Injectable depot formulation comprising crystals of iloperidone
AssigneeNovartis AG
InventorsDierk Wieckhusen, Alexandra Glausch, Markus Ahlheim
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Abstract
An injectable depot formulation comprising crystals having structure (I) wherein R is (FII) and the X50 value of the crystals is from 1 to 200 microns. Depot formulations containing crystals of iloperidone or its metabolites have the following advantages: (i) release of the crystals in plasma can be correlated with the size of the crystals; (ii) absorption of the crystals in plasma can be correlated with the size of the crystals; (iii) the particle size of the crystals can be controlled by crystal engineering and/or milling; and (iv) the crystals are stable upon storage, and stable to sterilization procedures, such as gamma irradiation.
Claims17
An injectable depot formulation comprising about 100 to about 750 mg of crystals of iloperidone or of its metabolite, suspended in an aqueous suspension, wherein the X50 value of the crystals is from 1 to 200 microns, which formulation, following administration to a patient suffering a psychotic disorder by subcutaneous or intramuscular injection, provides an effective treatment amount over a period of about 2 to about 8 weeks.
Dependencies are inferred from the claim text.