Pharmacokinetics and bioequivalence of Ligustazine phosphate pills in healthy volunteers

Objective To study the pharmacokinetics and bioequivalence of Ligustazine phosphate pills (test) and its tablet ( reference) in 20 Chinese healthy male volunteers. Methods A single oral dose 300 mg Ligustazine phosphate of test or reference formulations was given to each volunteer according to an open randomized crossover design. The Ligustazine phosphate concentrations in serum were determined by HPLC with UV detection method. The pharmacokinetic parameters were determined by BAPP 2. 0 program and bioequivalence were compared. Results The main pharmacokinetic parameters of Ligustazine phosphate were as the following:Cmax were (4. 50 ±0.96) and (4.45 ±1.69)μg·mL-1,tmax were (0.5 ±0.2) and (0.8 ±0.3) h, t1/2 were (1.32 ±0.24) and (1. 30 ±0. 22)h, MRT were (1.94 ±0.26) and (2. 02 ±0. 22) h, AUC0-8 were (6. 88 ±1.71) and (6.71 ±1.25)μg·h·mL-1, AUC0-∞ were (7.01 ±1.76) and (6.82 ±1. 27) μg·h·mL-1 for test and reference, respectively. The relative bioavailability of test to reference drug were (102. 7 ± 18. 6) %. Conclusion The results of statistical analysis showed that two formulations were bioequivalent.