Buccal application

Administration of testosterone via the buccal mucosa bypasses the liver and avoids first-pass clearance by delivering the drug directly into systemic circulation. Compared to sublingual administration, buccal mucosa is less permeable and potentially better suited for sustained delivery systems. An initial randomized, double-blind, placebo-controlled study in hypogonadal patients receiving 10 mg testosterone or placebo buccal tablets showed unfavourable pharmacokinetics with serum levels of testosterone far above the upper normal range and returning to baseline as soon as four to six hours after administration (Dobs etal. 1998).

Significantly improved pharmacokinetics were obtained with newly formulated buccal tablets. In a randomized, double-blind, crossover design 24 healthy men received a GnRH agonist for suppression of endogenous testosterone (Baisley etal. 2002). Buccal tablets containing 10, 20 or 30 mg testosterone were taken daily at 8.00 h for 10 days. Steady state was reached by day 5. Peak total and free testosterone were reached eight to nine hours after tablet application (Fig. 14.3). Hormone concentrations increased with the testosterone dose of the tablets, but this increase was less than dose-proportional. Whereas the average concentration of testosterone did not exceed the normal range, some individual blood samples still showed sup-raphysiological testosterone concentrations. About half of the volunteers reported local discomfort at the buccal application site, in most subjects during the first treatment period. The advantage of this buccal testosterone preparation seems to be the mimicking of the physiological circadian testosterone rhythm, however, long-term studies in hypogonadal patients including evaluation of acceptability are awaited.

A new testosterone bioadhesive buccal system was designed to adhere rapidly to the buccal mucosa and gellify for delivering testosterone steadily into the circulation. The pharmacokinetics were evaluated in 82 hypogonadal men. The tablet (30 mg testosterone) was applied twice daily to the upper gums for three months. 73% of the patients reached an average testosterone concentration over 24 hours within the physiological range. Local problems associated with tablet use were transient and minimal. This bioadhesive buccal system is approved for use in hypogonadal men in the U.S.A. and approval in Europe is expected.

Hair Loss Prevention

Hair Loss Prevention

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