FORMULATION AND IN VIVO PHARMACOKINETIC STUDIES OF ILOPERIDONE DEPOT INJECTION
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Iloperidone is a new antipsychotic agent having a good tolerability and side-effects profile with respect to long term drug administration. Presently, it is only available as tablet dosage forms of 1-12 mg strengths for twice a day administration. This article reports the pharmacokinetic studies of a novel in situ depot injection formulation of iloperidone developed for once a month administration. The formulation is based on the use of sucrose acetate isobutyrate as gelling agent for depot formation in situ. It is simple to prepare, possesses an acceptable syringeability and exhibits a controlled and consistent zero order drug release in vitro for one month. The in vivo pharmacokinetic studies performed in male albino Wistar rats for one month showed a mean peak plasma drug concentration of 871.8 ng/ml in 3 days, mean residence time of 28.9 days, terminal half-life of 24 days, and a terminal elimination rate-constant of 0.0289/day. The plasma concentration profile of the developed formulation demonstrated a persistent plasma level of iloperidone for one month without any significant burst release and with a good in vitro - in vivo correlation.
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