A Comparison of a Novel Testosterone Bioadhesive Buccal System, Striant, with a Testosterone Adhesive Patch in Hypogonadal Males

Abstract

A novel delivery system has been developed for testosterone replacement. This formulation, COL-1621 (Striant), a testosterone-containing buccal mucoadhesive system, has been shown in preliminary studies to replace testosterone at physiological levels when used twice daily. Therefore, the current study compared the steady-state pharmacokinetics and tolerability of the buccal system with a testosterone-containing skin patch (Andropatch or Androderm) in an international multicenter study of a group of hypogonadal men. Sixty-six patients were randomized into two groups; one applied the buccal system twice daily, whereas the other applied the transdermal patch daily, in each case for 7 d. Serum total testosterone and dihydrotestosterone concentrations were measured at d 1, 3 or 4, and 6, and serially over the last 24 h of the study. Pharmacokinetic parameters for each formulation were calculated, and the two groups were compared. The tolerability of both formulations was also evaluated. Thirty-three patients were treated with the buccal preparation, and 34 were treated with the transdermal patch. The average serum testosterone concentration over 24 h showed a mean of 18.74 nmol/liter (SD =; 5.90) in the buccal system group and 12.15 nmol/liter (SD =; 5.55) in the transdermal patch group (P < 0.01). Of the patients treated with the buccal system, 97% had average steady-state testosterone concentrations within the physiological range (10.41-36.44 nmol/liter), whereas only 56% of the transdermal patch patients achieved physiological total testosterone concentrations (P < 0.001 between groups). Testosterone concentrations were within the physiological range in the buccal system group for a significantly greater portion of the 24-h treatment period than in the transdermal patch group (mean, 84.9% vs. 54.9%; P < 0.001). Testosterone/dihydrotestosterone ratios were physiological and similar in both groups. Few patients experienced major adverse effects from either treatment. No significant local tolerability problems were noted with the buccal system, other than a single patient withdrawal. We conclude that this buccal system is superior to the transdermal patch in achieving testosterone concentrations within the normal range. It may, therefore, be a valuable addition to the range of choices for testosterone replacement therapy.

Testosterone and Erectile Function: From Basic Research to a New Clinical Paradigm for Managing Men with Androgen Insufficiency and Erectile Dysfunction

“…Hormonal agents [82,83] include testosterone, DHEA, clomiphene citrate, aromatase inhibitors, 5-alpha reductase inhibitors, dopamine agonists, and thyroid therapies [82,83]. For androgen insufficiency, androgen delivery systems, listed chronologically, include oral testosterone [137], intramuscular depot injections [138], scrotal transdermal patch systems [139], nongenital skin transdermal patch systems [140], hydroalcoholic testosterone gels, [141,142], adhesive buccal tablets [143], and, recently, longacting intramuscular depot injections [144]. Nonhormonal treatments include vasodilators such as PDE5 inhibitors and intracavernosal/intraurethral agents [145].…”

The benefits and risks of testosterone replacement therapy: a review

“…This formulation has been shown to restore serum testosterone concentrations to the physiological range within 4 hours of application, with steady-state concentrations achieved within 24 hours of twice-daily dosing 72 and achieves testosterone levels within the normal range. 73 Studies indicate that Striant ® is an effective, well-tolerated, convenient and discreet treatment for male hypogonadism.…”

Late-onset hypogonadism or ADAM: treatment

“…In general, studies show that this form of ART is capable of maintaining physiological levels of serum testosterone, is safe and well tolerated, and is an interesting option for ART in hypogonadal men (D) 41 (B). 43,44 The underreported sublingual form of testosterone administration should be used at a dose of 2.5 mg or 5 mg, 3 times a day. It is rapidly absorbed and metabolized, and it does not lead to a sustained increase in serum levels of dihydrotestosterone (DHT) and estradiol (D).…”

“…41 The most commonly used patches are non-scrotal, releasing 5 mg/day of testosterone and should be applied once a day on clean and dry glabrous skin (B). 43 Due to the large number of patches on the international market from different manufacturers, in the opinions of the authors, the tolerability of patients is quite variable due to local adverse effects. They are considered large and uncomfortable to use, and some formulations cause local reactions and exhibit low adhesion that ends up causing low acceptability by patients (B).…”

“…They are considered large and uncomfortable to use, and some formulations cause local reactions and exhibit low adhesion that ends up causing low acceptability by patients (B). 43 There are reports of patients who have discontinued treatment due to allergic reactions at the application site, even when using a local corticosteroid ointment (B). 44 On the other hand, the authors are unanimous regarding the efficacy and safety of this type of ART.…”