PHARMACOKINETIC CHARACTERISTICS, EFFICACY, AND SAFETY OF BUCCAL TESTOSTERONE IN HYPOGONADAL MALES - A PILOT-STUDY

Transbuccal administration of drugs provides an easy route of administ ration. To test the safety and efficacy of a novel testosterone (T) pr oduct, we performed a randomized, double blind, placebo-controlled stu dy in a parallel design. Men with serum T levels below 250 ng/dL were administered either an active buccal tablet containing 10 mg T (n = 7) or a buccal placebo tablet (n = 6) containing 3 mg pseudoephedrine HC l for taste matching. Men were studied while taking a standard T enant hate dose, after 6 weeks of a wash-out period, and after 8 weeks of th erapy. The men were matched for age (mean +/- SD, 41 +/- 16 vs. 47 +/- 16) and type of hypogonadism (three primary testicular failures in ea ch group, with the remainder having a central etiology). Acute pharmac okinetic testing showed peak serum hormone levels at 30 min, with a me an serum T concentration of 2688 +/- 147 ng/dL (range, 1820-3770 ng/dL ). Levels returned to baseline in 4-6 h, resulting in a total T area u nder the curve level of 3865 ng/hn . dL, less than that using other av ailable forms of T administration. Similar pharmacokinetics were obser ved for the hormone's metabolites, bioavailable T, free T, and estradi ol. After 8 weeks of treatment, the results of nocturnal penile tumesc ence studies evaluating rigidity and circumference were significantly different from those in the placebo group (P < 0.05) and comparable to those during T enanthate therapy. In conclusion, transbuccal T therap y was sufficient to maintain normal sexual function while minimizing t he total time of exposure to elevated circulating serum T levels.