Pharmacokinetics of testosterone after percutaneous gel or buccal administration.
OBJECTIVE
To determine the pharmacokinetics of testosterone following its administration using transdermal gel or buccal lozenges.


METHODS
Pilot study.


METHODS
University-based hospital.


METHODS
Ten bilaterally oophorectomized women.


METHODS
Daily micronized testosterone gel (1 mg) and testosterone propionate lozenge (1 mg).


METHODS
Total testosterone, androstenedione, dihydrotestosterone, 3alpha-androstanediol glucuronide, and sex hormone-binding globulin were measured in serum by specific radioimmunoassays; free testosterone levels were also calculated.


RESULTS
Before treatment, serum testosterone levels in the groups using the lozenge and gel were 16 +/- 4.0 and 20 +/- 6.0 ng/dL, respectively. Mean maximum testosterone levels obtained with the lozenge occurred 1 hour after administration on days 1 (692 +/- 236 ng/dL) and 14 (836 +/- 309 ng/dL) of treatment and fell precipitously thereafter. In contrast, testosterone levels obtained with the gel showed a prolonged rise reaching maximal levels of 97 +/- 78 and 100 +/- 60 ng/dL after 18 hours. The serum level patterns of free testosterone, dihydrotestosterone, and 3alpha-androstanediol glucuronide were similar to the corresponding total testosterone levels.


CONCLUSIONS
Administration of testosterone lozenge by buccal absorption produced a rapid and brief elevation of testosterone levels, with levels reaching upper limits of the male range. In contrast, transdermal testosterone gel absorption resulted in a prolonged elevation of testosterone levels, which were in the hyperandrogenic female range but resembled steady state pharmacokinetics.
Slater
C C
CC
Department of Obstetrics and Gynecology, University of Southern California, Keck School of Medicine, Los Angeles, California, USA. coulam@hsc.usc.edu
Souter
I
I
Zhang
C
C
Guan
C
C
Stanczyk
F Z
FZ
Mishell
D R
DR
D000042:Absorption; D000279:Administration, Cutaneous; D000284:Administration, Oral; D015113:Androstane-3,17-diol / Q000031:analogs & derivatives / Q000097:blood; D002610:Cheek; D013196:Dihydrotestosterone / Q000097:blood; D005260:Female; D005782:Gels; D006801:Humans; D008875:Middle Aged; D010052:Ovariectomy; D010865:Pilot Projects; D013739:Testosterone / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D013997:Time Factors
D005782:Gels; D013196:Dihydrotestosterone; D015113:Androstane-3,17-diol; C028895:androstane-3,17-diol glucuronide; D013739:Testosterone