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Claims for Patent: 6,555,544

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Claims for Patent: 6,555,544

Title: Aqueous suspensions of submicron 9-hydroxyrisperidone fatty acid esters
Abstract: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-hydroxy-risperidone fatty acid ester or a salt, or a stereoisomer or a stereoisomeric mixture thereof in submicron form 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 psychosis, 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.
Inventor(s): Fran.cedilla.ois; Marc Karel Jozef (Kapellen, BE), Dries; Willy Maria Albert Carlo (Merksplas, BE), Basstanie; Esther Dina Guido (Zandhoven, BE)
Assignee: Janssen Pharmaceutica, N.V. (BE)
Application Number:09/530,687
Patent Claims: 1. A pharmaceutical composition suitable as a depot formulation for administration by intramuscular or subcutaneous injection, comprising a dispersion of particles consisting essentially of a therapeutically effective amount of a crystalline 9-hydroxyrisperidone fatty acid ester having the formula ##STR2##

or a salt, or a stereoisomer or a stereoisomeric mixture thereof, wherein R represents a straight C.sub.15 (pentadecyl) chain and the active ingredient is 9-hydroxyrisperidone palmitate ester; having a surfactant adsorbed to the surface thereof in an amount effective in maintaining a specific surface area >4 m.sup.2 /g (corresponding to an effective average particle size of less than 2,000 nm) in a pharmaceutically acceptable carrier comprising water.

2. A composition according to claim 1 wherein the composition further comprises a suspending agent, and optionally one or more of a preservative, a buffer and an isotonizing agent.

3. A composition according to claim 2 wherein the suspending agent is sodium carboxymethyl cellulose and the surfactant is polysorbate 20.

4. A composition according to ciaim 3 wherein the preservative is benzyl alcohol and the isotonizing agent is mannitol or a phosphate buffer.

5. A composition according to claim 1 having a viscosity of less than 75 mPa.multidot.s.

6. A composition according to claim 1 comprising by weight based on the total volume of the composition: (a) from 3 to 20% (w/v) of the 9-hydroxyrisperidone fatty acid ester having the formula or a salt, or a stereoisomer or a stereoisomer mixture thereof; (b) from 0.5 to 2% (+/v) of a wetting agent; (c) one or more buffering agents sufficient to render the composition neutral to very slightly basic (up to pH 8.5); (d) from 0.5 to 2% (w/v) of a suspending agent; (e) up to 2% (w/v) preservatives; and (f) water q.s. ad 100%.

7. A method for treating psychosis, schizophrenia, schizoaffective disorders, non-schizophrenic psychoses, behavioural disturbances associated with dementia, behavioural disturbances in mental retardation and autism, Tourette's syndrome, bipolar mania, depression, or anxiety in a warm-blooded animal in need thereof comprising administering to the animal a therapuetically effective amount of the composition of claim 1.
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