Pharmacokinetics and preliminary efficacy of two vaginal gel formulations of ultra-low-dose estriol in postmenopausal women

Climacteric : the Journal of the International Menopause Society
Juan L DelgadoC Nieto Magro

Abstract

To investigate the pharmacokinetics, safety and preliminary effectiveness of ultra-low-dose estriol vaginal gel formulations (20 μg/g (T1) and 50 μg/g (T2)) compared to Ovestinon® (estriol 500 μg/0.5 g (R)) and placebo in postmenopausal women. Forty-three volunteers were randomly assigned to received T1, T2, R or placebo once daily for 21 days. Absorption of estriol after single and multiple administration was analyzed. Cytological changes in the vagina, tolerability and safety were also investigated. Thirty-six women were included in the pharmacokinetic analysis. Systemic absorption was lower with test formulations (AUC0-t: 171.65 ± 80.18 (T1) and 406.75 ± 199.53 (T2) pg/ml × h) than with Ovestinon® (1221.97 ± 549.06 pg/ml × h). Estriol exposure of the test formulations after multiple administration (AUCss: 36.33 ± 30.52 (T1) and 73.71 ± 46.86 (T2) pg/ml × h) was significantly lower than after single-dose administration and not significantly different between them. In contrast, the exposure after repeated administration of Ovestinon® was considerable and not statistically different from levels after single administration. All estriol formulations produced similar improvement in the vaginal maturation value, while placebo showe...Continue Reading

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Aug 30, 2013·Menopause : the Journal of the North American Menopause Society

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Citations

May 16, 2017·Climacteric : the Journal of the International Menopause Society·G P SiliquiniN Biglia
Mar 17, 2017·Climacteric : the Journal of the International Menopause Society·M L'Hermite
Nov 28, 2018·British Journal of Clinical Pharmacology·Raimundo Vieira de Oliveira FilhoGilberto De Nucci
Nov 9, 2019·Minerva ginecologica·Angelo CagnacciUNKNOWN Società Italiana della Menopausa (SIM) and the Società Italiana di Ginecologia della Terza Età (SIGiTE)
Oct 24, 2019·Menopause : the Journal of the North American Menopause Society·Sônia M R R Lima, Juliana V Honorato
Sep 1, 2016·The Cochrane Database of Systematic Reviews·Anne LethabyHelen Roberts
Apr 10, 2020·Neurourology and Urodynamics·Nevine I D Te WestKate H Moore
Apr 11, 2017·Gynecological Endocrinology : the Official Journal of the International Society of Gynecological Endocrinology·Federica PalmaUNKNOWN as the writing group of the AGATA study
Nov 1, 2020·British Journal of Clinical Pharmacology·Nèvine Te WestKate Hilda Moore
Mar 2, 2021·The European Journal of Contraception & Reproductive Health Care : the Official Journal of the European Society of Contraception·Natalícia de Jesus AntunesGilberto De Nucci
May 14, 2021·Expert Opinion on Pharmacotherapy·Andrea R GenazzaniTommaso Simoncini

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