Bioavailability of estradiol from two matrix transdermal delivery systems: Menorest and Climara

Maturitas. 2000 Jan 15;34(1):57-64. doi: 10.1016/s0378-5122(99)00088-2.


Objectives: To compare two estradiol transdermal matrix systems with regard to bioavailability, pharmacokinetics and tolerability.

Methods: A single centre, open, randomized, comparative cross-over study in 20 healthy postmenopausal women. Menorest with 3 or 4 days of suggested use and Climara with 7 days of suggested use (both 50 microg/24 h) were compared at steady state. Two 14-day treatment periods were separated by a 4 week washout. Plasma levels of estradiol were monitored during the second week of each treatment. Tolerability was assessed by open questions and inspection of the application site.

Results: There were no differences between the two treatments with regards to AUC, Cmax, Cmin, Caverage or fluctuations of plasma estradiol. Tmax was significantly shorter for Menorest than Climara. Cmax and Cmin were significantly higher for the second Menorest patch during the monitoring period compared to the first. All local reactions were mild and there were three cases of erythema with Menorest and a total of 21 skin reactions in 15 subjects with Climara. Systemic tolerability was similar between treatments with eight estrogen-related adverse events in eight subjects (period pains, uterine bleeding, mastodynia, headache and vaginal discharge) with Menorest and 13 events in ten subjects with Climara.

Conclusions: The bioavailability of estradiol from the two matrix transdermal delivery systems Menorest and Climara was similar, but the products were not bioequivalent because Tmax was significantly shorter for Menorest than for Climara. Tolerability of treatment was good for both patches but with a higher number of local reactions and estrogen related adverse events for Climara.

Publication types

  • Clinical Trial
  • Comparative Study
  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Cutaneous
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Erythema
  • Estradiol / administration & dosage
  • Estradiol / blood
  • Estradiol / pharmacokinetics*
  • Female
  • Hormone Replacement Therapy*
  • Humans
  • Middle Aged
  • Postmenopause*


  • Estradiol