Single-dose pharmacokinetics of paliperidone extended-release tablets in healthy Chinese subjects.
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.
Si
Tianmei
T
Department of Clinical Psychopharmacology, Peking University Institute of Mental Health, Haidian District, Beijing, China. si.tian-mei@163.com
Shu
Liang
L
Liu
Yi
Y
Su
Yun' Ai
YA
Guo
Chunmei
C
Zhang
Hongyan
H
D000284:Administration, Oral; D000328:Adult; D014150:Antipsychotic Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D019540:Area Under Curve; D002681:China; D003692:Delayed-Action Preparations; D004311:Double-Blind Method; D005260:Female; D006207:Half-Life; D006801:Humans; D007555:Isoxazoles / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D008297:Male; D000068882:Paliperidone Palmitate; D011743:Pyrimidines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D014018:Tissue Distribution; D055815:Young Adult
D014150:Antipsychotic Agents; D003692:Delayed-Action Preparations; D007555:Isoxazoles; D011743:Pyrimidines; D000068882:Paliperidone Palmitate