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Published on: May 9, 2019
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.
Abstract:
A new microgranulated formulation of amoxicillin trihydrate for in-feed medication was developed using a lipogelled matrix. Its relative bioavailability was compared with powdered drug in pigs and an assessment was made to determine whether therapeutic concentrations were achieved. Microgranules containing 10% (MICR10) and 30% (MICR30) amoxicillin and free amoxicillin trihydrate powder (reference, AMX) were administered at dosages of 50 mg of amoxicillin/kg b.w. using a three-way-crossover design. Amoxicillin analysis in serum was performed by a sensitive high performance liquid chromatography (HPLC) method with fluorometric detection, using an extraction procedure already described for edible tissues of fish and adapted and validated for pig serum. The oral bioavailability of both microgranulated formulations was higher than that of the reference formulation [relative bioavailability (F): 153.9 +/- 58.2% for MICR10; 126.2 +/- 70.5% for MICR30] and the area under the concentration-time curve (AUC) values of MICR10 and AMX formulations were significantly different (P < 0.05). Differences between the mean maximum concentration (Cmax), time of Cmax (tmax) and mean residence time (MRT) of the drug formulations were not significant. Microgranulated amoxicillin is suitable for in-feed administration to pigs and, because of its higher oral bioavailability compared with the powdered compound, it may be more effective for the treatment of susceptible infections.
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.
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