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Single- and Multiple-Dose Pharmacokinetics and Dose Proportionality of the Psychotropic Agent Paliperidone Extended Release

From Johnson & Johnson Pharmaceutical Research & Development, Beerse, Belgium (Dr Boom, Mr Janssens, Dr Remmerie, Dr De Meulder, Dr Rossenu, Dr van Osselaer, Dr Eerdekens, and Dr Cleton); and Johnson & Johnson Pharmaceutical Research & Development, Titusville, New Jersey (Dr Talluri).

Paliperidone extended-release tablet (paliperidone ER) is a centrally active dopamine D₂- and serotonergic 5-HT_2A-receptor antagonist that is registered for the treatment of schizophrenia. The controlled rate of release of paliperidone from the ER formulation is designed to have a slower absorption rate, which results in gradual ascending plasma concentrations with observed maximum plasma concentrations occurring at 24 hours after dosing on the first dosing day. On subsequent treatment days, the ER formulation provides minimal fluctuations in plasma concentrations. Paliperidone is eliminated with a terminal half-life of approximately 24 hours. Steady state is achieved after 4 daily doses. Paliperidone ER exhibits time-invariant pharmacokinetics. It shows a 3.5-fold accumulation upon steady state, mainly caused by the controlled release characteristics of the formulation. Paliperidone ER displays dose proportionality over the dose range of 3 to 15 mg; the 90% confidence intervals of the pairwise dose comparisons are all included in the 80% to 125% bioequivalence limits.

Key Words: Paliperidone • pharmacokinetics • dose proportionality

Address for reprints: Nancy van Osselaer, Johnson & Johnson Pharmaceutical Research & Development, a division of Janssen Pharmaceutica NV, Turnhoutseweg 30, B-2340 Beerse, Belgium; e-mail: nvossela{at}its.jnj.com.

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