期刊
JOURNAL OF PHARMACEUTICAL SCIENCES
卷 107, 期 11, 页码 2860-2868出版社
ELSEVIER SCIENCE INC
DOI: 10.1016/j.xphs.2018.07.008
关键词
poorly water-soluble drug; polymorphs; surfactants; solubility; crystal structures; wetting and contact angles; X-ray powder diffraction (XRD); desolvation; HPLC
资金
- Shanghai Natural Science Foundation [18ZR1447900]
- Youth Innovation Promotion Association CAS [2016257]
- CAS Key Technology Talent Program
- SANOFI-SIBS Scholarship
Two polymorphs of celastrol were discovered and fully characterized by X-ray powder diffraction, thermogravimetry analysis, and differential scanning calorimetry. The single-crystal structures of form I and the isostructural solvate of form II were disclosed by single-crystal X-ray diffraction. The apparent solubility and wettability of both the crystalline forms were determined. It was found that surfactant can significantly improve the solubility of celastrol up to more than 104 times. Tween 80 and sodium dodecyl sulfate largely improved the wettability of the 2 crystals. Form I shows better wettability than form II in all the buffer solutions with polymers and surfactants. Compared with form II, form I exhibits higher solubility in carboxymethylcellulose and polyvinylpyrrolidone media but much lower solubility in tween 80 and sodium dodecyl sulfate solutions. An investigation of wettability and solubility mechanisms was fully explored, and a hypothesis was proposed to understand the abnormal solubility differences. (c) 2018 American Pharmacists Association (R). Published by Elsevier Inc. All rights reserved.
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