Insight into the conformational polymorph transformation of a block-buster multiple sclerosis drug fingolimod hydrochloride (FTY 720)

Journal of Pharmaceutical and Biomedical Analysis
Jian-Rong WangXuefeng Mei

Abstract

Single-crystal structures of fingolimod hydrochloride (FTY 720), a block-buster multiple sclerosis drug, were revealed for the first time in this study. Three different conformational polymorphs (designated as forms I-III) were characterized using a variety of analytical techniques, including single-crystal XRD, VT-PXRD, DSC, HSM, and VT-confocal Raman spectroscopy. A temperature-dependent solid-solid transformation between different conformational polymorphs was observed to be reversible, and the transition process was studied using both VT-PXRD and VT-Raman techniques. Structural analysis revealed that the FTY 720 molecules adopt distinctive conformations in different polymorphs. Single-crystal to single-crystal transformation from form I to II was observed and was closely monitored by X-ray diffraction.

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Citations

Jan 5, 2018·Oncotarget·Ingo LangeDana-Lynn T Koomoa
Dec 29, 2020·Carbohydrate Polymers·Mohammed Nadim SardoiwalaSubhasree Roy Choudhury
Jan 7, 2021·Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy·Hesham SalemDina Heshmat

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