Pharmacokinetics of a new testosterone transdermal delivery system, TDS^®‐testosterone in healthy males

Abstract

Aims The Transdermal Delivery System (TDS®) is a liquid formulation that can be applied to the skin via a metered pump spray to deliver drug to the systemic circulation. The aims of this study were to assess the ability of the TDS® preparation to deliver testosterone systemically, and to characterize the pharmacokinetic profiles of the hormone in healthy males. Methods An open label, comparative, randomized placebo controlled study involving three treatments and three periods with a minimum of a 1 week washout period was conducted. Twelve healthy males received 50 mg TDS®‐testosterone, TDS®‐placebo, and 50 mg of a commercially available topical testosterone preparation (Androgel®, 1% topical testosterone gel). Results The mean AUC(0,12 h) was higher following application of TDS®‐testosterone (61.8 ng ml−1 h), compared with Androgel® (57.7 ng ml−1 h) and TDS®‐placebo (50.7 ng ml−1 h. The mean Cmax (0,12 h) was similar for TDS®‐testosterone (6.6 ng ml−1) and Androgel® (6.5 ng ml−1) and these values were higher than those for TDS®‐placebo (5.7 ng ml−1). Analysis of variance showed that the 90% confidence intervals on the relative difference of the ratio for the AUC(0,12 h) and the Cmax (0,12 h) between TDS®‐testosterone and Androgel®, were contained within the bioequivalence limit (80, 125%) (Cmax 89.2, 112.3% and AUC 93.5, 120.5%). Serum testosterone concentrations were lower following TDS®‐Placebo and were not bioequivalent either to the gel or spray. Conclusions The TDS® preparation was shown to deliver testosterone systemically to humans and the concentrations of the hormone in the 12 h following TDS® administration were bioequivalent to an existing topical delivery gel.

Effects of solvent deposited enhancers on transdermal permeation and their relationship with Emax

“…These topical preparations include gels, topical aerosols, and spray systems that contain volatile solvent(s) such as ethanol and/or water which evaporates upon application leaving the active drug and chemical enhancer on the skin surface. It has been suggested that these delivery systems are more convenient and patient friendly in comparison to other delivery systems such as transdermal patches [8]. For example, the metered dose aerosol system for the systemic delivery of drugs such as testosterone, estradiol, and buspirone has been recently investigated [9].…”

Therapeutic Potential of Testosterone Gels

“…Chik et al reported on a liquid T formulation that can be applied to the skin via a metered pump spray [147]. Comparing the pharmacokinetics of this spray (T 50 mg per dose) with those of T gel 50 mg, the serum T concentrations in the first 12 h following administration were found to be bioequivalent to the T gel.…”

“…Comparing the pharmacokinetics of this spray (T 50 mg per dose) with those of T gel 50 mg, the serum T concentrations in the first 12 h following administration were found to be bioequivalent to the T gel. Another group is also working on the development of T transdermal sprays [147,148].…”

Pharmacokinetic study of a new testosterone-in-adhesive matrix patch applied every 2 days to hypogonadal men

“…The 24 subjects had concomitant endocrine disorders (hypopituitarism (16), primary hypogonadism (5), hyperprolactinaemia (2), goitre (1) and hypothyroidism (1)). This resulted in concomitant medication for 22 subjects including thyroid hormones (14), glucocorticoids (12), somatropin or analogues (10) and prolactine inhibitors (8). Seven subjects affected by primary hypogonadism had FSH levels higher than the upper normal limit of 8 IU/L and the remaining 17 subjects suffering from secondary hypogonadism had FSH values lower than 8 IU/L except one hypopituitaric subject.…”