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Published on: September 9, 2015
Relative bioavailability of microgranulated sulfadimidine in veal calves
P Anfossi1, C Montesissa, P Pezzi
1Department of Public Veterinary Health and Animal Pathology, Faculty of Veterinary Medicine, University of Bologna, Ozzano Emilia (BO), Italy.
Abstract:
The kinetics of free and microgranulated sulfadimidine were compared in milk-fed calves dosed orally (180 mg/kg) in a crossover study. Microgranulation results in delayed absorption of sulfadimidine and poor bioavailability, with the area under the plasma concentration-time curve (AUC(0-infinity)) reduced from 7400 to 3781 micrograms.h/mL, and maximum plasma concentration (Cmax) reduced from 188.1 +/- 39.0 to 84.41 +/- 22.6 micrograms/mL. It is concluded that sulfadimidine microgranulated with long chain fatty acids is not suitable for use in milk-fed calves; the gastrointestinal transit time is too rapid to allow full release of the drug, markedly limiting its bioavailability. In adult animals, or in the young of other animal species in which digesta transit time is slower than in calves, the bioavailability of microgranulated sulfadimidine may be much greater.
Insights
Microgranulated sulfadimidine shows poor bioavailability in milk-fed calves due to rapid gastrointestinal transit. This formulation is unsuitable for calves, though it may be effective in species with slower digestion.
Area of Science:
- Veterinary pharmacology
- Animal science
Background:
- Sulfadimidine is a commonly used sulfonamide antibiotic in veterinary medicine.
- Formulation affects drug absorption and bioavailability.
Purpose of the Study:
- To compare the pharmacokinetics of free and microgranulated sulfadimidine in milk-fed calves.
- To evaluate the suitability of microgranulated sulfadimidine for this animal model.
Main Methods:
- Oral administration of sulfadimidine (180 mg/kg) in a crossover study design.
- Comparison of plasma concentration-time profiles, including Area Under the Curve (AUC) and maximum plasma concentration (Cmax).
Main Results:
- Microgranulation significantly delayed sulfadimidine absorption and reduced bioavailability.
- AUC(0-infinity) decreased from 7400 to 3781 micrograms.h/mL.
- Cmax reduced from 188.1 +/- 39.0 to 84.41 +/- 22.6 micrograms/mL.
Conclusions:
- Microgranulated sulfadimidine is not suitable for milk-fed calves due to rapid gastrointestinal transit limiting drug release and bioavailability.
- This formulation might be more effective in animal species with slower gastrointestinal transit times.
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