124782-63-4Relevant articles and documents
Simultaneous Improvement of Epalrestat Photostability and Solubility via Cocrystallization: A Case Study
Putra, Okky Dwichandra,Umeda, Daiki,Nugraha, Yuda Prasetya,Nango, Kazuya,Yonemochi, Etsuo,Uekusa, Hidehiro
, p. 373 - 379 (2018)
In this study, we attempt to simultaneously improve the photostability and solubility of epalrestat (a drug used for neuropathy treatment) by preparing epalrestat-betaine zwitterionic cocrystals and characterize the physicochemical property alterations ac
New epalrestat crystal form as well as preparation method and application thereof
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Paragraph 0079-0081; 0103-0114, (2021/11/19)
The invention belongs to the technical field of medicines, and provides a novel epalrestat crystal form as well as a preparation method and application thereof. The X-ray powder diffraction pattern of the epalrestat new crystal form has characteristic diffraction peaks when the diffraction angles 2 theta are 6.39 +/-0.2 degrees, 7.57 +/-0.2 degrees, 12.69 +/-0.2 degrees, 14.67 +/-0.2 degrees, 15.04 +/-0.2 degrees, 21.79 +/-0.2 degrees, 24.36 +/-0.2 degrees, 25.59 +/-0.2 degrees, 27.30 +/-0.2 degrees and 31.48 +/-0.2 degrees. The epalrestat novel crystal form has excellent dissolution performance and water solubility, and the bioavailability of the epalrestat novel crystal form is improved; moreover, the epalrestat new crystal form has excellent flowability, the angle of repose can reach 26 degrees or below, the compression coefficient is smaller than 10%, the Hausner ratio is 1.00-1.11, and the epalrestat new crystal form is suitable for being used as a raw material medicine for production of prodrugs or pharmaceutical preparations of the epalrestat new crystal form.
STRUCTURAL ELUCIDATION OF EPALRESTAT(ONO-2235), A POTENT ALDOSE REDUCTASE INHIBITOR, AND ISOMERIZATION OF ITS DOUBLE BONDS
Ishida, Toshimasa,In, Yasuko,Inoue, Masatoshi,Ueno, Yoko,Tanaka, Chiaki,Hamanaka, Nobuyuki
, p. 959 - 962 (2007/10/02)
The structure of epalrestat (ONO-2235) is revised by X-ray single crystal analysis.The structures of the photoisomers are proposed on the basis of NMR and UV spectroscopic evidences.