Pharmacokinetics and Tissue Distribution of Amoxicillin plus Clavulanic Acid after Oral Administration in Man

Summary

Alimentili (875 amoxicillin and 125 mg potassium clavulanate) was administered orally to patients with chronic bronchitis. Concentrations of amoxicillin and clavulanic acid were measured in serum, sputum and urine. Peak serum levels for amoxicillin of 11.23 ± 2.61 μg/ml were observed at 2 hours and for clavulanic acid of 2.55 ± 0.54 μg/ml at 1 hour. After 9 hours, 50% of the amoxicillin and 39% of the clavulanic acid had been renally excreted. The peak sputum concentration of amoxicillin was 1.31 ± 0.42 μg/ml at 4 hours and of clavulanate was 0.79 ± 0.23 ± μg/ml at 2 hours.

Patients awaiting surgery received an oral dose of augmentin as above. Samples of lung, tonsil, middle ear mucosa and prostate were obtained and tissue concentrations of both compounds measured. Peak levels of amoxicillin ranged from 0.87 μg/g (tonsil) to 2.56 μg/g (lung) and of clavulanic acid from 0.20 μg/g (prostate) to 0.56 μg/g (lung) between 3 and 4 hours after dosing.

Key Words:

• Amoxicillin
• clavulanate
• augmentin
• pharmacokinetics.