Pharmacokinetics and bioequivalence of cefaclor sustained release tablets in healthy volunteers

Objective To study pharmacokinetics and relative bioavailability of two cefaclor sustained release tablets in healthy volunteers. Methods Twenty healthy male volunteers took 375 mg cefaclor sustained-release tablet (the test product or the reference product) in a single and multiple oral dosing open label, randomized, two-way crossover study. Cefaclor concentrations in human plasma were determined by a sensitive liquid chromatographic - tandem mass spectrometric (LC/MS/MS) method. Results After a single oral dose administration, Cmax were 2.54 ± 0.89 mg·L-1 at 2.23 ±0.64 h for the test and 2.38 ± 0.65 mg1-1 at 2.05 ± 0.56 h for the reference. AUC0-t were 7.38 ± 1.66 and7.09 ± 1.71 mg·h·L-1,and t1/2 1.08 ± 0.12 and 1.07 ± 0.13 h for the test and reference, respectively. The relative bioavailability of the test was (105.0 ± 11.2)%. After multiple oral dose administration, for the test and the reference,Cmax were 2.61 ± 0.61 and2.34 ± 0.55 mg·L-1, Cmin were 3.48 ± 1.33 and 3.65 ± 1.23μ·L-1, Cav were 602 ± 114and 585 ± 128μg·L-1, and DF were 4.3 ± 0.7 and4.0 ± 0.6, respectively. AUCss of the test was 7.22± 1.37mg·h·L-1 and that of the reference was 7.02 ± 1.53 mg·h·L-1. The relative bioavailability of the test was (105.5 ± 19.9)%. The analysis of variance on pharmacokinetic parameters such as Cmax and AUC indicated that there was no significant difference between the two formulations. All the 90% confidence intervals of the test/reference geometric mean ratio of parameters were within the bioequivalence limits. Conclusion Pharmacokinetic profiles of the two formulations showed good sustained release properties and the two products were bioequivalent.