The pharmacokinetics of ciprofloxacin (Bay o 9867) was examined after a single oral dose of 250 mg and a single intravenous dose of 100 mg respectively in six healthy male volunteers in an open, randomized crossover study. Although ciprofloxacin concentrations were measured in serum, plasma and urine by HPLC with fluorimetric detection and by microbiological assay, all pharmacokinetic calculations are based on the highly sensitive HPLC method only. The mean serum concentration of ciprofloxacin peaked approximately 1 h after the oral dose (0.94 mg/l). The elimination half-life was about 4 h and the renal clearance was 4.75 ml/min . kg; both were independent of the route of administration. The total clearance (9.62 ml/min . kg) was about twofold higher than the renal clearance. The volume of distribution of the central compartment was calculated to be 0.161 l/kg and the total volume at steady state was 2.0 l/kg. About 27% of the oral dose was excreted in urine, whereas the urinary recovery of the i.v. dose was 46%. The absolute bioavailability of ciprofloxacin was found to be approximately 60%. Ciprofloxacin appears to follow first-order, three compartment model kinetics.

The tetra- and mono-thionated cyclic octadepsipeptides represent novel cyclic octadepsipeptide derivatives with broad-spectrum activity against parasitic nematodes in mice and sheep. Some of these show better activity than the potent natural anthelmintic cyclic octadepsipeptide PF1022A against Hymenolepis nana, Heterakis spumosa and Trichinella spiralis larvae in mice. In particular, they show improved efficacy against Haemonchus contortus and Trichostrongylus colubriformis in sheep compared with PF1022A. Here we report on two different and simple synthetic pathways for this new class of thionated cyclic octadepsipeptides.

Serum concentrations and urinary excretion of ciprofloxacin were studied in female and male volunteers following a single oral administration of 100 mg, 250 mg, 500 mg or 1000 mg. Serum and urine concentrations increased proportionally to the increasing dose administered but independently of sex. Twenty-five percent of the administered dose was excreted in the urine as unmetabolized ciprofloxacin within the first 24 hours after oral administration. Renal clearance averaged 5 ml/min X kg.

No abstract

No abstract