药学学报, 2021, 56(2): 585-592
吴秀娟, 庞遵霆, 杨思彤, 严梦梦, 高缘. 共无定形技术改善葛根素水溶性及增溶机制研究[J]. 药学学报, 2021, 56(2): 585-592.
WU Xiu-juan, PANG Zun-ting, YANG Si-tong, YAN Meng-meng, GAO Yuan. Mechanistic study on the solubility enhancement of puerarin by coamorphous technology[J]. Acta Pharmaceutica Sinica, 2021, 56(2): 585-592.

吴秀娟, 庞遵霆, 杨思彤, 严梦梦, 高缘
中国药科大学中药学院, 江苏 南京 211198
关键词:    葛根素      烟酰胺      溶出      液-液相分离      络合     
Mechanistic study on the solubility enhancement of puerarin by coamorphous technology
WU Xiu-juan, PANG Zun-ting, YANG Si-tong, YAN Meng-meng, GAO Yuan
School of Traditional Chinese Pharmacy, China Pharmaceutical University, Nanjing 211198, China
Puerarin (PUE), as an isoflavone component, has a wide range of pharmacological activities, while its poorly aqueous solubility limits the development of solid oral dosage forms. In this study, PUE along with nicotinamide (NIC) were prepared into the coamorphous system by solvent-evaporation method and characterized by powder X-ray diffraction (PXRD), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FT-IR). In addition, its dissolution behavior and solubilization mechanism were also investigated. PUE-NIC coamorphous was a single homogeneous binary system, with a single glass transition temperature at 35.1℃. In comparison to crystalline PUE, during the dissolution process, coamorphous PUE-NIC not only exhibited the "liquid-liquid phase separation" (LLPS) phenomenon, but the formation of Ap type complexation (1:1 and 1:2) between PUE and NIC molecules was also verified, which significantly improved the solubility of PUE and prolonged the supersaturation time, and would benefit its absorption.
Key words:    pueparin    nicotinamide    dissolution    liquid-liquid phase separation    complexation   
收稿日期: 2020-07-28
DOI: 10.16438/j.0513-4870.2020-1261
基金项目: 国家自然科学基金资助项目(81703712,81773675,81873012);中国药科大学“双一流”建设(CPU2018GY11,CPU2018GY27).
通讯作者: 高缘,Tel/Fax:86-25-83379418,E-mail:newgaoyuan@163.com
Email: newgaoyuan@163.com
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