Abstract: 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 RP-HPLC 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: C_max were (5382± 1558)and (3419±1034) μg/L, T_max were (1.7±0.6)and(4.2±1.8) h, t_1/2 were(8.2±1.0) and(7.6±1.8) h, MRT were(8.6±0.9) and(10.3±1.4) h;AUC_0-t were (33764±5297) and(31280±4412) μg·L^-1·h,AUC_0→∞ 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 statistically significant difference about C_max,T_max,MRT between the reference preparation and test preparation, but there were no statistically significant difference about t_1/2,AUC_0-t,AUC_0→∞. The 90% confidence limit of AUC_0-t and AUC_0→∞ between the reference preparation and test preparation were 89.0%-97.0% and 91.4%-97.8% respectively. The multi-dose were as follows: C_max were (3732±1502)and (3564±982) μg/L, C_min were (750±193),(438±89) μg/L,T_max were (1.5±0.5) and(3.7±1.7) h, AUC_SS were (32689±4786) and(33591±7929) μg·L^-1·h, C_av 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 C_max,C_av,AUC_SS, DF between the reference preparation and test preparation. The 90% confidence limit of C_max, AUC_SS,C_av 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.

Key words: Ofloxacin sustained-release tablet, High-performance liquid chromatography, Pharmacokinetics, Bioavailability, Bioequivalent