Relative oral bioavailability of microgranulated amoxicillin in pigs

P Anfossi1, A Zaghini, G Grassigli

  • 1Dipartimento di Sanità Pubblica Veterinaria e Patologia Animale, Via Tolara di Sopra 50, 40064 Ozzano Emilia (BO), Italy.

Insights

A novel microgranulated amoxicillin formulation demonstrated higher oral bioavailability in pigs compared to the standard powder. This lipogelled matrix enhances amoxicillin delivery for effective in-feed medication against bacterial infections.

Area of Science:

  • Veterinary Pharmacology
  • Drug Delivery Systems
  • Animal Health

Background:

  • Amoxicillin trihydrate is a widely used antibiotic in swine production.
  • Optimizing amoxicillin delivery for in-feed medication is crucial for effective disease control.
  • Existing formulations may have limitations in bioavailability and therapeutic efficacy.

Purpose of the Study:

  • To develop and evaluate a new microgranulated amoxicillin trihydrate formulation for in-feed administration in pigs.
  • To compare the relative oral bioavailability of the novel formulation against a conventional amoxicillin powder.
  • To assess if therapeutic drug concentrations are achieved with the new formulation.

Main Methods:

  • Development of a lipogelled matrix for amoxicillin microgranules (10% MICR10 and 30% MICR30).
  • Administration of microgranules and powdered amoxicillin (AMX) at 50 mg/kg body weight in a three-way crossover study in pigs.
  • Serum amoxicillin analysis using high-performance liquid chromatography (HPLC) with fluorometric detection, adapted for pig serum.

Main Results:

  • Both microgranulated formulations (MICR10 and MICR30) showed significantly higher oral bioavailability than the reference powder (AMX).
  • Relative bioavailability (F) was 153.9% for MICR10 and 126.2% for MICR30.
  • Area under the concentration-time curve (AUC) differed significantly between MICR10 and AMX (P < 0.05); Cmax, tmax, and MRT were not significantly different.

Conclusions:

  • The microgranulated amoxicillin formulation is suitable for in-feed administration in pigs.
  • Its enhanced oral bioavailability suggests improved efficacy for treating susceptible bacterial infections compared to powdered amoxicillin.
  • The lipogelled matrix effectively improves amoxicillin delivery and absorption in swine.