Study On Pharmacokinetics And Bioavailability Of Cefaclor Sustained Release Tablets In Healthy Volunteers

An analytical method for the determination of pharmacokinetics and bioavailability of cefaclor in human plasma has been developed based on liquid chromatography with tandem mass spectrometry. 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 cross over study. After a single oral dose administration, C_max values were 2.54 ± 0.89 mg/L at 2.23 ± 0.64 h for the test and 2.38 ±0.65 mg/L at 2.05 ± 0.56 h for thi reference. AUCo-t values were 7.38 ± 1.66 and 7.09 ± 1.71 mg·h/mL, and t_1/2 values were 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, C_max values were 2.611 ±0.61 and 2.341 ±0.55 mg/L, C_min values were 3.48 ± 1.33 and 3.65 ± 1.23 μg/L, C_av values were 602 ± 114 and 585 ± 128 μg/L, and DF values were 4.31 ±0.7 and 4.01 ±0.6, respectively. AUC_ss of the test was 7.22 ± 1.37 mg·h/mL and that of the reference was 7.02 ± 1.53 mg· h/mL. The relative bioavailability of the test was 105.5 ±19.9 %. The analysis of variance on pharmacokinetic parameters such as C_max 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. Pharmacokinetic profiles of the two formulations showed good sustained release properties and the two products were bioequivalent.