Comparison of the pharmacokinetics of 17 beta-estradiol after a single 4-day application of Oesclim 50, Oesclim 100, and Vivelle 0.05 (Menorest 50) transdermal delivery systems.
Oesclim (Laboratoires Fournier, Dijon, France), also known as Esclim or Esclima, is a new estradiol transdermal delivery system (TDS) developed 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 50, Oesclim 100, and Vivelle 0.05 (CibaGeneva Pharmaceuticals, Summit, NJ; known as Menorest 50 in Europe, Rhône-Poulenc Rorer) on the upper buttock. Serum estradiol concentrations were determined by a validated radioimmunoassay method from samples taken before and during each TDS application. The concentration-time profiles for Vivelle 0.05 and Oesclim 50 were comparable with a similar absorption rate, giving a maximum concentration (Cmax) of 49 and 53 pg/mL above baseline, respectively, followed by a plateau throughout the 96-hour application period. At the end of this period, mean corrected estradiol concentrations were 18 and 19 pg/mL, respectively. The estradiol serum concentrations obtained after an application of Oesclim 100 were approximately twice as high than with Oesclim 50. All products were well tolerated, but skin intolerance was more frequent with Vivelle 0.05 (4 patients; four reports) and Oesclim 100 (3 patients; three reports) than with Oesclim 50 (none). Problems of imperfect adhesion were more than five times as frequent with Vivelle 0.05 (44%) than with Oesclim (8%).
Guichard
J P
JP
Department of Pharmacokinetics, Metabolism, and Toxicology, Laboratoires Fournier SA, Daix, France.
Sauron
R
R
Jones
A B
AB
D000279:Administration, Cutaneous; D000368:Aged; D019540:Area Under Curve; D001247:Asthenia / Q000139:chemically induced; D018592:Cross-Over Studies; D016503:Drug Delivery Systems; D004890:Erythema / Q000139:chemically induced; D004958:Estradiol / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics*; D005260:Female; D006261:Headache / Q000139:chemically induced; D006801:Humans; D008595:Menorrhagia / Q000139:chemically induced; D008875:Middle Aged; D010146:Pain / Q000139:chemically induced; D012867:Skin / Q000187:drug effects / Q000473:pathology; D013997:Time Factors
D004958:Estradiol