PHARMACOKINETICS OF ORAL CEFCANEL DALOXATE HYDROCHLORIDE IN HEALTHY-VOLUNTEERS AND PATIENTS WITH VARIOUS DEGREES OF IMPAIRED RENAL-FUNCTION

Cefanel daloxate hydrochloride is a new oral cephalosporin prodrug. It is a double cephem ester of cefcanel, which is the active principle released in the body after uptake of an intermediate cephem mono ester. The present study investigated the pharmacokinetics of cefcanel following a single oral dose of cefcanel daloxate hydrochloride 300 mg to healthy volunteers and to patients with various degrees of stable renal insufficiency. Twenty individuals from 21 to 74 years of age received a single oral dose of cefcanel daloxate hydrochloride together with an iv bolus injection of iohexol for a simultaneous assessment of glomerular filtration rate (GFR). The concentrations of cefcanel and iohexol in plasma and urine were measured using high performance liquid chromatography. Cefcanel renal clearance and fraction excreted in the urine were linearly correlated with renal function and thus, logarithmic increases in plasma area under the concentration versus time curve and plasma elimination half-life were seen with decreasing GFR. Although steady state kinetics were not performed our findings suggest that a dosage reduction is not necessary even in pre-uraemic patients. © 1994 The British Society for Antimicrobial Chemotherapy.