文献类型：期刊文献

英文题名：Enhancing the solubility of natural compound xanthotoxin by modulating stability via cocrystallization engineering

作者：Chen, Jin-Yao[1,2,3];Wu, Hao[1,2,3];Guo, Chun-Yang[1,2,3];Zhu, Bin[1,2,3,4];Ren, Guo-Bin[1,2,3]

机构：[1]East China Univ Sci & Technol, Sch Pharm, State Key Lab Bioreactor Engn, 130 Meilong Rd, Shanghai 200237, Peoples R China;[2]East China Univ Sci & Technol, Sch Pharm, Engn Res Ctr Pharmaceut Proc Chem, Minist Educ, 130 Meilong Rd, Shanghai 200237, Peoples R China;[3]East China Univ Sci & Technol, Sch Pharm, Lab Pharmaceut Crystal Engn & Technol, 130 Meilong Rd, Shanghai 200237, Peoples R China;[4]Dali Univ, Yunnan Key Univ Lab Genuine Med Mat Resources Dev, Coll Pharmaceut Sci, 22 Wanhua Rd, Dali 671000, Peoples R China

年份：2019

卷号：572

外文期刊名：INTERNATIONAL JOURNAL OF PHARMACEUTICS

收录：;WOS:【SCI-EXPANDED(收录号:WOS:000500308000036)】；

基金：This work was supported by the National Natural Science Foundation of China (No. 21706064, No. 21776073, and No. 21908055), China, and Fundamental Research Funds for the Central Universities (No. 222201814049), China.

语种：英文

外文关键词：Xanthotoxin; Cocrystals; Crystal structure; Solubility; Stability

摘要：A comprehensive cocrystal study for the insoluble natural pharmaceutical compound xanthotoxin (XT) was conducted, in which xanthotoxin-para aminobenzoic acid (XT-PABA) and xanthotoxin-oxalic acid (XT-OA) cocrystals were obtained. The xanthotoxin cocrystals were characterized by powder X-ray diffraction, thermal analysis, and FT-IR spectra, and the crystal structures were determined by single-crystal X-ray diffraction. Crystal structures and thermal analysis showed that XT-OA was more stable than XT-PABA. Energy framework calculation indicated that H-bond and pi center dot center dot center dot pi interactions generated in XT-OA were stronger than that in XT-PABA and xanthotoxin. The powder dissolution experiments of xanthotoxin and its cocrystals suggested the XT-OA cocrystal might be applied as an alternative formulation of API, on account of its enhanced solubility and stability in the hydrochloric acid buffer solution (pH 1.2). The cocrystallization engineering can prolong the enhanced apparent solubility via modulating the stability.