Skip to main content
SpringerLink
Log in

Bambuterol: Uptake and Metabolism in Guinea Pig Isolated Lungs

  • Published:
Pharmaceutical Research Aims and scope Submit manuscript

Abstract

The lung uptake and biotransformation of 3H-bambuterol, a prodrug to terbutaline, were studied using isolated perfused and ventilated guinea pig lungs. 14C-Sucrose was used as an extracellular marker. The lung uptake of bambuterol was significantly (0.05 ≥P≥ 0.001) higher than that found for sucrose in single-pass perfusion experiments. High-performance liquid chromatographic (HPLC) analysis showed that 95.6 ± 3.6% of the effluent 3H radioactivity was attributable to bambuterol. In recirculating experiments (120 min) the lung biotransformation of 3H-bambuterol (8.5 pmol/ml) was studied. Both oxidative and hydrolytic metabolism took place. The dominating metabolites were hydroxylated bambuterol and the monocarbamate derivative which is a product of hydrolysis of bambuterol. Traces of terbutaline were also formed. The results show that bambuterol has a certain affinity to lung tissue and that the drug is, to some extent, biotransformed in the guinea pig lung.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

Similar content being viewed by others

REFERENCES

  1. L. Å Svensson. Pharm. Res. 4:156–162 (1985).

    Google Scholar 

  2. O. A. T. Olsson and L. Å Svensson. Pharm. Res. 1:19–23 (1983).

    Google Scholar 

  3. A. Tunek and E. Nilsson (in press).

  4. Y. Gnosspelius, G. Persson, G. Eklundh, et al. Respiration (Suppl.) 46:S1 (1984).

    Google Scholar 

  5. Å Ryrfeldt and E. Nilsson. Acta Pharmacol. Toxicol. 48:390–396 (1981).

    Google Scholar 

  6. Amdur and Mead. Am. J. Physiol. 192:364–368 (1958).

    Google Scholar 

  7. F. Kröll, J.-A. Karlsson, E. Nilsson, et al. Acta Physiol. Scand. 128:1–8 (1986).

    Google Scholar 

  8. Å Ryrfeldt and E. Nilsson. Biochem. Pharmacol. 27:301–305 (1978).

    Google Scholar 

  9. R. Ben-Harari and Y. S. Bakhle. Biochem. Pharmacol. 29:489–494 (1980).

    Google Scholar 

  10. E. H. Butler, K. M. Moser, and P. A. Kot. J. Lab. Clin. Med. 74:129–137 (1969).

    Google Scholar 

  11. J. S. Fowler, B. M. Gallagher, R. MacGregor, and A. P. Wolf. J. Pharmacol. Exp. Ther. 198:133–145 (1976).

    Google Scholar 

  12. R. K. Brazzell, R. B. Smith, and H. B. Kostenbauder. J. Pharm. Sci. 71:1274–1281 (1982).

    Google Scholar 

Download references

Author information

Authors and Affiliations

  1. AB Astra, Safety Assessment, S-151 85 Södertälje, Sweden

    Åke Ryrfeldt

  2. Research and Development Laboratories, AB Draco, Box 1707, S-221 01 Lund, Sweden

    Elisabeth Nilsson, Anders Tunek & Leif-Åke Svensson

Authors
  1. Åke Ryrfeldt
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Elisabeth Nilsson
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Anders Tunek
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Leif-Åke Svensson
    View author publications

    You can also search for this author in PubMed Google Scholar

Rights and permissions

Reprints and permissions

About this article

Cite this article

Ryrfeldt, Å., Nilsson, E., Tunek, A. et al. Bambuterol: Uptake and Metabolism in Guinea Pig Isolated Lungs. Pharm Res 5, 151–155 (1988). https://doi.org/10.1023/A:1015908822131

Download citation

  • Issue Date:

  • DOI: https://doi.org/10.1023/A:1015908822131

Search

Navigation