Effect of food on the pharmacokinetic profile of baicalein chewable tablets in healthy volunteers / 中国药学杂志

ABSTRACT

OBJECTIVE: To characterize the effects of food intake on the pharmacokinetic (PK) profile of oral baicalein chewable tablets at dose of 400 mg. METHODS: In this randomized, 2-way crossover, placebo-control study, 12 healthy adult volunteers were assigned to receive a single dose of baicalein 400 mg or placebo after an overnight fast (fasted condition) or high-fat breakfast (fed condition). Concentrations of baicalein and its major metabolite baicalin in plasma were measured using HPLC-MS/MS. PK parameters were analyzed and safety was assessed. RESULTS: The pharmacokinetic parameters of baicalein in fasted and fed states were as follows ρmax(15.752 ± 9.328) vs (19.572 ± 9.439) ng · mL-1; AUC0-t(89.468 ± 48.631) vs (122.073 ± 28.285) ng · h · mL-1; AUC0-∞(93.356 ± 50.110) vs (126.212 ± 28.270) ng · h · mL-1. The pharmacokinetic parameters of baicalin in fasted and fed states were as follows ρmax(182.472 ± 99.555) vs (154.782 ± 10.834) ng · mL-1; AUC0-t(1 193.230 ± 693.408) vs (933.921 ± 282.318) ng · h · mL-1; AUC(0-∞) (1 266.425 ± 866.664) vs (940.882 ± 286.192) ng · h · mL-1. CONCLUSION: There suits of this study show that an increase in systemic exposure is observed for baicalein and a decrease in exposure is observed for baicalin when baicalein was taken with food. Baicalein 400 mg was generally well tolerated, with comparable adverse events in both the fed and the fasted states. The increase in exposure did not appear to impact the tolerability of the formulation.