Comparison of the pharmacokinetics of 17 beta-estradiol after a single 4-day application of Oesclim (R) 50, Oesclim (R) 100, and Vivelle (R) 0.05 (Menorest (R) 50) transdermal delivery systems

Oesclim(R) (Laboratoires Fournier Dijon, France), also known as Esclim(R) o r Esclima(R), is a new estradiol transdermal delivery system (TDS) develope d for the treatment of menopausal vasomotor symptoms. This open, randomized , three-way crossover study compared in 24 healthy postmenopausal women the pharmacokinetics of estradiol after a single 4-day application of Oesclim( R) 50, Oesclim(R) 100, and Vivelle(R) 0.05 (CibaGeneva Pharmaceuticals, Sum mit, NJ; known as Menorest(R) 50 in Europe, Rhone-Poulenc Rorer) on the upp er buttock Serum estradiol concentrations were determined by a validated ra dioimmunoassay method from samples taken before and during each TDS applica tion. The concentration-time profiles for Vivelle(R) 0.05 and Oesclim(R) 50 were comparable with a similar absorption rate, giving a maximum concentra tion (C-max) of 49 and 53 pg/mL above baseline, respectively, followed by a plateau throughout the 96-hour application period. At the end of this peri od, mean corrected estradiol concentrations were 18 and 19 pg/mL, respectiv ely. The estradiol serum concentrations obtain ed after an application of O esclim(R) 100 were approximately twice as high than with Oesclim(R) 50. All products were well tolerated, but skin intolerance was more frequent with Vivelle(R) 0.05 (4 patients; four reports) and Oesclim(R) 100 (3 patients; three reports) than with Oesclim(R) 50 (none). Problems of imperfect adhesi on were more than five times as frequent with Vivelle(R) 0.05 (44%) than wi th Oesclim(R) (8%). Journal of Clinical Pharmacology, 1999;39:821-816 (C) 1 999 the American College of Clinical Pharmacology.