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New solid forms of tetrahydrocurcumin with improved solubility

文献类型：期刊论文

作者Tian, Fanyu2,3; Xia, Mengyuan1,2; Wang, Hao2,3; Zhang, Bingrui1,2; Ding, Zhenfeng1,2; Rong, Xiaoyi2; Zhu, Bingqing2; Mei, Xuefeng1,2,3
刊名CRYSTENGCOMM
出版日期2024-04-25
页码8
DOI10.1039/d4ce00259h
通讯作者Zhu, Bingqing() ; Mei, Xuefeng(xuefengmei@simm.ac.cn)
英文摘要Tetrahydrocurcumin (THC), one of the active metabolites of curcumin, possesses pharmacological activities similar to those of curcumin, such as hypoglycemic, hypolipidemic and antioxidant effects. However, poor water solubility of THC leads to unfavorable absorption, which limits its application. The aim of this study was to improve the solubility of THC through cocrystallization. Five cocrystals of THC with l-proline (THC-l-PRO), d-proline (THC-d-PRO), dl-proline (THC-dl-PRO), 4,4 '-bipyridine (THC-BPY), and betaine (THC-BTN) were discovered for the first time using liquid-assisted grinding. Single crystal structures of all THC co-crystals were analyzed and comprehensive characterization was performed through PXRD, thermal analysis, DVS and FT-IR. Dissolution studies were further conducted on two edible cocrystals THC-l-PRO and THC-BTN, and THC-l-PRO exhibits the highest apparent solubility compared with THC-BTN and the raw material. Moreover, THC-form II was found in THC-l-PRO dissolution experiments, and subsequently, the melt crystallization method was used to obtain the pure form of THC-form II. THC-form II was characterized for its physicochemical properties and the result of the dissolution experiment showed that it has better solubility compared to THC-form I. Tetrahydrocurcumin (THC), one of the active metabolites of curcumin, possesses pharmacological activities similar to those of curcumin, such as hypoglycemic, hypolipidemic and antioxidant effects.
WOS关键词CURCUMIN ; COCRYSTALS ; STABILITY
WOS研究方向Chemistry ; Crystallography
语种英语
WOS记录号WOS:001234103800001
出版者ROYAL SOC CHEMISTRY
源URL[http://119.78.100.183/handle/2S10ELR8/311788]  
专题中国科学院上海药物研究所
通讯作者Zhu, Bingqing; 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, 555 Zuchongzhi Rd, Shanghai 201203, Peoples R China
3.Nanjing Univ Chinese Med, Sch Chinese Mat Med, 138 Xianlin Ave, Nanjing 210023, Peoples R China
推荐引用方式
GB/T 7714		 Tian, Fanyu,Xia, Mengyuan,Wang, Hao,et al. New solid forms of tetrahydrocurcumin with improved solubility[J]. CRYSTENGCOMM,2024:8.
APA Tian, Fanyu.,Xia, Mengyuan.,Wang, Hao.,Zhang, Bingrui.,Ding, Zhenfeng.,...&Mei, Xuefeng.(2024).New solid forms of tetrahydrocurcumin with improved solubility.CRYSTENGCOMM,8.
MLA Tian, Fanyu,et al."New solid forms of tetrahydrocurcumin with improved solubility".CRYSTENGCOMM (2024):8.

入库方式： OAI收割

来源：上海药物研究所

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