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Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule

Objective To evaluate the bioavailability and safety of a novel vaginal capsule containing solubilized bioidentical 17β-estradiol for vulvar and vaginal atrophy and compare its pharmacokinetics with that of an approved vaginal estradiol tablet in healthy postmenopausal women. Methods Two randomized,...

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Autores principales: Pickar, J. H., Amadio, J. M., Bernick, B. A., Mirkin, S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Taylor & Francis 2016
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4819841/
https://www.ncbi.nlm.nih.gov/pubmed/26857443
http://dx.doi.org/10.3109/13697137.2015.1136926
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author Pickar, J. H.
Amadio, J. M.
Bernick, B. A.
Mirkin, S.
author_facet Pickar, J. H.
Amadio, J. M.
Bernick, B. A.
Mirkin, S.
author_sort Pickar, J. H.
collection PubMed
description Objective To evaluate the bioavailability and safety of a novel vaginal capsule containing solubilized bioidentical 17β-estradiol for vulvar and vaginal atrophy and compare its pharmacokinetics with that of an approved vaginal estradiol tablet in healthy postmenopausal women. Methods Two randomized, single-dose, two-way cross-over, relative bioavailability trials compared the pharmacokinetics of a solubilized vaginal estradiol softgel capsule (TX-004HR, test) with that of a vaginal estradiol tablet (Vagifem®, reference) in postmenopausal women (aged 40–65 years) at 10-μg and 25-μg doses. In each study, women were randomly assigned to receive a single dose of the test capsule or reference tablet, followed by a single dose of the alternate drug after a 14-day washout. Results Thirty-five women completed the 10-μg study and 36 completed the 25-μg study. Significantly lower systemic levels of estradiol, estrone, and estrone sulfate at both doses of the test product were observed compared with equivalent doses of the reference product, with lower AUC(0-24) and C (max) and earlier t (max). No adverse events were reported in either trial. Conclusion TX-004HR, a novel estradiol vaginal softgel capsule, exhibited significantly lower systemic exposure than equivalent doses of an approved vaginal estradiol tablet at both 10-μg and 25-μg doses. Both doses of each product were safe and well-tolerated.
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spelling pubmed-48198412016-04-22 Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule Pickar, J. H. Amadio, J. M. Bernick, B. A. Mirkin, S. Climacteric Original Article Objective To evaluate the bioavailability and safety of a novel vaginal capsule containing solubilized bioidentical 17β-estradiol for vulvar and vaginal atrophy and compare its pharmacokinetics with that of an approved vaginal estradiol tablet in healthy postmenopausal women. Methods Two randomized, single-dose, two-way cross-over, relative bioavailability trials compared the pharmacokinetics of a solubilized vaginal estradiol softgel capsule (TX-004HR, test) with that of a vaginal estradiol tablet (Vagifem®, reference) in postmenopausal women (aged 40–65 years) at 10-μg and 25-μg doses. In each study, women were randomly assigned to receive a single dose of the test capsule or reference tablet, followed by a single dose of the alternate drug after a 14-day washout. Results Thirty-five women completed the 10-μg study and 36 completed the 25-μg study. Significantly lower systemic levels of estradiol, estrone, and estrone sulfate at both doses of the test product were observed compared with equivalent doses of the reference product, with lower AUC(0-24) and C (max) and earlier t (max). No adverse events were reported in either trial. Conclusion TX-004HR, a novel estradiol vaginal softgel capsule, exhibited significantly lower systemic exposure than equivalent doses of an approved vaginal estradiol tablet at both 10-μg and 25-μg doses. Both doses of each product were safe and well-tolerated. Taylor & Francis 2016-03-03 2016-02-09 /pmc/articles/PMC4819841/ /pubmed/26857443 http://dx.doi.org/10.3109/13697137.2015.1136926 Text en © 2016 J. H. Pickar. Published by Taylor & Francis http://creativecommons.org/Licenses/by-nc-nd/4.0/ This is an Open Access article distributed under the terms of the Creative Commons Attribution-NonCommercial-NoDerivatives License (http://creativecommons.org/Licenses/by-nc-nd/4.0/), which permits non-commercial re-use, distribution, and reproduction in any medium, provided the original work is properly cited, and is not altered, transformed, or built upon in any way
spellingShingle Original Article
Pickar, J. H.
Amadio, J. M.
Bernick, B. A.
Mirkin, S.
Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
title Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
title_full Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
title_fullStr Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
title_full_unstemmed Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
title_short Pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
title_sort pharmacokinetic studies of solubilized estradiol given vaginally in a novel softgel capsule
topic Original Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4819841/
https://www.ncbi.nlm.nih.gov/pubmed/26857443
http://dx.doi.org/10.3109/13697137.2015.1136926
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