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Updated: Jun 11, 2026

An Intestine/Liver Microphysiological System for Drug Pharmacokinetic and Toxicological Assessment
Published on: December 3, 2020
Single-dose pharmacokinetics of paliperidone extended-release tablets in healthy Chinese subjects
Tianmei Si1, Liang Shu, Yi Liu
1Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Haidian District, Beijing, China. si.tian-mei@163.com
Objective:
Paliperidone is the active metabolite of risperidone. This single-center, double-blind, randomized, single-dose study characterized the pharmacokinetics of 3 mg and 9 mg of paliperidone ER OROS in healthy Chinese subjects.
Methods:
24 subjects (13 male, 11 female), aged 19-35 years, with a BMI of 19.0-24.6 kg/m(2) participated. Blood samples were collected immediately before and over 96 h following single oral doses of 3 mg and 9 mg paliperidone. Plasma paliperidone concentrations were determined, and pharmacokinetic parameters were analyzed.
Results:
Paliperidone's disposition after oral administration was characterized by a one-compartment pharmacokinetic model. Paliperidone was well absorbed (median t(max): 24 h after a 3-mg dose, and 26 h after a 9-mg dose). Apparent clearance and apparent volume of distribution were not significantly different between the two doses. C(max), AUC(0-t), and AUC(0-infinity) were dose-dependent. Pharmacokinetics was linear with respect to time; Geometric mean t(1/2) was 22.8 h and 21.4 h in 3-mg and 9-mg groups, respectively. No clinically significant safety issues were identified.
Conclusions:
The pharmacokinetic results obtained in Chinese subjects were similar to those obtained in Japanese and Caucasian subjects.
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