Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability
文献类型:期刊论文
作者 | Zhu, Bingqing1,2; Zhang, Qj2; Wang, Jian-Rong2![]() ![]() |
刊名 | CRYSTAL GROWTH & DESIGN
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出版日期 | 2017-04 |
卷号 | 17期号:4页码:1893-1901 |
ISSN号 | 1528-7483 |
DOI | 10.1021/acs.cgd.6b01863 |
文献子类 | Article |
英文摘要 | Baicalein (Bai) is one of the most, important bioactive flayonids isolated from the well-known traditional Chinese medicine called "Huang Qm". Though,it has broad therapeutic capability, the bioavailability is limited due to its poor solubility. In this study, we aimed to modulate its solubility-through cocrystallization. Cocrystals of Bai with isoniazide (Inia), isonicotinamide (Inam), caffeine (Caf), and theophylline (Tph) were obtained. And different cocrystallilation methods lead to different cocrystal phases for Inam and Tph. These cocrystals were characterized using powder X-ray diffraction, thermogravimetric analysis, differential scanning calorinietry, dynamic vapor :sorption, and Fourier transform infrared spectroscopy. Among all the cocrystals studied, BaiCaf is found to be superior in powder dissolution and pharmacokinetic behavior. Area under the curve values of BaiCaf is improved by a factor of 4:1, and the,bioavailability of baicalein is thus expected to be accordingly increased. Given that Caf is a central nervous system stimulant available in many prescription and nonprescription medications, BaiCaf can be a promising, alternative solid form: of Bai to be developed. |
WOS关键词 | IMPROVING SOLUBILITY ; ORAL BIOAVAILABILITY ; CANCER-CELLS ; NICOTINAMIDE ; DISSOLUTION ; FORMULATION ; POLYMORPHS ; ADVANTAGE |
资助项目 | National Natural Science Foundation of China[81273479] ; National Natural Science Foundation of China[81402898] ; Youth Innovation Promotion Association CAS[2016257] ; CAS Key Technology Talent Program[00000000] ; SANOFI-SIBS Scholarship[00000000] |
WOS研究方向 | Chemistry ; Crystallography ; Materials Science |
语种 | 英语 |
WOS记录号 | WOS:000398884400055 |
出版者 | AMER CHEMICAL SOC |
源URL | [http://119.78.100.183/handle/2S10ELR8/272720] ![]() |
专题 | 药物质量控制与固体化学研究中心 |
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 | Zhu, Bingqing,Zhang, Qj,Wang, Jian-Rong,et al. Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability[J]. CRYSTAL GROWTH & DESIGN,2017,17(4):1893-1901. |
APA | Zhu, Bingqing,Zhang, Qj,Wang, Jian-Rong,&Mei, Xuefeng.(2017).Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability.CRYSTAL GROWTH & DESIGN,17(4),1893-1901. |
MLA | Zhu, Bingqing,et al."Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability".CRYSTAL GROWTH & DESIGN 17.4(2017):1893-1901. |
入库方式: OAI收割
来源:上海药物研究所
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