Pharmacokinetics of a single dose of buccal testosterone.

ABSTRACT

The bioavailability, pharmacokinetics, and metabolism of a novel transbuccal delivery system of testosterone was investigated in five healthy eugonadal men. Total serum testosterone (T), dihydrotestosterone (DHT), and sex hormone-binding globulin (SHBG) concentrations were determined from blood samples obtained at 800 a.m. (zero hour), and 30 min and 1, 2, 3, 4, 6, 12 and 24 hours later on day 1, and again on day 2, after dosing. This single transbuccal administration of Buccal T induced a prompt rise in serum T and DHT concentrations. The maximal concentration (Cmax) of T was 19.56 7.64 ng/mL (mean +/- SD; 5.3-fold increase from the baseline) at< 30 min (Tmax) after administration. The elimination half-life of Buccal T was about 1.75 h. Serum DHT peaked at 1 h at a concentration of 1.46 +/- 0.46 ng/mL (2.3-fold increase from the baseline). The drug was well tolerated. This study suggests that the Buccal T is a promising delivery system for natural T.