Ampicillin (AP), d(-)-α-aminobenzylpenicillin, is a widely used semisynthetic penicillin-like drug (Fig. 1). A series of AP derivatives, produced by esterification of the carboxyl group at C-3, have been developed to improve its oral bioavailability. These include pivampicillin, talampicillin, bacampicillin (BAP) and the novel prodrug lenampicillin (LAP), obtained by esterification of AP with an oxodioxolone (acetoin) group. In previous investigations, this prodrug has yielded a systemic bioavailability higher than that after administering AP as such 1.2. In this work, two methods were standardized in order to investigate the in vitro stability of LAP and the comparative bioavailability of AP after the oral administation of LAP and BAP to twelve healthy volunteers, according to the cross-over design. © 1990.
