Pharmacokinetics and residues of a new oral amoxicillin formulation in piglets: A preliminary study

The pharmacokinetic properties of amoxicillin and clavulanic acid were studied in healthy, fasted pigs after single intravenous (i.v.) and oral (p.o.) dosage of 20 mg/kg of amoxicillin and 5 mg/kg of clavulanic acid. The plasma concentrations of the drugs were determined by validated high-performance liquid chromatographic methods and the pharmacokinetic parameters were calculated by compartmental and noncompartmental analyses. After i.v. administration of the two drugs, plasma concentration-time curves were best described by a three-compartmental open model for amoxicillin and a two-compartmental open model for clavulanic acid. Amoxicillin (with a t(1/2 gamma) = 1.03 h and a clearance of 0.58 L/h.kg) and clavulanic acid (with a t(1/2 beta) of 0.74 h and a clearance of 0.41 L/h.kg) were both rapidly eliminated from plasma. Both drugs had apparently the same volume of distribution of 0.34 L/kg. After p.o. administration of the two drugs, a noncompartmental model was used. Elimination half-lives of amoxicillin and clavulanic acid were not significantly different, i.e. 0.73 and 0.67 h respectively. The mean maximal plasma concentrations of amoxicillin and clavulanic acid were 3.14 and 2.42 mg/L, and these were reached after 1.19 and 0.88 h respectively. The mean p.o. bioavailability was found to be 22.8% for amoxicillin and 44.7% for clavulanic acid.

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“…administration of amoxicillin in pigs was described by Martinez‐Larranaga et al. (2004) and Hernandez et al. (2005).…”

Section: Discussionmentioning

confidence: 99%

Disposition and oral bioavailability of amoxicillin and clavulanic acid in pigs

Reyns

Boever

Baert

et al. 2007

Vet Pharm & Therapeutics

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“…Previous studies have showed the oral bioavailability of AMO can be variable, which may be associated with the different methods of oral administration[19] [25]. In the present study, the relative bioavailability of AMO in fasted-pigs following gavage administration of GRANULE amo + apr at 16 mg·kg -1 compared to i.m.…”

Section: Discussionmentioning

confidence: 71%

“…(C max = 0.76 μg·mL -1 and t max = 5.78 h) and Martinez-Larranaga et al . (C max = 7.37 μg·mL -1 and t max = 0.97 h) [19, 20]. The discrepancy maybe related to differences in the varied methods of oral administration of AMO and its different formulation (i.e powder, granulation) [21].…”

Section: Discussionmentioning

confidence: 99%

“…Hernandez et al . reported that the bioavailability of AMO (AMO 10% Premix) in pigs following administration in-feed medication at 15 mg·kg -1 was 11% [19]. Similarly, Anfossi et al .…”

Section: Discussionmentioning

confidence: 99%

“…orally administered to pigs by in-feed medication, which is only two-fold higher than the AUC INF values reported by Agersø and Friis [25] and 1.35-fold higher than that in the present study. This variability may be attributable to the absorption of AMO across the intestinal mucosa by both passive diffusion and active transport processes [19, 25–27]. It also contributed to explain the non-sigificantance ( P values among 0.22 to 1; Table 1) of all pharmacokinetic parameters between oral administration of GRANULE amo + apr and POWDER amo in pigs, although the minor changes was present with the different formulation of AMO.…”

Section: Discussionmentioning

confidence: 99%

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Pharmacokinetics and relative bioavailability of an oral amoxicillin-apramycin combination in pigs

et al. 2017

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A new compound granular premix of amoxicillin (20% w/w dry mass)/apramycin (5% w/w dry mass) was developed, and its pharmacokinetics and relative bioavailability were determined in pigs following oral administration following a cross-over study design. The pharmacokinetic parameters of amoxicillin (t1/2λ = 6.43 ± 4.85h, Cmax = 3.2 ± 1.35 μg·mL-1, Tmax = 1.92 ± 0.58, AUCINF = 8.98 ± 2.11 h·μg·mL-1) and apramycin (t1/2λ = 8.67±4.4h, Cmax = 0.23 ± 0.12 μg·mL-1, Tmax = 2.25 ± 0.82 h, AUCINF = 12.37 ± 8.64h·μg·mL-1) when administered as the amoxicillin-apramycin granular premix did not significantly differ from those for the single-ingredient powder form of each component. The relative bioavailability of amoxicillin following oral administration of the amoxicillin-apramycin granular premix was 22.62% when compared to the intramuscular administration of commercial amoxicillin sodium-powder. This is the first report of a new amoxicillin-apramycin combination which has a potential veterinary application the for prevention and treatment digestive tract infections in pigs.

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