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Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability

文献类型：期刊论文

作者Jiang, Yihua1,2; Cheng, Yinxiang1,2; Xia, Mengyuan1,2; Zhang, Bingrui1,2; Ding, Qiaoce2; Lu, Liye2; Wang, Jian-Rong2; Mei, Xuefeng1,2
刊名PHARMACEUTICS
出版日期2022-11-01
卷号14期号:11页码:20
关键词DHEA cocrystallization crystal structure solubility bioavailability
DOI10.3390/pharmaceutics14112478
通讯作者Wang, Jian-Rong(jrwang@simm.ac.cn) ; Mei, Xuefeng(xuefengmei@simm.ac.cn)
英文摘要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 mu g/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.
WOS关键词INTERMOLECULAR INTERACTIONS ; CRYSTAL
资助项目Natural Science Foundation of Shanghai ; [22ZR1473900]
WOS研究方向Pharmacology & Pharmacy
语种英语
WOS记录号WOS:000910824000001
出版者MDPI
源URL[http://119.78.100.183/handle/2S10ELR8/303787]  
专题中国科学院上海药物研究所
通讯作者Wang, Jian-Rong; Mei, Xuefeng
作者单位1.Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China
2.Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Jiang, Yihua,Cheng, Yinxiang,Xia, Mengyuan,et al. Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability[J]. PHARMACEUTICS,2022,14(11):20.
APA Jiang, Yihua.,Cheng, Yinxiang.,Xia, Mengyuan.,Zhang, Bingrui.,Ding, Qiaoce.,...&Mei, Xuefeng.(2022).Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability.PHARMACEUTICS,14(11),20.
MLA Jiang, Yihua,et al."Dehydroepiandrosterone Cocrystals with Improved Solubility and Bioavailability".PHARMACEUTICS 14.11(2022):20.

入库方式： OAI收割

来源：上海药物研究所

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