ObjectiveThe aim of the study was to better understand blonanserin population pharmacokinetic (PK) characteristics in Chinese healthy subjects.MethodsData from two studies with 50 subjects were analyzed to investigate the population PK characteristics of blonanserin at single dose (4, 8, and 12 mg) under fasting, multidose (4 mg bid or 8 mg qd for 7 days) and under food intake condition (single dose, 8 mg). Blonanserin plasma concentrations were detected using the high performance liquid chromatography tandem mass spectrometry (LC/MS/MS). A nonlinear mixed‐effects model was developed to describe the blonanserin concentration–time profiles.ResultsA two compartment model with first‐order absorption was built to describe the time‐course of blonanserin. The population‐predicted system apparent clearance (CL/F), volume of apparent distribution in center (V1/F), and the first‐order absorption rate constant (Ka) of blonanserin under fasting was 1230 L/h, 9500 L, and 3.02 h−1, respectively. Food intake decreased Ka of blonanserin to 0.78 h−1. The relative bioavailability between fasting and food intake estimated by the final model was 55%. No clinically significant safety issues were identified.ConclusionThis is the first study assessing the PK profile of blonanserin with population PKs method. The results can be used for simulation in further clinical trial and optimize individual dosage regimens using a Bayesian methodology in patients. Copyright © 2013 John Wiley & Sons, Ltd.