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Claims for Patent: 6,077,843

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Claims for Patent: 6,077,843

Title: Aqueous suspensions of 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-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.
Inventor(s): Fran.cedilla.ois; Marc Karel Jozef (Kalmthout, BE), Embrechts; Roger Carolus Augusta (Oud-Turnhout, BE), Borghijs; Herman Karel (Willebroek, BE), Monbaliu; Johan (Turnhout, BE)
Assignee: Janssen Pharmaceutica, N.V. (Beerse, BE)
Application Number:09/180,659
Patent Claims: 1. A pharmaceutical composition in the form of a depot formulation for administration by intramuscular or subcutaneous injection, comprising:

(1) as an active ingredient a therapeutically effective amount of a 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.9-19 alkyl radical; and

(2) a pharmaceutically acceptable carrier;

characterized in that the pharmaceutically acceptable carrier is water and the active ingredient is suspended therein.

2. A composition according to claim 1 wherein R represents a straight C.sub.15 (pentadecyl) chain and the active ingredient is 9-hydroxyrisperidone palmitate ester.

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

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

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

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

7. 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 active ingredient;

(b) from 0.05 to 0.2% (w/v) of a wetting agent;

(c) from 0.5 to 2% (w/v) of a suspending agent;

(d) up to 2% (w/v) preservatives;

(e) optionally one or more isotonizing agents sufficient to render the composition isotonic with serum; and

(f) water q.s. ad 100%.

8. A process of preparing a pharmaceutical composition as claimed in claim 1 comprising intimately mixing the active ingredient with the carrier.

9. A process according to claim 8 comprising the steps of:

(a) stirring the wetting agent with the water;

(b) adding the preservative to the mixture while stirring;

(c) dispersing the suspending agent in the mixture while stirring;

(d) optionally dissolving the isotonizing agent in the mixture while stirring;

(e) dispersing the active ingredient in the mixture while stirring, followed by homogenizing the mixture.

10. A method of treating a warm-blooded animal suffering from a disorder selected from schizophrenia, non-schizophrenic psychoses, behavioral disturbances associated with neurodegenerative disorders, e.g., dementia, behavioral disturbances in mental retardation and autism, bipolar mania, depression, or anxiety, comprising administering to the warm-blooded animal a therapeutically effective amount of the composition of claim 1.
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