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Comparison of the Pharmacokinetics of 17β‐Estradiol after a Single 4‐Day Application of Oesclim® 50, Oesclim® 100, and Vivelle® 0.05 (Menorest® 50) Transdermal Delivery Systems
Author(s) -
Guichard JeanPierre,
Sauron Ren ée,
Jones Anthony B.
Publication year - 1999
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1177/00912709922008470
Subject(s) - transdermal , pharmacokinetics , crossover study , medicine , radioimmunoassay , pharmacology , alternative medicine , pathology , placebo
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 (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 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%).