Pharmacokinetics and relative bioavailability study of roxithromycin tablet in Chinese healthy volunteers by LC-MS

Objective To study the pharmacokinetics and relative bioavailability of roxithromycin in Chinese healthy volunteers. Methods 20 male healthy volunteers randomly received a single crossover oral dose of 150 mg test tablet or reference tablet. The concentration of roxithromycin in plasma was determined by LC-MS. Results The method was linear in the range from 0.0111 mg/L to 11.14 μg/ml (r=0.9991). The relative bioavalability was more than 93% and the absolute bioavalability was more than 81%.The inter-day and intra-day RSD were less 10%.The main pharmacokinetic parameters of test and reference roxithromycin tablets were as following:Tmax:(2.1±1.4) and (2.2±1.5)h, Cmax:(5.8±1.8) and (6.1±2.0)μg/ml, AUC0~60 h:(80±28) and (84±28)mg·L-1·h-1, AUC0~∞:(83±30) and (87±30)mg·L-1·h-1, T1/2:(12.4±2.3) and (12.3±1.6)h, F0~60 h was (97±13)%. Conclusion The test roxithromycin tablet was bioequivalent to the reference tablet.