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Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability
Dehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol...
Autores principales: | , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2022
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9699216/ https://www.ncbi.nlm.nih.gov/pubmed/36432669 http://dx.doi.org/10.3390/pharmaceutics14112478 |
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author | Jiang, Yihua Cheng, Yinxiang Xia, Mengyuan Zhang, Bingrui Ding, Qiaoce Lu, Liye Wang, Jian-Rong Mei, Xuefeng |
author_facet | Jiang, Yihua Cheng, Yinxiang Xia, Mengyuan Zhang, Bingrui Ding, Qiaoce Lu, Liye Wang, Jian-Rong Mei, Xuefeng |
author_sort | Jiang, Yihua |
collection | PubMed |
description | Dehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol (CAT), hydroquinone (HQ), resorcinol (RES), phloroglucinol (PG), 1,5-dihydroxy naphthalene (DHN), p-hydroxybenzoic acid (PHBA), gallic acid (GA), and 5-hydroxyisophthalic acid (5HIPA) were designed and synthesized. Some basic characterization tools, including powder X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, and Fourier transform infrared spectroscopy, were also applied in our work for basic analyses of cocrystals. It is indicated that DHEA-GA exhibits its superiority in dissolution and pharmacokinetic behaviors. While the area under the curve values of DHEA-GA is improved at the ratio of 2.2, the corresponding bioavailability of DHEA is expected to be accordingly increased. |
format | Online Article Text |
id | pubmed-9699216 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2022 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-96992162022-11-26 Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability Jiang, Yihua Cheng, Yinxiang Xia, Mengyuan Zhang, Bingrui Ding, Qiaoce Lu, Liye Wang, Jian-Rong Mei, Xuefeng Pharmaceutics Article Dehydroepiandrosterone (DHEA) is an FDA-approved food supplement used as an assisted reproductive sex hormone. The bioavailability is severely limited by its poor solubility (23 µg/mL). Herein, we aimed to modulate its solubility through cocrystallization. Eight cocrystals of DHEA with pyrocatechol (CAT), hydroquinone (HQ), resorcinol (RES), phloroglucinol (PG), 1,5-dihydroxy naphthalene (DHN), p-hydroxybenzoic acid (PHBA), gallic acid (GA), and 5-hydroxyisophthalic acid (5HIPA) were designed and synthesized. Some basic characterization tools, including powder X-ray diffraction, thermogravimetric analysis, differential scanning calorimetry, and Fourier transform infrared spectroscopy, were also applied in our work for basic analyses of cocrystals. It is indicated that DHEA-GA exhibits its superiority in dissolution and pharmacokinetic behaviors. While the area under the curve values of DHEA-GA is improved at the ratio of 2.2, the corresponding bioavailability of DHEA is expected to be accordingly increased. MDPI 2022-11-16 /pmc/articles/PMC9699216/ /pubmed/36432669 http://dx.doi.org/10.3390/pharmaceutics14112478 Text en © 2022 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (https://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Jiang, Yihua Cheng, Yinxiang Xia, Mengyuan Zhang, Bingrui Ding, Qiaoce Lu, Liye Wang, Jian-Rong Mei, Xuefeng Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
title | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
title_full | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
title_fullStr | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
title_full_unstemmed | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
title_short | Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability |
title_sort | dehydroepiandrosterone cocrystals with improved solubility and bioavailability |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9699216/ https://www.ncbi.nlm.nih.gov/pubmed/36432669 http://dx.doi.org/10.3390/pharmaceutics14112478 |
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