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. (c) 2010 John Wiley & Sons, Ltd.
RCT Entities:
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. (c) 2010 John Wiley & Sons, Ltd.
Authors: Hiroko Shimizu; Martine Neyens; Marc De Meulder; Srihari Gopal; Yuko Tsukamoto; Mahesh N Samtani; Bart Remmerie Journal: Clin Pharmacol Drug Dev Date: 2019-12-25