DrugPatentWatch Database Preview
« Back to Dashboard
Summary 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)|
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.
For more information try a trial or see the plans and pricing
Serving leading biopharmaceutical companies globally:
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.