W. Taggart et al., The effect of site of application on the transcutaneous absorption of 17-beta estradiol from a transdermal delivery system (Climara), MENOPAUSE, 7(5), 2000, pp. 364-369
Citations number
22
Categorie Soggetti
Reproductive Medicine
Journal title
MENOPAUSE-THE JOURNAL OF THE NORTH AMERICAN MENOPAUSE SOCIETY
Objective: The effect of site of application on 17-beta estradiol bioavaila
bility was assessed in an open-label, randomized, crossover study of a once
-weekly transdermal estradiol patch (Climara).
Design: After placement of a transdermal patch delivering 0.1 mg/day of est
radiol on either the buttocks or abdomen, serial plasma samples were obtain
ed over 7 days and for the immediate 24 h after patch removal. Plasma estra
diol concentrations were used to estimate pharmacokinetic parameters for th
e rate and extent of absorption between the two sites.
Results: Plasma estradiol concentrations were sustained at premenopausal le
vels over the week in most subjects. After application on the buttock, mean
peak plasma concentration (C-max) was 125.1% and mean relative bioavailabi
lity (AUC(0-168)) was 117.2% of that from the abdomen site.
Conclusions: in summary, the buttocks seem to be an acceptable site for the
application for this once-weekly 17-beta estradiol transdermal delivery sy
stem. Because the extent of absorption was significantly more for buttock t
han for abdomen application, this application site may provide an advantage
in women who experience menopausal symptoms at the end of the week. (Menop
ause 2000;7:364-369. (C) 2000, The North American Menopause Society.).