Interstitial ciprofloxacin concentrations in soft tissues were measured by
microdialysis following intravenous administration of 200 mg to each of eig
ht healthy volunteers. Interstitial ciprofloxacin concentrations were signi
ficantly lower than corresponding total serum drug concentrations; the inte
rstitium-to-serum concentration ratios ranged from 0.55 to 0.73. An in vitr
o simulation based on interstitial pharmacokinetics showed a substantially
lower antimicrobial activity than did the simulation based on serum pharmac
okinetics. Thus, ciprofloxacin concentrations at the site of effect may be
subinhibitory although effective concentrations are attained in serum.