The pharmacokinetics and sputum penetration of ampicillin and amoxycillin following simultaneous i.v. administration

Five patients with exacerbation of chronic bronchitis received as a single iv injection 500 mg of ampicillin and 500 mg of amoxycillin. Blood and sputum samples were collected at timed intervals following dosing and the concentrations of the two antibiotics present in the samples were determined by HPLC analysis. No statistically significant differences were observed between the serum concentrations of ampicillin and amoxycillin, and the pharmacokinetics of the two drugs were almost identical, with half lives of 93 min (amoxycillin) and 103 min (ampicillin). Sputum amoxycillin concentrations were significantly higher (Student's paired t-test; P less than 0.001) than those of ampicillin, with mean levels two hours after dosing of 2.9 mg/l (range 1.9-4.0) for amoxycillin and 1.4 mg/l (range 0.8-2.4) for ampicillin.