Abstract
PURPOSE: Although blonanserin is widely used in clinical practice, existing studies have shown significant variations in the magnitude of food effects on its pharmacokinetics. This study was conducted to evaluate the impact of food on the pharmacokinetics and safety of 4-mg blonanserin tablets in healthy Chinese subjects. METHODS: The findings were derived from a bioequivalence study in which subjects were randomly assigned to receive blonanserin tablets under fasting or fed conditions. Serial blood samples were collected and plasma concentrations of blonanserin were accurately determined using a validated high-performance liquid chromatography-mass spectrometry (HPLC-MS/MS). Pharmacokinetic parameters, including the maximum plasma concentration (C(max)), the area under the concentration-time curve from zero to the last quantifiable time point (AUC(0-t)), and the area under the concentration-time curve from zero to infinity (AUC(0-∞)) were estimated using the non-compartmental method and statistically analyzed by the BE module of WinNonLin. Safety assessments were performed throughout the study period. RESULTS: 106 healthy subjects were enrolled and divided into a fasted group and a fed group. The C(max), AUC(0-t) and AUC(0-∞) of blonanserin in plasma after a high-fat meal increased 5.23-fold, 4.77-fold and 4.82-fold, relative to the fasted conditions. The 90% confidence interval (90% CI) were outside the 80.00-125.00% range. The incidence of adverse drug reaction (ADR) was similar between the fasted group and the fed group, with the majority being mild in severity. CONCLUSION: The results revealed that a high-fat meal significantly increased blonanserin bioavailability by approximately 5-fold at the 4-mg dose. Blonanserin was well tolerated in most subjects under both fasting and fed conditions, and food intake did not significantly alter its safety profile. These findings highlight the need to consider food effects when determining clinical dosing regimens.