Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability

doi:10.1021/acs.cgd.6b01863

CORC > 上海药物研究所 > 中国科学院上海药物研究所 > 药物质量控制与固体化学研究中心

	Cocrystals of Baicalein with Higher Solubility and Enhanced Bioavailability
	Zhu, Bingqing 1,2; Zhang, Qj 2; Wang, Jian-Rong2 ; Mei, Xuefeng2
刊名	CRYSTAL GROWTH & DESIGN
	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.
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关键词	IMPROVING SOLUBILITY ; ORAL BIOAVAILABILITY ; CANCER-CELLS ; NICOTINAMIDE ; DISSOLUTION ; FORMULATION ; POLYMORPHS ; ADVANTAGE
WOS研究方向	Chemistry ; Crystallography ; Materials Science
语种	英语
出版者	AMER CHEMICAL SOC
WOS记录号	WOS:000398884400055
内容类型	期刊论文
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.