Clinical pharmacokinetic evaluation of bacampicillin

Bacampicillin is a recently synthesized prodrug of ampicillin. It differs from ampicillin in having an ethoxycarbonyloxyethyl group attached to the carboxyl group in C3 of the penicillin nucleus, thus forming an ester with higher bioavailability than ampicillin. The present study was carried out in 30 patients suffering from acute exacerbations of chronic bronchitis. Bacampicillin was administered orally according to the following outline: Group A--800 mg, group B--1,200 mg, and group C--1,800 mg. The peak mean serum levels were 9.50, 12.07, and 15.83 micrograms/ml, respectively, and were reached in one hour with all doses. The peak mean bronchial mucus levels were 0.49, 0.62, and 0.95 micrograms/ml, respectively, and were achieved in four hours with all doses. During the eight hours after administration of the antibiotic, 71%, 68%, and 73% of the administered doses were excreted in the urine. Blood levels versus time curve were interpreted in terms of a one-compartment open model. Bronchial mucus and serum peaks were in good correlation with progressive doses.