Disposition and oral bioavailability of amoxicillin and clavulanic acid in pigs

J Vet Pharmacol Ther. 2007 Dec;30(6):550-5. doi: 10.1111/j.1365-2885.2007.00910.x.

Abstract

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.

MeSH terms

  • Administration, Oral
  • Amoxicillin / administration & dosage
  • Amoxicillin / blood
  • Amoxicillin / pharmacokinetics*
  • Animals
  • Anti-Bacterial Agents / administration & dosage
  • Anti-Bacterial Agents / blood
  • Anti-Bacterial Agents / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Clavulanic Acid / administration & dosage
  • Clavulanic Acid / blood
  • Clavulanic Acid / pharmacokinetics*
  • Cross-Over Studies
  • Female
  • Swine / metabolism*

Substances

  • Anti-Bacterial Agents
  • Clavulanic Acid
  • Amoxicillin