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Single‐ and Multiple‐Dose Pharmacokinetics and Dose Proportionality of the Psychotropic Agent Paliperidone Extended Release
Author(s) -
Boom Sandra,
Talluri Krishna,
Janssens Luc,
Remmerie Bart,
Meulder Marc,
Rossenu Stefaan,
Osselaer Nancy,
Eerdekens Marielle,
Cleton Adriaan
Publication year - 2009
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/0091270009339190
Subject(s) - paliperidone , paliperidone palmitate , pharmacokinetics , pharmacology , dosing , risperidone , medicine , bioequivalence , chemistry , schizophrenia (object oriented programming) , psychiatry
Paliperidone extended‐release tablet (paliperidone ER) is a centrally active dopamine D 2 ‐ 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.