Pharmacokinetic Comparison and Bioequivalence Evaluation between a Newly Formulated Generic and the Brand Cefuroxime Axetil Tablets in Healthy Male Adult Fasting Subjects

Abstract

Cefuroxime axetil (CA) is a broad-spectrum second-generation cephalosporin antibiotic resistant to beta-lactamase used for treating different kinds of infections. This study was conducted to compare the pharmacokinetics (PK) and to evaluate the bioequivalence (BE) between a newly formulated generic CA 500mg tablets as a test formula with the same dose of the brand formula as the reference product applying 2-way, 2-treatment, 2-period, 2-sequence, randomized crossover design with six days washout interval between dosing. After overnight fasting for 12 hours, both CA products were administered to 28 healthy male adult Arabic subjects, followed by serial blood samples obtained from each subject before drug dosing (0-hr) and then up to 8 hours post-dosing. The calculated PK parameters Cmax, Tmax, AUC0–t, AUC0–∞, Thalf, MRT, Cl and Vd obtained from each product were statistically compared by ANOVA and 90% confidence interval tests to evaluate the BE between both products. Based on international guidance on bioequivalences like FDA and EMEA, it was concluded from this research that the test and the reference formulas are bioequivalent since the 90% confidence intervals were within the accepted ranges of 80.00-125.00%. All participants tolerated both products well, and they were discharged without any significant alterations in their clinical baseline characteristics. Therefore, the newly formulated generic CA 500mg tablets may be prescribed in clinical practice and used as a safe and effective alternative to the brand product.