PMID: 9647353Jul 1, 1998Paper

Pharmacokinetics of the transdermal reservoir membrane system delivering beta-estradiol: in vitro/in vivo-correlation

Pharmaceutical Research
U D RohrT Kissel

Abstract

The aim of our study was to investigate the high fluctuations of Estradiol (E2) plasma levels transdermally delivered in postmenopausal women by a commercially available membrane controlled reservoir system (MCRS). The transdermal E2 flux either out of a complete MCRS or across its membrane out of defined ethanol water mixtures was determined, as well as E2 plasma profiles in 6 postmenopausal women produced by a MCRS. The transdermal in vitro E2 flux rate out of a complete MCRS, claimed to deliver 25 microg/day, increased steadily, reaching a maximum value of 2.06 +/- 0.58 microg/h at 30 to 40 hours and decreased to a rate of about 0.5 microg/h from 60 to 90 hours. No statistically significant differences between plasma profiles calculated from the in vitro investigation and derived from a clinical study could be identified. The E2 flux in defined ethanol/water mixtures across MCRS-membrane, adhesive and skin layer increased with increasing ethanol concentrations up to a maximum of 227 +/- 34 ng/cm2/h at an ethanol concentration of 62.5% (V/V) and decreased with further increase in the volume fraction of ethanol. In vitro as well as in vivo investigations showed high fluctuation of E2 plasma profiles in postmenopausal women pro...Continue Reading

Citations

Jul 1, 2009·Acta Pharmaceutica : a Quarterly Journal of Croatian Pharmaceutical Society and Slovenian Pharmaceutical Society, Dealing with All Branches of Pharmacy and Allied Sciences·Priya Ranjan Prasad Verma, Ashok R Chandak
May 1, 2010·Pharmaceutical Development and Technology·Ashok R Chandak, Priya Ranjan Prasad Verma
Dec 21, 2004·Skin Pharmacology and Physiology·A MahmoudM Schafer-Korting
Sep 23, 2010·Pharmaceutical Research·Yogeeta Narkar

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