High-performance liquid chromatographic determination of 17β-estradiol and 17β-estradiol-3-acetate solubilities and diffusion coefficients in silicone elastomeric intravaginal rings

Julie A. Russell*, R. Karl Malcolm, Katrina Campbell, A. David Woolfson

*Corresponding author for this work

Research output: Contribution to journalArticle

46 Citations (Scopus)

Abstract

A rapid, sensitive reversed-phase high-performance liquid chromatographic method has been developed for the determination of in vitro release of 17β-estradiol and its ester prodrug, 17β-estradiol-3-acetate, from silicone intravaginal rings. Partial hydrolysis of the acetate under the aqueous conditions provided by the 1% benzalkonium chloride release medium necessitates its conversion to 17β-estradiol prior to HPLC analysis. Both steroid peaks have been fully resolved from the benzalkonium chloride peaks by the reported chromatographic method, which employs a C18 bonded reversed-phase column, an acetonitrile-water (50:50, v/v) mobile phase and a UV detection wavelength of 281 nm. The peak area versus 17β-estradiol concentration was found to be linear over the range of 0.0137-1347 μgml-1. The HPLC method has also been used to determine the silicone solubilities and diffusion coefficients of the two related steroids. The almost 100-fold increase in 17β-estradiol-3-acetate release from the silicone core-type intravaginal rings compared to 17β-estradiol is shown to be due to a 60-fold increase in silicone solubility and a one and a half-fold increase in diffusitivity. The results demonstrate that an effective estrogen replacement therapy dose of 17β-estradiol may be administered from a silicone intravaginal reservoir device containing the labile 17β-estradiol-3-acetate prodrug. Copyright (C) 2000 Elsevier Science B.V.

Original languageEnglish
Pages (from-to)157-163
Number of pages7
JournalJournal of Chromatography B: Biomedical Sciences and Applications
Volume744
Issue number1
DOIs
Publication statusPublished - 07 Jul 2000

Keywords

  • 17β-Estradiol
  • 17β-Estradiol-3-acetate
  • Silicone

ASJC Scopus subject areas

  • Chemistry(all)

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