Oral bioavailability and pharmacokinetics of ciprofloxacin in patients with AIDS

Abstract

Few reports on the effects of AIDS on the absorption of orally (p.o.) administered agents exist. To help fill this informational gap, we administered ciprofloxacin to 12 patients with AIDS by two dosing regimens (400 mg given intravenously [i.v.] and 500 mg given p.o. every 12 h) in a randomized, crossover fashion. Pharmacokinetic parameters were determined by noncompartmental methods. Mean values (± standard deviations [SD]) for p.o. ciprofloxacin were us follows: peak concentration of drug in serum (C(max)), 2.94 ± 0.51 μg/ml; time to C(max), 1.38 ± 0.43 h; area under the concentration-time curve from 0 to 12 h (AUC(0-12)), 12.13 ± 3.21 μg · h/ml; and half-life (t( 1/4 )), 3.86 ± 0.48 h. Mean values (± SD) for i.v. ciprofloxacin were as follows: C(max), 3.61 ± 0.82 μg/ml; time to C(max), 1.0 h; AUC(0-12) 11.92 ± 2.92 μg · h/ml; and t( 1/4 ), 3.98 ± 0.94 h. The mean percent absolute bioavailability for ciprofloxacin was calculated to he 82% ± 13%, similar to the value for healthy volunteers. We conclude that ciprofloxacin when administered p.o. to patients with AIDS is well absorbed, as evidenced by excellent bioavailability and is not affected by gastrointestinal changes in the absence of infectious gastroenteritis and severe diarrhea.