Pharmacokinetics, safety and tolerability of three dosage regimens of buccal adhesive testosterone tablets in healthy men suppressed with leuprorelin

J Endocrinol. 2002 Dec;175(3):813-9. doi: 10.1677/joe.0.1750813.

Abstract

We used a randomised, double-blind, crossover design to evaluate the pharmacokinetics, safety and tolerability of three doses of buccal adhesive testosterone tablets (BATT). Twenty-four healthy men, whose endogenous testosterone was suppressed to </=5.38 nmol/l with leuprorelin acetate, took BATT (10, 20 or 30 mg) daily for 10 days. There was a 4-day washout between treatments. Substantial testosterone absorption occurred from BATT, and mean serum testosterone, free testosterone and dihydrotestosterone (DHT) concentrations over 24 h showed circadian variation. Steady state was reached by day 5. Average 24-h concentrations for the three BATT doses were within the normal range for eugonadal men: testosterone 11.67-14.57 nmol/l, free testosterone 0.026-0.33 nmol/l and DHT 1.66-2.03 nmol/l. On all three doses, peak testosterone and free testosterone was reached 8-9 h after tablet application; DHT peaked about 1-2 h later, and declined more slowly. Hormone concentrations increased with BATT dose, but increases were less than dose-proportional. There was no evidence of testosterone accumulation. BATT was well tolerated.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial

MeSH terms

  • Administration, Buccal
  • Adult
  • Aged
  • Analysis of Variance
  • Area Under Curve
  • Cheek
  • Circadian Rhythm
  • Cross-Over Studies
  • Dihydrotestosterone / blood
  • Double-Blind Method
  • Drug Administration Schedule
  • Electrocardiography
  • Gingiva
  • Hormone Antagonists / pharmacology
  • Humans
  • Leuprolide / pharmacology
  • Lip
  • Male
  • Middle Aged
  • Mouth Mucosa / drug effects
  • Patient Satisfaction
  • Testosterone / administration & dosage*
  • Testosterone / blood
  • Testosterone / pharmacokinetics

Substances

  • Hormone Antagonists
  • Dihydrotestosterone
  • Testosterone
  • Leuprolide