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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...

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Autores principales: Jiang, Yihua, Cheng, Yinxiang, Xia, Mengyuan, Zhang, Bingrui, Ding, Qiaoce, Lu, Liye, Wang, Jian-Rong, Mei, Xuefeng
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2022
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.
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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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