Vaginal drug absorption in the rhesus monkey: Bioavailability method and assessment of estrogens
dc.contributor.author | Park, J. Y. | en_US |
dc.contributor.author | Langworthy, M. | en_US |
dc.contributor.author | Behl, Charan R. | en_US |
dc.contributor.author | Higuchi, William I. | en_US |
dc.contributor.author | Flynn, Gordon L. | en_US |
dc.contributor.author | Ho, Norman F. H. | en_US |
dc.date.accessioned | 2006-04-07T17:35:05Z | |
dc.date.available | 2006-04-07T17:35:05Z | |
dc.date.issued | 1979-05 | en_US |
dc.identifier.citation | Park, J. Y., Langworthy, M., Behl, C. R., Higuchi, W. I., Flynn, G. L., Ho, N. F. H. (1979/05)."Vaginal drug absorption in the rhesus monkey: Bioavailability method and assessment of estrogens." International Journal of Pharmaceutics 2(3-4): 215-238. <http://hdl.handle.net/2027.42/23573> | en_US |
dc.identifier.uri | http://www.sciencedirect.com/science/article/B6T7W-4772HRT-1J/2/3263ac9b736cc0ab3ec2404e1e8670b8 | en_US |
dc.identifier.uri | https://hdl.handle.net/2027.42/23573 | |
dc.description.abstract | Novel experimental and theoretical methods in evaluating the systemic bioavaliability of estrogens delivered via the vaginal route have been developed. The approaches were demonstrated for estrone and estradiol in the rhesus monkey. These newly developed techniques have made it possible to quantify first pass vaginal membrane metabolism for estrone and for estradiol and to distinguish this process from peripheral tissue metabolism. This was achieved by obtaining steady-state blood levels of the steroids and all significant metabolites resulting from identical zero-order infusion rates of the steroid by the vaginal and intravenous routes. Comparison of the blood levels gave rapid estimations of bioavailability. The modeling of the steady-state situation and quantification of the kinetic parameters were employed such that differences in blood levels from vaginal and intravenous drug infusion mirrored the membrane transport and metabolic events. Membrane metabolism of infused estrone and estradiol reduced the blood levels of these steroids by about 55 and 61%, respectively, of that expected in the absence of membrane metabolism.About 45% of vaginally administered estrone appeared directly in the blood as estrone and 9% as estradiol and 46% as total conjugates. The dominant route of membrane metabolism of estrone was estrone conjugation rather than reduction to estradiol. When estradiol was infused vaginally, 26% estradiol appeared in the blood and 35% as estrone and 39% as total conjugates; the dominant route of metabolism was the oxidation to estrone and not estradiol conjugation. | en_US |
dc.format.extent | 1839661 bytes | |
dc.format.extent | 3118 bytes | |
dc.format.mimetype | application/pdf | |
dc.format.mimetype | text/plain | |
dc.language.iso | en_US | |
dc.publisher | Elsevier | en_US |
dc.title | Vaginal drug absorption in the rhesus monkey: Bioavailability method and assessment of estrogens | en_US |
dc.type | Article | en_US |
dc.rights.robots | IndexNoFollow | en_US |
dc.subject.hlbsecondlevel | Pharmacy and Pharmacology | en_US |
dc.subject.hlbtoplevel | Health Sciences | en_US |
dc.description.peerreviewed | Peer Reviewed | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Mich. 48109, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Mich. 48109, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Mich. 48109, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Mich. 48109, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Mich. 48109, U.S.A. | en_US |
dc.contributor.affiliationum | College of Pharmacy, The University of Michigan, Ann Arbor, Mich. 48109, U.S.A. | en_US |
dc.description.bitstreamurl | http://deepblue.lib.umich.edu/bitstream/2027.42/23573/1/0000534.pdf | en_US |
dc.identifier.doi | http://dx.doi.org/10.1016/0378-5173(79)90022-X | en_US |
dc.identifier.source | International Journal of Pharmaceutics | en_US |
dc.owningcollname | Interdisciplinary and Peer-Reviewed |
Files in this item
Remediation of Harmful Language
The University of Michigan Library aims to describe library materials in a way that respects the people and communities who create, use, and are represented in our collections. Report harmful or offensive language in catalog records, finding aids, or elsewhere in our collections anonymously through our metadata feedback form. More information at Remediation of Harmful Language.
Accessibility
If you are unable to use this file in its current format, please select the Contact Us link and we can modify it to make it more accessible to you.