Pharmacokinetics and Relative Bioavailability of Zaleplon Tablet in Healthy Volunteers after A Single Oral Administration

OBJECTIVE:To study the pharmacokinetics and relative bioavailability of zaleplon in 20 healthy volunteers. METHODS:A single oral dose 10mg zaleplon of reference or test drugs was given to each volunteer according to an open randomized crossover study. The concentrations in plasma were determined by HPLC-ESI-MS method after liquid-liquid extraction methods. RESULT:The main pharmacokinetics parameters of zaleplon were as follows: rt/2were 1.17±0.19h and 1.14±0.12h, tmax were 0.83 ± 0.12h和0.91± 0.12h, Cmax were 28.47 ± 2.62mg.L-1 and 28.12 ± 3.44mg.L-1, AUC0-8 were 52.83 ± 4.81mg.h-l-1 and 54.92± 8.83mg.h.L-1 for test tablet and reference capsule, respectively. The relative bioavailability of F0-8 and F0-∞ were (98.3 ± 16.5) % and (98.0 ± 16.4) %, respectively . CONCLUSION':The result of statistical analysis showed that two formulations were bioequivalent.