporte à une composition pharmaceutique utilisable comme formulation de dépôt pour une administration par injection intramusculaire ou sous-cutanée comprenant: (1) comme principe actif une quantité thérapeutiquement efficace d'un ester d'acide gras de 9-hydroxy-rispéridone, ou d'un sel, ou d'un stéréo-isomère ou d'un mélange stéréo-isomère de cet ester, sous la forme de particules de l'ordre du sous-micron; et (2) à un excipient acceptable sur le plan pharmaceutique qui est constitué par de l'eau et dans lequel le principe actif est mis en suspension. Outre un procédé de préparation d'une telle composition, cette invention concerne également une composition pharmaceutique utilisable comme médicament dans le traitement des psychoses, de la schizophrénie, des troubles schizo-affectifs, des psychoses non schizophrènes, des troubles du comportement associés aux maladies neurodégénératives, telles que la démence, les troubles du comportement dans l'arriération mentale et l'autisme, le syndrome de Tourette, les manies bipolaires, la dépression, l'anxiété.

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