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Background:Posaconazole (POS) is a broad-spectrum triazole antifungal compound.Systemic exposure is enhanced by approximately 2.6- to 4-fold when POS oral suspension is taken with a nutritional supplement or high-fat meal compared with fasting state.The current study was designed to evaluate safety and tolerability and to determine the relative bioavailability of POS oral suspension under fasting and fed conditions when given to healthy Chinese subjects.Objective: This study was to determine the relative availability of POS suspension and to evaluate the safety and tolerability following single-dose administration with fast or high-fat food in Chinese healthy subjects.Methods: This was a randomized,open-label,single-dose,2 × 2 crossover study.Twelve healthy subjects received one dose of POS oral suspension (5 mL; 200 mg) while fasting or with a high-fat Chinese meal.Plasma concentrations of POS were measured through 120 h after dosing.The measured plasma concentration data were calculated with a noncompartment model,while Cmax and Tmax were measured values.The pharmacokinetic parameters were statistically analyzed using a crossover analysis of variance model.Relative bioavailability based on log-transformed data was expressed as the ratio of the AUC estimates for the suspension in the fed and fasting states.Safety assessments were conducted throughout the study.Results: Of the 12 enrolled subjects,4 were females with a mean age of 22.5 years.Mean Cmax values were 128.02 and 354.29 ng/mL,for fasting and fed conditions,respectively,and corresponding mean AUC0-t values were 3075.27 and 12,229.08 ng · h/mL.Food enhanced exposure with a relative bioavailability of 510% (AUC).Conclusions: Similar to results of previous studies in other populations,significant differences in AUC,Cmax,and Tmax (P< 0.05) were found in Chinese subjects who received oral POS suspension while fasting and after a high-fat meal.The high-fat meal increased Cmax by 3.58-fold and AUC by 5.10-fold,as well as significantly influencing the rate and extent of absorption.A single dose of oral POS suspension was safe and well tolerated in healthy Chinese subjects.