Pharmacokinetics of oxatomide tablets in healthy Chinese volunteers

The pharmacokinetics of oxatomide tablets in healthy Chinese volunteers after single and multiple-dose oral administration and the effect of food on it were studied.Single-dose study was carried out according to a replicated 3×3 Latin square design,with 12 volunteers orally receiving test tablets in single dose of 30 mg,60 mg and 120 mg,respectively.Blood samples were collected at specified time intervals up to 48 hours.The washout interval was 1 week.Multiple-dose study was carried out according to a 1-period design.Each volunteer orally received 30 mg oxatomide tablet twice daily (at 7:00 and 19:00) until the morning of the 7th day.Venous blood (4.0 mL) was drawn at the 5th and 6th mornings before administration to make sure that the steady state has appeared.On the 7th day,blood samples were collected again following the pre-specified time points after the last dose up to 48 h.After a washout period of 1 week,food effect was studied out according to an open,randomized,2-period crossover design.Oxatomide tablets (30 mg) were administered in fasting or eating state.The washout period was 1 week.Blood samples were collected at specified time intervals up to 48 hours.The plasma concentration-curves of oxatomide in this pharmacokinetic study were determined by a validated HPLC-MS method.The main pharmacokinetic parameters were calculated by software DAS 2.0.The validated method was proved to be simple,sensitive and rapid.The results exhibited that the absorption and disposition of oxatomide in human body followed the first order kinetics.There was no statistically significant difference between the phamacokinetic parameters of multiple- and single-dose study,which demonstrated that there was basically no accumulation of oxatomide in multiple-dose study.Food would affect the absorption rate of oxatomide,but not the extent of its absorption.