Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects

ObjectiveThe objective of this study was to characterize the pharmacokinetics of 25, 100, and 150mg equivalents (eq.) of paliperidone long-acting injection in Chinese subjects with schizophrenia. MethodsThis was an open-label, randomized, parallel group, multicenter study. A total of 48 patients were randomized in a 1:1:1 ratio to one of three groups. Sequential blood samples were collected immediately before injection on day1 and up to 210days after the first injection. The plasma paliperidone concentrations were determined by a validated high-performance liquid chromatography/tandem mass spectrometry method. ResultsA total of 47 patients received at least one injection of the study medication, and 43 completed the study. The pharmacokinetic (PK) parameters, such as time to maximum concentration, t1/2, and CL/F, were comparable across the three treatment groups (p=0.935, 0.349, and 0.794, respectively). The differences in maximum plasma concentration, AUC (035days), AUC (0-210days), and AUC (0-) were significant (p<0.001) and dose proportional. The inter-individual variation of PK parameters was large. The most frequent treatment-emergent adverse events were prolactin level increasing, injection site pain, tremor, dry mouth, and constipation. ConclusionsThe pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150mg eq. Copyright (c) 2014 John Wiley & Sons, Ltd.http://gateway.webofknowledge.com/gateway/Gateway.cgi?GWVersion=2&SrcApp=PARTNER_APP&SrcAuth=LinksAMR&KeyUT=WOS:000333015700012&DestLinkType=FullRecord&DestApp=ALL_WOS&UsrCustomerID=8e1609b174ce4e31116a60747a720701Clinical NeurologyPharmacology & PharmacyPsychiatryPsychologySCI(E)PubMed3ARTICLEsi.tian-mei@163.com2203-2102