Aqueous suspensions of 9-hydroxyrisperidone fatty acid esters

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/505 (2006.01) A61K 31/517 (2006.01) A61K 47/00 (2006.01) A61K 47/02 (2006.01) A61K 47/10 (2006.01) A61K 47/26 (2006.01) A61K 47/38 (2006.01)

Patent

CA 2236691

The present invention is concerned with a pharmaceutical composition suitable as a depot formulation for administration via intramuscular or subcutaneous injection, comprising: (1) as an active ingredient a therapeutically effective amount of a 9-hydroxyrisperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof and (2) a pharmaceutically 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 schizophrenia, non-schizophrenic psychoses, behavioural disturbances associated with neurodegenerative disorders, e.g. in dementia, behavioural disturbances in mental retardation and autism, bipolar mania, depression, anxiety.

L'invention concerne une composition pharmaceutique convenant comme formulation à effet retard à administrer par injection intramusculaire ou sous-cutanée, qui comprend: (1) comme principe actif une quantité thérapeutiquement efficace d'un ester ou d'un sel d'un acide gras de 9-hydroxy-risperidone, ou un stéréo-isomère ou un mélange stéréo-isomérique de ceux-ci; et (2) un support pharmaceutiquement acceptable, ledit support étant l'eau et le principe actif étant en suspension dans l'eau. L'invention concerne également un procédé permettant de fabriquer ladite composition. Elle concerne enfin une composition pharmaceutique destinée à être utilisée comme médicament pour traiter la schizophrénie, les psychoses non schizophréniques, les troubles comportementaux associés à des troubles neurodégénératifs, par exemple dans la démence, les troubles comportementaux associés aux retard mental et à l'autisme, la psychose maniaco-dépressive, la dépression et l'angoisse.

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