Bioequivalence study of baicalin tablets in healthy volunteers by HPLC-MS/MS

Objective To develop a high performance LC-tandem mass spectrometry(HPLC-MS/MS) method to study the pharmacokinetics and bioequivalence of baicalin in healthy volunteers.Methods According to a randomized crossover design,a single oral dose of 0.50 g baicalin(test or reference) was given to 18 healthy volunteers.The concentration of baicalin in the plasma was detected by HPLC-MS/MS.The main pharmacokinetic parameters were calculated to evaluate the bioequivalence of the 2 preparations.Results The pharmacokinetic parameters of test and reference preparation were as follows: AUC0~16 was(1 251.7±836.1)and(1 191.7±644.0) ng·h·mL-1,AUC0~∞ was (1 501.2±978.7) and(1 445.3± 866.1) ng·h·mL-1,Cmax was(207.9±128.9) and(218.1±129.3) ng·mL-1,tmax was(8.4±2.8) and(8.4±3.0) h,t1/2 was(3.7±1.3) and(3.5±1.5) h.The relative bioavailability of baicalin based on the AUC0~16 data was(103.5±20.6)%.Conclusion This method is rapid,highly sensitive and accurate,and suitable for the pharmacokinetic study of baicalin.The two formulations are bioequivalent.