Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects.

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Pharmacokinetics and tolerability of paliperidone palmitate injection in Chinese subjects.

Hum Psychopharmacol. 2014 Mar;29(2):203-10

Authors: Si T, Su Y, Liu Y, Zhang H, Li H, Rui Q, Shu L

Abstract
OBJECTIVE: 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.
METHODS: 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.
RESULTS: 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 (p = 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 (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.
CONCLUSIONS: The pharmacokinetics of paliperidone palmitate are linear with respect to time in Chinese subjects with schizophrenia at injections from 25 to 150 mg eq.

PMID: 24590546 [PubMed - indexed for MEDLINE]