Single-dose and multi-dose pharmacokinetics and bioavailability of ofloxacin sustained-release tablets in healthy volunteers

AIM:To study the single-dose and multi-dose pharmacokinetics and bioavailability of ofloxacin sustained-release tablets in healthy volunteers.METHODS:The plasma concentrations of ofloxacin were determined by a RPHPLC method.The reference or test preparation was given to healthy male volunteers according to an open randomized crossover study. The pharmacokinetic parameters and bioavailability of test preparation were compared with reference preparation.RESULTS:The main pharmacokinetic parameters of the test preparation and the reference preparation,the single-dose were as follows:Cmax were(5382± 1558)and(3419±1034)μg/L,Tmax were(1.7±0.6)and(4.2±1.8)h,t1/2 were(8.2±1.0)and(7.6± 1.8)h,MRT were(8.6±0.9)and(10.3±1.4) h;AUC0-t were(33764±5297)and(31280± 4412)μg·L-1·h,AUC0→∞ were(34643± 5356)and(32642±4257)μg·L-1·h.The relative bioavailability of reference to test preparation was(97.9±12.4)%.There were statistical-ly significant difference about Cmax,Tmax,MRT between the reference preparation and test preparation,but there were no statistically significant difference about t1/2,AUC0-t,AUC0→∞. The 90% confidence limit of AUC0-t and AUC0→∞ between the reference preparation and test preparation were 89.0%- 97.0% and 91.4%-97.8% respectively.The multi-dose were as follows:Cmax were(3732±1502)and(3564±982)μg/L,Cmin were(750±193),(438 ±89)μg/L,Tmax were(1.5±0.5)and(3.7± 1.7)h,AUCSS were(32689±4786)and(33591 ±7929)μg·L-1·h,Cav were(1362±199)and(1405±337)μg/L,DF were(216±76)and(222 ±34)%.The relative bioavailability of reference to test preparation was(102.9±22.5)%.There were no statistically significant difference about Cmax,Cav,AUCSS,DF between the reference preparation and test preparation.The 90%confidence limit of Cmax,AUCSS,Cav and DF were 80.8%-114.6%,89.3%-111.9%,89.5%-112.4% and 93.7%-122.4%.CONCLUSION: The results of statistics analysis showed that the test preparation exhibited sustained-release characteristics,and it was bioequivalent between the test preparation and the reference preparation.