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Related Experiment Videos

17Beta-estradiol delivered by three different matrix patches 50 microg/day: a three way cross-over study in 21

U D Rohr1, C Nauert, B Stehle

  • 1Department of Pharmaceutical Technology and Biopharmaceutics, Philipps-University, Marburg, Germany. uwerohr@t-online.de

Maturitas
|December 10, 1999
PubMed
Summary
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Maturitas·2000

Menorest patches demonstrated superior 17beta-estradiol (E2) bioavailability and reduced fluctuations compared to Tradelia and Estraderm MX. These findings suggest Menorest may offer more consistent E2 delivery for postmenopausal symptom management.

Area of Science:

  • Pharmacology
  • Endocrinology
  • Drug Delivery Systems

Background:

  • Transdermal 17beta-estradiol (E2) delivery is crucial for managing menopausal symptoms.
  • Comparing the pharmacokinetic profiles of different E2 matrix patches is essential for optimizing therapy.

Purpose of the Study:

  • To investigate and compare the systemic bioavailability and plasma profiles of E2 from three transdermal patches: Menorest, Tradelia, and Estraderm MX.
  • To evaluate pharmacokinetic parameters including AUC0-96h, Cmax, Tmax, Cmin, and C(average).

Main Methods:

  • A randomized, 3-way crossover study involving 21 postmenopausal women.
  • Application of three E2 matrix patches (Menorest, Tradelia, Estraderm MX) for 96 hours each, with a 7-day washout period.
  • Blood samples analyzed using radioimmunoassay to determine E2 plasma levels and pharmacokinetic parameters.

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Main Results:

  • Menorest exhibited the highest E2 bioavailability (AUC0-96h) and average plasma concentration (C(average)), with the lowest fluctuation.
  • Tradelia showed comparable bioavailability but higher fluctuations, while Estraderm MX displayed the lowest E2 plasma profiles.
  • Significant interindividual variability in E2 bioavailability was observed, with responders maintaining consistent responses across patches.

Conclusions:

  • The three transdermal E2 patches demonstrated distinct pharmacokinetic performances, with Menorest showing the most favorable profile for consistent E2 delivery.
  • Menorest and Tradelia provided the greatest reduction in menopausal symptoms compared to Estraderm MX.
  • Individual response variability is a key factor in transdermal E2 therapy effectiveness.