Bioequivalence Evaluation Of Three Kinds Of Cefdinir Formulations In Chinese Healthy Subjects

Cefdinir is an advanced generation, broad/extended-spectrum oral semisynthetic cephalosporin. The drug is an oral aminothiazolyl cephalosporin. Cefdinir a broad spectrum cephalosporin is effective against enteric gram-positive and gram-negative bacteria. The beta lactamase instability is the weakness of cephalosporin. Cefdinir is stable in the presence of some, but not all, β-lactamase enzymes. As a result, many organisms are resistant to penicillins and some cephalosporins are susceptible to cefdinir. It has been proven to be ective for common bacterial infections of the ear, sinus, throat, and skin. In this paper, in this Paper, Pharmaeokineties and relative bioavailability of cefdinir tablets/dispersible tablets (produeed by Guangdong Xianqiang Pharmaceutical factory) were studied with cefdinir capsules (produeed by Guangzhou Baiyunshan Guanghua Pharmaceutical Co.) as a standard reference formulation.Objective:To establish a high performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method for the determination of cefdinir in human plasma. To evaluate bioequivalence of three kinds of cefdinir formulations in healthy volunteers.Methods:In a randomized,3 way-crossover and self-control study,24 healthy male volunteers were orally administrated with three kinds of cefdinir formulations (test sample and reference sample) 100mg, to evaluate bioequivalence of cefdinir formulations. The plasma concentrations of cefdinir were determined by LC/MS/MS. The main pharmacokinetic parameters were calculated by DAS 2.1 software.Results:The method was validated by investigating the accuracy and precision for intra and inter-day runs in a linear concentration from 11.50～2300.00 ng·mL-1.The main pharmacokinetic parameters of test(cefdinir tables, A drug; cefdinir dispersible tables, B drug) and reference (cefdinir capsules, C drug) formulations in plasma were shown as follows:Tmax were (3.0 ±0.8)、(3.2±0.9) and (3.5 ± 0.7) h; Cmax were (548.96 ±184.58)、(607.09 ±236.38) and (570.18 ± 172.37) ng·mL-1; t1/2 were (2.0 ±0.3)、(1.9 ±0.4) and (1.9 ±0.3) h;AUC0-t were (2755.30 ±956.10)、 (3037.50 ±1014.40) and (2756.40 ± 804.10) ng·h·ml-1, AUC0-∞ were (2857.90± 1011.60)、(3143.80± 1038.40) and (2862.10 ±821.20) ng·h·ml-1, respectively. The relative bioavailability F were (104.2 ± 37.5)% and (111.5 ± 29.7)%.Conclusion:The method was proved to be accurate, rapid and sensitive, and can be used for the study. Tested preparation and reference preparations are bioequivalent.