Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects. (March 2014)

• Record Type: Journal Article
• Authors: Si, Tianmei; Su, Yun'ai; Liu, Yi; Zhang, Hongyan; Li, Huafang; Rui, Qing; Shu, Liang
• Is Part Of: Human psychopharmacology. Volume 29:Number 2(2014:Mar.)
• Page Start: 203
• Page End: 210
• Publication Date: 2014-03
• Subjects: Psychopharmacology -- Periodicals; Psychotropic drugs -- Periodicals; Psychopharmacology -- Periodicals; Psychotropic Drugs -- pharmacology -- Periodicals; 615.78
• DOI: 10.1002/hup.2388
• Languages: English
• ISSNs: 0885-6222

Abstract

<abstract abstract-type="main"> <title> <x xml:space="preserve">Abstract</x> </title> <sec id="hup2388-sec-0001" sec-type="section"> <title>Objective</title> <p>The objective of this study was to characterize the pharmacokinetics of 25, 100, and 150 mg equivalents (eq.) of paliperidone long‐acting injection in Chinese subjects with schizophrenia.</p> </sec> <sec id="hup2388-sec-0002" sec-type="section"> <title>Methods</title> <p>This 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 day 1 and up to 210 days after the first injection. The plasma paliperidone concentrations were determined by a validated high‐performance liquid chromatography/tandem mass spectrometry method.</p> </sec> <sec id="hup2388-sec-0003" sec-type="section"> <title>Results</title> <p>A 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 (<italic>p</italic> = 0.935, 0.349, and 0.794, respectively). The differences in maximum plasma concentration, AUC (035 days), AUC (0–210 days), and AUC (0–∞) were significant (<italic>p</italic> < 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.</p> </sec> <sec id="hup2388-sec-0004" sec-type="section"> <title>Conclusions</title> <p>The pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150 mg eq. Copyright © 2014 John Wiley & Sons, Ltd.</p> </sec> </abstract>