SAGE Journals Online
Advertisement
Sign In to gain access to subscriptions and/or personal tools.

 

Advanced Search

Journal Navigation

Journal Home

Subscriptions

Archive

Contact Us

Table of Contents

Advertisement

Sign In to gain access to subscriptions and/or personal tools.
Human & Experimental Toxicology
This Article
Right arrow Full Text (PDF)
Right arrow References
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to Saved Citations
Right arrow Download to citation manager
Right arrowRequest Permissions
Right arrow Request Reprints
Right arrow Add to My Marked Citations
Citing Articles
Right arrow Citing Articles via Google Scholar
Right arrow Citing Articles via Scopus
Google Scholar
Right arrow Articles by Bast, G. E
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Bast, G. E
Social Bookmarking
Add to CiteULike   Add to Complore   Add to Connotea   Add to Del.icio.us   Add to Digg   Add to Reddit   Add to Technorati   Add to Twitter  
What's this?

Influence of solubility and permeant size on absorption and metabolism of xenobiotics in rabbit skin

Gabriele E Bast

Walther-Straub-Institut für Pharmakologie und Toxikologie, Medizinische Fakultät der Ludwig-Maximilians-Universität, Nussbaumstr. 26, 80336 München, Germany

1 In order to obtain an understanding of the risks associated with dermal uptake of xenobiotics it is necessary to investigate the principles governing percutaneous absorption and metabolism. The sin gle-pass perfused rabbit ear served as a convenient model for the simultaneous study of absorption and metabolism of a variety of substances.

We found:

2 When substances are applied in a lipophilic vehicle the permeation coefficient K P is notably decreased when the distribution coefficient (n-octanol/perfusion buffer (pH 7.4)) Poct. exceeds 2000. KP also decreases with increasing molecular weight.

3 Substances which are in the ionized state at pH 7.4 may have a higher permeation coefficient than would be expected from Poct. or by molecular weight.

4 The partition of a drug from the stratum corneum to the epidermal enzymes controls the extent of its metabo lism. However, substances with increased solubility at physiological pH are metabolized to a lesser extent than expected from their absorption rate.

Key Words: dermal metabolism • percutaneous absorption • skin • rabbit

Human & Experimental Toxicology, Vol. 16, No. 8, 435-440 (1997)
DOI: 10.1177/096032719701600804
Add to CiteULike CiteULike   Add to Complore Complore   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us   Add to Digg Digg   Add to Reddit Reddit   Add to Technorati Technorati   Add to Twitter Twitter    What's this?




Advertisement