Issue 39, 2015

Versatile solid modifications of icariin: structure, properties and form transformation

Abstract

A comprehensive solid-state screening experiment was performed for icariin (ICA), an active substance in Traditional Chinese Medicine (TCM) which has long been used to treat osteroporosis. Two new polymorphs in their pure forms and ten different solvate modifications were obtained and the single crystal structures were successfully determined. The isostructural phenomenon was readily observed among various organic solvates. Notably, the single crystal structure of the marketed hydrate form H1 was determined for the first time through a single crystal–single crystal transformation (SCSCT) process. The physicochemical properties of various solid forms were further studied. The results show that the newly discovered pure form α presents better thermal stability, lower hygroscopicity and higher solubility compared to the currently marketed form. The superior physicochemical properties render a better drug development ability for this widely applied TCM.

Graphical abstract: Versatile solid modifications of icariin: structure, properties and form transformation

Supplementary files

Article information

Article type
Paper
Submitted
20 Jul 2015
Accepted
29 Aug 2015
First published
31 Aug 2015

CrystEngComm, 2015,17, 7500-7509

Versatile solid modifications of icariin: structure, properties and form transformation

L. Jia, Q. Zhang, J. Wang and X. Mei, CrystEngComm, 2015, 17, 7500 DOI: 10.1039/C5CE01422K

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