Pharmacokinetic Characteristics, Efficacy, and Safety of Buccal Testosterone in Hypogonadal Males: A Pilot Study1

Abstract

Transbuccal administration of drugs provides an easy route of administration. To test the safety and efficacy of a novel testosterone (T) product, we performed a randomized, double blind, placebo-controlled study 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 ϭ 7) or a buccal placebo tablet (n ϭ 6) containing 3 mg pseudoephedrine HCl for taste matching. Men were studied while taking a standard T enanthate dose, after 6 weeks of a wash-out period, and after 8 weeks of therapy. The men were matched for age (mean Ϯ SD, 41 Ϯ 16 vs. 47 Ϯ 16) and type of hypogonadism (three primary testicular failures in each group, with the remainder having a central etiology). Acute pharmacokinetic testing showed peak serum hormone levels at 30 min, with a mean serum T concentration of 2688 Ϯ 147 ng/dL (range, 1820 -3770 ng/dL). Levels returned to baseline in 4 -6 h, resulting in a total T area under the curve level of 3865 ng/hn⅐dL, less than that using other available forms of T administration. Similar pharmacokinetics were observed for the hormone's metabolites, bioavailable T, free T, and estradiol. After 8 weeks of treatment, the results of nocturnal penile tumescence studies evaluating rigidity and circumference were significantly different from those in the placebo group (P Ͻ 0.05) and comparable to those during T enanthate therapy. In conclusion, transbuccal T therapy was sufficient to maintain normal sexual function while minimizing the total time of exposure to elevated circulating serum T levels. (J Clin Endocrinol Metab 83: 33-39, 1998)

The Roles of Androgens in Humans: Biology, Metabolic Regulation and Health

“…A number of other approaches to an efficient, safe (and comfortable) method of administration of T have been postulated and commercialized [ 451 ]: subcutaneous pellets [ 423 ], nasal gel or other applications [ 458 , 459 ], buccal tablets [ 460 ], subcutaneous injections [ 425 ], new oral preparations [ 427 ], combined transdermal and injected T [ 461 ], etc. In all cases, we encounter the same inactivation barrier problems (liver, digestive tract), and/or the difficulties of assessing concrete and precise doses of T for defined periods of time.…”

Andropause: Hormone Replacement Therapy in the Ageing Male

“…This induces high testosterone concentrations during a few hours, exceeding the physiological concentration. Later the testosterone concentration drops to values below normal [15, 16]. …”