S Bielecka-Grzela1, A Klimowicz. 1. Dermatopharmacotherapy Division, Department of Dermatology and Venereology, Pomeranian Medical University, Szczecin, Poland.
Abstract
OBJECTIVE: To measure the concentration of ciprofloxacin and its desethylenemetabolite in plasma and cutaneous microdialysates and to compare ciprofloxacin penetration into cutaneous microdialysates against theoretically predicted penetration in a peripheral compartment. METHOD: A single oral dose of 0.5 g of the parent drug was administered to 10 healthy male volunteers. Microdialysis probes with 2 kDa molecular weight cut-off were inserted intradermally and were perfused with Ringer solution up to 8 h after drug ingestion. Drug and metabolite concentrations were measured by high performance liquid chromatography. RESULTS: Mean maximum concentrations of ciprofloxacin in plasma, cutaneous microdialysates and theoretical peripheral compartment were 7.01+/-1.69, 2.95+/-0.64 and 3.37+/-0.60 micromol/L, respectively, and were achieved after about 2.0+/-0.6, 2.4+/-0.9 and 4.8+/-0.9 h. The extent of penetration into cutaneous microdialysates and theoretical peripheral compartment relative to plasma were 0.550+/-0.150 and 0.788+/-0.131, respectively, and differed significantly. Similarly, time to maximum concentration as well as area under the concentration-time curve in these compartments also differed significantly unlike the maximum concentration. CONCLUSION: Microdialysis permits the evaluation of the penetration of drug and its metabolites into target tissues. Such evaluation is helpful to optimize treatment strategies. After a single 0.5 g oral dose, ciprofloxacin penetrated into skin and achieved concentrations above the minimum inhibitory concentrations for susceptible pathogens, recommended by the National Committee for Clinical Laboratory Standards (NCCLS).
OBJECTIVE: To measure the concentration of ciprofloxacin and its desethylenemetabolite in plasma and cutaneous microdialysates and to compare ciprofloxacin penetration into cutaneous microdialysates against theoretically predicted penetration in a peripheral compartment. METHOD: A single oral dose of 0.5 g of the parent drug was administered to 10 healthy male volunteers. Microdialysis probes with 2 kDa molecular weight cut-off were inserted intradermally and were perfused with Ringer solution up to 8 h after drug ingestion. Drug and metabolite concentrations were measured by high performance liquid chromatography. RESULTS: Mean maximum concentrations of ciprofloxacin in plasma, cutaneous microdialysates and theoretical peripheral compartment were 7.01+/-1.69, 2.95+/-0.64 and 3.37+/-0.60 micromol/L, respectively, and were achieved after about 2.0+/-0.6, 2.4+/-0.9 and 4.8+/-0.9 h. The extent of penetration into cutaneous microdialysates and theoretical peripheral compartment relative to plasma were 0.550+/-0.150 and 0.788+/-0.131, respectively, and differed significantly. Similarly, time to maximum concentration as well as area under the concentration-time curve in these compartments also differed significantly unlike the maximum concentration. CONCLUSION: Microdialysis permits the evaluation of the penetration of drug and its metabolites into target tissues. Such evaluation is helpful to optimize treatment strategies. After a single 0.5 g oral dose, ciprofloxacin penetrated into skin and achieved concentrations above the minimum inhibitory concentrations for susceptible pathogens, recommended by the National Committee for Clinical Laboratory Standards (NCCLS).