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European Journal of Clinical Pharmacology

, Volume 25, Issue 5, pp 703–708 | Cite as

Protein binding of enprofylline

  • K. Tegnér
  • O. Borgå
  • I. Svensson
Originals

Summary

The protein binding of enprofylline, 3-propylxanthine, in plasma was studied by equilibrium dialysis and ultrafiltration under various experimental conditions. A limited comparison with theophylline was also undertaken. The mean fraction of enprofylline bound in human plasma at 20°C was 47.3±1.1% (SD), which was only 2% less than theophylline. The binding of the two drugs increased dramatically in the pH range 7.2 to 7.8, as reported previously for theophylline. Reasonable agreement was found between equilibrium dialysis and ultrafiltration, but the latter technique proved impractical, because pH control was difficult to achieve. A pronounced species difference in the binding of enprofylline was found. At pH 7.4 an almost constant level of binding of 57% in dog and 81% in rat was found up to 2 · 10−5 M (approx. 4 mg/l). Corresponding values in human and monkey plasma were 47 and 48%, respectively, up to 10−4 M (approx. 20 mg/l).

Key words

enprofylline 3-propylxanthine protein binding equilibrium dialysis theophylline ultrafiltration pH effect species differences 

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Copyright information

© Springer-Verlag 1983

Authors and Affiliations

  • K. Tegnér
    • 1
  • O. Borgå
    • 1
  • I. Svensson
    • 1
  1. 1.AB Draco, Pharmacokinetic Laboratory, Research and Development LaboratoriesLundSweden

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