Pharmacokinetics and tissue localization of doxycycline polyphosphate and doxycycline hydrochloride in the rat.

Two doxycycline derivatives Doxycycline polyphosphate and Doxycycline hydrochloride were administered to rats at a dose of 20 mg/kg body weight. Doxycycline tissue levels were determined using a microbiological assay. Only an insignificant fraction of the antibiotics was found to cross the blood brain barrier. Doxycycline was highly concentrated in excretory organs: liver, kidneys and caecum. The high intestinal drug level observed is probably related to the entero-hepatic cycle of this antibiotic. There was a good correlation between serum and heart doxycycline concentration; heart level was about twice that of serum. In lung, antibiotic level was always higher than in serum.