A single-dose, open-label, parallel, randomized, dose-proportionality study of paliperidone after intramuscular injections of paliperidone palmitate in the deltoid or gluteal muscle in patients with schizophrenia

摘要

Paliperidone palmitate (PP) is a long-acting injectable (LAI) antipsychotic, developed for monthly intramuscular (i.m.) administration into deltoid/gluteal muscle, approved for the treatment of schizophrenia in many countries. To assess the options for i.m. injection sites, dose-proportionality of PP was investigated after injection of a single dose (25-150mgeq.) of PP in either gluteal (n=106) or deltoid (n=95) muscle of schizophrenic patients. Overall, mean (geometric) area under plasma concentration-time curve from time zero to infinity (AUC∞) of paliperidone increased proportionally with increasing PP doses, regardless of injection site. Mean maximum plasma concentration (Cmax) was slightly less than dose-proportional for both injection sites at PP doses 50mgeq. Mean C max was higher after injection in the deltoid compared with the gluteal muscle, except for the 100mgeq. dose, while AUC∞ for both injection sites was comparable at all doses. Median time to reach C max (tmax) ranged from 13-14 days after deltoid and 13-17 days after gluteal injection across all doses. Single PP injections in deltoid and gluteal muscles in the dose range of 25-150mgeq. were generally tolerable both locally and systemically.