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Keywords:

  • Chinese;
  • paliperidone ER;
  • pharmacokinetics;
  • tolerability

Abstract

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/m2 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 tmax: 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. Cmax, AUC0-t, and AUC0-∞ were dose-dependent. Pharmacokinetics was linear with respect to time; Geometric mean t1/2 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. Copyright © 2010 John Wiley & Sons, Ltd.