Skip to main content
Log in

Correlation betweenin vitro andin vivo drug metabolism rate: Oxidation of ethoxybenzamide in rat

  • Published:
Journal of Pharmacokinetics and Biopharmaceutics Aims and scope Submit manuscript

Abstract

In vitroand in vivocorrelations of the microsomal oxidation of drugs were examined, using ethoxybenzamide as a model drug. Ethoxybenzamide disappearance time course from rat plasma in vivowas analyzed by a two-compartment model assuming a Michaelis-Menten type elimination process. Ethoxybenazmide oxidation in vitrowas measured by the appearance rate of salicylamide in rat liver microsomal suspension. Parameters obtained were Vmax=3.46 and 3.77 μmoles/min/kg body weight and Km=0.378 and 0.192mM, in vitroand in vivo,respectively.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Similar content being viewed by others

References

  1. G. R. Wilkinson. Pharmacokinetics of drug disposition: Hemodynamic considerations.Ann. Rev. Pharmacol. 15:11–27 (1975).

    Article  CAS  PubMed  Google Scholar 

  2. R. L. Dedrick. Animal-scale-up.J. Pharmacokin. Biopharm. 1:435–461 (1973).

    Article  CAS  Google Scholar 

  3. R. L. Dedrick, D. D. Forrester, and D. H. W. Ho.In vitro-in vivo correlation of drug metabolism-deamination of 1-β-D-arabinofuranosylcytosine.Biochem. Pharmacol. 21:1–16 (1972).

    Article  CAS  PubMed  Google Scholar 

  4. A. B. Makar and G. J. Mannering. Kinetics of ethanol metabolism in the intact rat and monkey.Biochem. Pharmacol. 19:2017–2022 (1970).

    Article  CAS  PubMed  Google Scholar 

  5. R. L. Dedrick and D. D. Forrester. Blood flow limitations in interpreting Michaelis constants for ethanol oxidationin vivo.Biochem. Pharmacol. 22:1133–1140 (1973).

    Article  CAS  PubMed  Google Scholar 

  6. H. Nogami, M. Hanano, S. Awazu, and H. H. Moon. Pharmacokinetic analysis on the disappearance of ethoxybenzamide from plasma: Statistical treatment of data of two compartmental model by a digital computer.Chem. Pharm. Bull. (Tokyo) 17:2097–2104 (1969).

    Article  CAS  Google Scholar 

  7. G. Levy and T. Matsuzawa. Pharmacokinetics of salicylamide elimination in man.Pharmacol. Exp. Ther. 156:285–293 (1967).

    CAS  Google Scholar 

  8. S. Awazu, M. Hanano, H. H. Moon, T. Fuwa, T. Iga, and H. Nogami. Pharmacokinetic analysis by digital computer [in Japanese]. In K. Kakemi (ed.),Absorption, Metabolism, and Excretion of Drugs. Hirokawa Publishing Co., Tokyo, 1971, pp. 301–332.

    Google Scholar 

  9. S. Awazu. Analogue and digital computer [in Japanese]. In K. Tsuda and H. Nogami (eds.),Biopharmacy, Chijin Shokan, Tokyo, 1971, pp. 448–489.

    Google Scholar 

  10. H. G. Boxenbaum, S. Riegelman, and R. M. Elashoff. Statistical estimations in phar-macokinetics.J. Pharmacokin. Biopharm. 2:123–148 (1974).

    Article  CAS  Google Scholar 

  11. R. Grundin, P. Moldéus, S. Orrenius, K. O. Borg, I. Skanberg, and C. von Bahr. The possible role of cytochrome P-450 in the liver “first pass elimination” of aβ-receptor blocking drug.Acta Pharmacol. Toxicol. 35:242–260 (1974).

    Article  CAS  Google Scholar 

Download references

Author information

Authors and Affiliations

Authors

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Lin, J.H., Hayashi, M., Awazu, S. et al. Correlation betweenin vitro andin vivo drug metabolism rate: Oxidation of ethoxybenzamide in rat. Journal of Pharmacokinetics and Biopharmaceutics 6, 327–337 (1978). https://doi.org/10.1007/BF01060096

Download citation

  • Received:

  • Revised:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/BF01060096

Key words

Navigation