Pharmacokinetics of a transdermal testosterone cream in healthy postmenopausal women.
OBJECTIVE
The steady-state pharmacokinetics of two doses of a transdermal testosterone cream (TTC) was investigated after daily application for 21 days.


METHODS
This was a two-way cross-over study conducted for 6 weeks. Seven healthy postmenopausal women (mean age, 59.3 y) were randomly allocated to 5 or 10 mg of TTC applied daily to the upper arm. Serum total testosterone (TT), free testosterone (fT), sex hormone-binding globulin, and metabolite concentrations were measured. Baseline-corrected and uncorrected serum TT and fT pharmacokinetic parameters (AUC0-24, C avg, Cmax, and Tmax) were calculated using a standard model-independent approach.


RESULTS
After the single-dose application of 5 mg of TTC on day 22, the median uncorrected TT C avg was found to be 0.54 ng/mL (range, 0.43-1.31), and the median uncorrected fT C avg was found to be 4.14 pg/mL (range, 2.41-9.72). Doubling of the dose only resulted in a 30% increase in baseline-corrected TT C avg (0.52 vs 0.69 ng/mL for 5 and 10 mg, respectively) and a 31% increase in baseline-corrected fT C avg (4.75 vs 6.24 pg/mL for 5 and 10 mg, respectively). Neither dose resulted in any meaningful variation in dihydrotestosterone, estrone, estradiol, or sex hormone-binding globulin across the postdose sampling period.


CONCLUSIONS
The 5-mg TTC dose restores TT and fT levels to levels above and within the reference range, respectively, for premenopausal women.
From the 1Women's Health Research Program, School of Public Health and Preventive Medicine, Monash University, Melbourne, VIC, Australia; and 2School of Pharmacy and Medical Sciences and 3Sansom Institute for Health Research, University of South Australia, Adelaide, SA, Australia.
Ensieh
E
Fooladi
Stephanie E
SE
Reuter
Robin J
RJ
Bell
Penelope J
PJ
Robinson
Susan R
SR
Davis
D000279:Administration, Cutaneous; D015113:Androstane-3,17-diol / Q000097:blood; D018592:Cross-Over Studies; D013196:Dihydrotestosterone / Q000097:blood; D004970:Estrone / Q000097:blood; D005260:Female; D006801:Humans; D008875:Middle Aged; D017698:Postmenopause / Q000502:physiology*; D012738:Sex Hormone-Binding Globulin / Q000032:analysis; D013739:Testosterone / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*
D012738:Sex Hormone-Binding Globulin; D013196:Dihydrotestosterone; D015113:Androstane-3,17-diol; D004970:Estrone; D013739:Testosterone