Menopause. 2000 Sep-Oct;7(5):364-9.
The effect of site of application on the transcutaneous absorption of 17-beta estradiol from a transdermal delivery system (Climara).
Abstract
OBJECTIVE:
The effect of site of application on 17-beta estradiol bioavailability was assessed in an open-label, randomized, crossover study of a once-weekly transdermal estradiol patch (Climara).
DESIGN:
After placement of a transdermal patch of estradiol on either the buttocks or abdomen, serial plasma samples were obtained over 7 days and for the immediate 24 h after patch removal. Plasma estradiol concentrations were used to estimate pharmacokinetic parameters for the rate and extent of absorption between the two sites.
RESULTS:
Plasma estradiol concentrations were sustained at premenopausal levels over the week in most subjects. After application on the buttock, mean peak plasma concentration (Cmax) was 125.1% and mean relative bioavailability (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 system. Because the extent of absorption was significantly more for buttock than for abdomen application, this application site may provide an advantage in women who experience menopausal symptoms at the end of the week.
J Clin Pharmacol. 1996 Nov;36(11):998-1005.
Pharmacokinetics of a 7-day 17 beta-estradiol transdermal delivery system: effect of application site and repeated applications on serum concentrations of estradiol and estrone.
FemPatch (Parke-Davis Pharmaceutical Research, Division of Warner-Lambert Company, Ann Arbor, MI), a new 7-day 17 beta-estradiol transdermal delivery system (TDS), has been developed for treatment of menopausal vasomotor symptoms. This two-period crossover study was conducted to determine the effects of TDS application site (buttocks versus abdomen) and early TDS replacement on estradiol and estrone concentrations, and to quantify intersubject and intrasubject pharmacokinetic variability. Eighteen healthy, postmenopausal female volunteers received a single 7-day TDS application to the abdomen and repeated TDS applications to the buttocks (regular replacement on days 7 and 14, intentional early replacement on day 17, and removal on day 21). Serial serum samples were assayed for estradiol and estrone by validated radioimmunoassay methods. The 7-day TDS delivers estradiol at a constant, near zero-order rate for the duration of application, independent of application site. Mean serum estradiol concentrations were higher after application to the buttocks than after application to the abdomen (19 and 15 pg/mL above baseline, respectively), making the buttocks the preferred site for TDS application.