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 language | English |
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Pages (from-to) | 157-163 |
Number of pages | 7 |
Journal | Journal of Chromatography B: Biomedical Sciences and Applications |
Volume | 744 |
Issue number | 1 |
DOIs | |
Publication status | Published - 07 Jul 2000 |
Keywords
- 17β-Estradiol
- 17β-Estradiol-3-acetate
- Silicone
ASJC Scopus subject areas
- Chemistry(all)