Preparation and evaluation of cefquinome-loaded gelatin microspheres and the pharmacokinetics in pigs.

Cefquinome (CEF) is widely used for veterinary clinical applications because of its broad spectrum and high efficiency. However, frequent administrations are required due to its short elimination half-life. In this study, cefquinome sulfate gelatin microspheres (CEF-GMS) were prepared as a sustained-release formulation using emulsion chemical cross-linking technique. Physical properties, stability, sustained-release property in vitro, and pharmacokinetics in pigs were assessed. The morphology of CEF-GMS showed a good sphericity with porous structure on the surface, and the mean diameter was 8.80 ± 0.78 μm, with 90.60 ± 3.98% of the total in the range of 5-20 μm. There were no significant changes of all estimated indexes in the stability tests. In vitro drug release study showed that the release of CEF from CEF-GMS was much slower than that from crude CEF in a release medium. Pharmacokinetic characteristics were evaluated following intramuscular administration of CEF-GMS or Cefquinome sulfate injection (CEF-Inj) in pigs at a dosage of 4 mg CEF/kg body weight. The plasma drug concentration-time data of CEF-GMS and CEF-Inj were both best fitted by two-compartment models with first-order absorption, and the elimination half-life of CEF-GMS was almost 10 times that of CEF-Inj. Overall, CEF-GMS might be used as a sustained-release formulation of CEF for veterinary clinical applications.