Preparation of a newly formulated long-acting ceftiofur hydrochloride suspension and evaluation of its pharmacokinetics in pigs

Abstract

A new long-acting ceftiofur hydrochloride preparation was formulated and its physical properties, stability, and pharmacokinetics were investigated in this study. The prepared ceftiofur hydrochloride suspension demonstrated a milk white consistency, was easy to re-disperse and was stable in light, heat and humidity stability tests. Its other physical properties such as flowability, syringeability, settling volume ratio, particle size and distribution were perfectly consistent with the standard of Ministry of Agriculture of the People's Republic of China. After intramuscular administration of a single dose in swine (5 mg/kg B.W.), the drug concentration-time data in plasma were well fitted using the two-compartment open model. Compared with the ceftiofur hydrochloride preparation (EXCENEL) from Pfizer, the peak concentration (C(max)) in plasma was decreased by 2.34 times (P < 0.001), the half-life of elimination phase (T(1/2beta)) was 1.65 times longer (P < 0.001), and the therapeutic level of ceftiofur above the lowest effective plasma concentration of 0.2 microg/mL (T > 0.2) was prolonged from 87.20 h to 135.36 h (P < 0.001). The ceftiofur hydrochloride suspension prepared in this study provides therapeutically effective plasma concentrations for a longer duration, which make it more effective and more convenient to use in the treatment of respiratory diseases that require the maintenance of therapeutic plasma concentrations over a long duration.