Summary
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.
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Craig W.A., Byungse Suh. (1978): Theory and practical impact of binding of antimicrobials to serum proteins and tissue. Scand. J. Infect. Dis. (Suppl.),14, 92–99.
Craig W.A., Welling P.G. (1977): Protein binding of antimicrobials: clinical pharmacokinetics and therapeutic implications. Clin. Pharmacokinet.,2, 252–268.
Fourtillan J.B., Lefebvre M.A. (1979): Corrélations structure-activité dans la famille des tétracyclines. Nouv. Presse Med.,2, 64–70.
Welling P.G., Koch P.A., Lau C., Craig W.A. (1977): Bioavailibility of tetracyclin and doxycyclin in fasted and non-fasted subjects. Antimicrob. Agents. Chemother,11, 462–469.
Bennet J.V., Brodie J.L., Brenner E.J., Kirby W.M. (1966): Simplified accurate method for antibiotic assay of clinical specimens. Appl. Microb.,14, 170–177.
Mingat J., Micoud M. (1979): Passage de la doxycycline à travers la barrière hémoméningée. Nouv. Presse méd.,2, 136–137.
Zalta J.P., Asselineau J. (1973): Les antibiotiques, Herman ed. Paris.
Fabre J. (1960): Pharmacocinétique tissulaire de la doxycycline comparée à celle d’autres antibiotiques chez le rat. Nouv. Presse Méd.,2, 71–76.
Campistron G., Fabre J., Guiraud R., Le Net R., Cros J. and Puget A. (1979): The measurement of circulating blood volume and of the blood volume. Int. J. Nucl. Med. Biol.,6, 167–168.
Cahen R., Gantes P., Daussaud G. (1968): La doxycycline (Vibramycine), deoxy-6 hydroxy 5 tetracycline un nouvel antibiotique. Thérapie,23, 779–792.
Gartmann J. (1972): Doxyzyklinkonzentrationen im Lungengewebe in der Bronchialwand und im Bronchialsekret. Schweiz. Med. Wochenschr.,102, 1484–1486.
Hartnett B.J.S., Marlin G.E. (1976): Doxycycline in serum and bronchial secretions. Thorax,31, 144–148.
Liss R.H., Norman J.C. (1975): Visualisation of doxycyclin in lung tissue and sinus secretions by fluorescent techniques. Chemotherapy,21, (suppl.), 27–35.
Bergogne-Berezin E., Lambert-Zechovsky N. (1976): La doxycycline: quelques propriétés bactériologiques et pharmacologiques. Gaz. Med. France,83, 53–58.
Favre J., Kunz J.P., Virieux C., Laurencet J.L., Pitton J.S. (1968): Le comportement de la doxycycline chez l’homme. Chemotherapy,13, (suppl.ad.), 23–40.
Schach von Wittenau, Delahunt C.S. (1966): The distribution of tetracycline in tissues of dogs after repeated oral administrations. J. Pharmacol. Exp. Ther.,152, 164–169.
Schach von Wittenau M., Twomey T.M. (1971): The disposition of doxycycline by man and dog. Chemotherapy,16, 217–228.
Fourtillan J.B., Lefevbre M.A., Saux M.C., Becq-Giraudon B. (1979): Etude pharmacocinétique de la doxycycline chez l’homme par chromatographie liquide haute performance. Nouv. Presse Med.,2, 77–81.
Whelton A. (1974): Doxycyclin pharmacokinetics in the absence of renal function Kidney. Int.,45, 365–371.
Whelton A. (1979): Utilisation des tétracyclines au cours de l’insuffisance rénale. Nouv. Presse Méd.,2, 86–92.
Schach von Wittenau M., Yeary R. (1963): The excretion and distribution in body fluids of tetracyclines after intraveinous administration to dogs. J. Phamacol. Exp. Ther.,140, 258–266.
Schach von Wittenau M., Twomey T.M., Swindell A.V. (1972): The disposition of doxycyclin by the rat. Chemotherapy,17, 26–39.
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Michel, G., Mosser, J. & Olle, J. Pharmacokinetics and tissue localization of doxycycline polyphosphate and doxycycline hydrochloride in the rat. European Journal of Drug Metabolism and Pharmacokinetics 9, 149–153 (1984). https://doi.org/10.1007/BF03189618
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DOI: https://doi.org/10.1007/BF03189618