Naunyn-Schmiedeberg's Archives of Pharmacology

, Volume 306, Issue 1, pp 89–92 | Cite as

Interaction of cations and chelators with the intestinal absorption of tetracycline

  • H. Poiger
  • Ch. Schlatter
Article

Summary

The influence of certain compounds on intestinal absorption of tetracycline was tested, using two different in vivo techniques: a) Disappearence of the drug from perfused intestinal segments of the rabbit; b) Measuring urinary excretion in the rat after oral dosage.

Ca2+ and Fe2+ ions both reduced the permeation rate of tetracycline by about 30%. In presence of Ca2+ and salicylate ions, leading to ion-pair formation with the antibiotic, intestinal uptake was significantly increased in comparison to experiments where only calcium was present. A more pronounced increase was observed with EDTA.

Phosphate ions had different effects on the uptake of the antibiotic in both experimental techniques. Possible mechanisms are discussed.

Key words

Tetracycline absorption Salicylic acid EDTA Phosphate Ions 

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References

  1. Albert, A.: Avidity of terramycin and aureomycin for metabllic cations. Nature 172, 201 (1953)Google Scholar
  2. Albert, A., Rees, C. W.: Avidity of the tetracyclines for the cations of metals. Nature 177, 433–434 (1956)Google Scholar
  3. Banerjee, S., Chakrabarti, K.: The transport of tetracyclines across the mouse ileum in vitro: the effect of cations and other agents. J. Pharm. Pharmacol. 28, 133–138 (1975)Google Scholar
  4. Chin, T.-F., Lach, J. L.: Drug diffusion and bioavailability: Tetracycline metallic chelation. Am. J. Hosp. Pharm. 32, 625–629 (1975)Google Scholar
  5. Collett, J. H., Withington, R., Cox, B.: Correlation between the in vivo and in vitro availability of salicylic acid for membrane transfer from polysorbate 20 solutions. J. Pharm. Pharmacol. 26, 34–38 (1974)Google Scholar
  6. Doluisio, J. T., Martin, A. N.: Metal complexation of the tetracycline hydrochlorides. J. Med. Chem. 6, 16–20 (1963)Google Scholar
  7. Eisenberg, G. M., Weiss, W., Flippin, H. F.: The effect of ethylenediaminetetraacetic acid (EDTA) and ascorbic acid on tetracycline blood serum concentrations. J. Lab. Clin. Med. 52, 895–898 (1958)Google Scholar
  8. Harcourt, R. S., Hamburger, M.: The effect of magnesium sulfate in lowering tetracycline blood levels. J. Lab. Clin. Med. 50, 464–468 (1957)Google Scholar
  9. Kakemi, K., Sezaki, H., Ogata, H., Nadai, T.: Effect of Ca2+ on the absorption of tetracycline from the small intestine (1). Chem. pharm. Bull. (Tokyo) 16, 2200–2205 (1968a)Google Scholar
  10. Kakemi, K., Sezaki, H., Hayashi, M., Nadai, T.: Effect of Ca2+ on the absorption of tetracycline from the small intestine (2). Chem. pharm. Bull. (Tokyo) 16, 2206–2212 (1968b)Google Scholar
  11. Kohn, K. W.: Determination of tetracycline by extraction of fluorescent complexes. Analyt. Chem. 33, 862–866 (1961)Google Scholar
  12. Neuvonen, P. J.: Interactions with the absorption of tetracycline. Drugs 11, 45–54 (1976)Google Scholar
  13. Poiger, H., Schlatter, Ch.: Fluorimetric determination of tetracyclines in biological materials. Analyst 101, 808–814 (1976)Google Scholar
  14. Schanker, L. S., Tocco, D. J., Brodie, B. B., Hogben, C. A. M.: Absorption of drugs from the rat small intestine. J. Pharmacol. exp. Ther. 123, 81–88 (1958).Google Scholar
  15. Seeger, K., Hentschel, G.: Der Einfluß von Äthylendiamintetraessigsäure auf die antibakterielle Aktivität einiger Antibiotika und ihre enterale Resorption beim Schwein. Arzneim.-Forsch. 21, 1590–1594 (1971)Google Scholar
  16. Youssef, M. K., Ibrahim, EL. A., Attia, I. A.: Paper chromatographic determination of tetracycline. J. Pharm. Sci. 62, 1998–2001 (1973)Google Scholar

Copyright information

© Springer-Verlag 1979

Authors and Affiliations

  • H. Poiger
    • 1
  • Ch. Schlatter
    • 1
  1. 1.Institute of ToxicologySwiss Federal Institute of Technology and University of ZürichSchwerzenbach-ZürichSwitzerland

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