Important effect of food on the bioavailability of oral testosterone undecanoate.
OBJECTIVE
To assess the effects of food on the bioavailability of testosterone undecanoate, testosterone, and 5alpha-dihydrotestosterone (DHT) after administration of a new oral testosterone undecanoate formulation, Andriol Testocaps.


METHODS
Randomized, open-label, crossover study with a 1-week washout period.


METHODS
Clinical pharmacology unit.


METHODS
Sixteen healthy postmenopausal women.


METHODS
Single oral doses of testosterone undecanoate 80 mg were administered either during a fasting period or after consumption of a standardized continental breakfast.


RESULTS
Serum concentrations of testosterone undecanoate were assayed by liquid chromatography with mass spectrometry detection; testosterone and DHT were assayed by gas chromatography with mass spectrometry detection. Serum concentrations of testosterone, testosterone undecanoate, and DHT were low to negligible when testosterone undecanoate was administered to subjects in a fasting state; these values were significantly higher when the test drug was coadministered with food. For testosterone, the maximum serum concentration and area under the plasma concentration-time curve were 0.67 ng/ml and 5.37 ng x hr/ml, respectively, in the fasting state, versus 10.7 ng/ml and 56.4 ng x hr/ml, respectively, in the fed state. The same parameters were also significantly higher for testosterone undecanoate and DHT in the fed versus fasting subjects.


CONCLUSIONS
Food increases the bioavailability of testosterone undecanoate, testosterone, and DHT. For proper absorption, Andriol Testocaps must be taken with meals.
Bagchus
Wilma M
WM
Clinical Pharmacology Department, Organon, Oss, The Netherlands. wilma.bagchus@organon.com
Hust
Rita
R
Maris
Frans
F
Schnabel
Peter G
PG
Houwing
Natalie S
NS
D000284:Administration, Oral; D000368:Aged; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D005215:Fasting / Q000378:metabolism; D005260:Female; D005502:Food; D006801:Humans; D007408:Intestinal Absorption; D008593:Menopause / Q000378:metabolism*; D008875:Middle Aged; D013739:Testosterone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000097:blood / Q000494:pharmacology*
D013739:Testosterone; C010792:testosterone undecanoate