Physicochemical Characterization of Tamoxifen Citrate Pseudopolymorphs, Methanolate and Ethanolate

概要

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Two novel pseudopolymorphs, methanolate and ethanolate of tamoxifen [(Z)-2-[4-(1, 2-diphenyl-1-butenyl)-phenoxy]-N, N-dimethylethylamine] citrate, were prepared in addition to forms A and B reported previously. Their crystalline forms were identified and characterized by powder and single crystal X-ray diffractometry, differential scanning calorimetry, thermogravimetric analysis, hot-stage microscopy, scanning electron microscopy and diffuse reflectance infrared Fourier-transform spectroscopy, and their physicochemical stability was also evaluated. The results of single crystal X-ray analysis and thermogravimetric analysis of methanolate and ethanolate suggested that the stoichiometry of tamoxifen citrate: methanol and tamoxifen citrate : ethanol could be composed of a 1 : 1 molecular ratio for both solvates. The results of physicochemical stability evaluations at 75 and 97% RH at 40 and 60℃ indicated that the metastable form A was quite stable for at least 2 months even under severe storage conditions, whereas methanolate immediately transformed to a crystalline mixture of forms A and B, and subsequently changed to the stable form B.
公益社団法人日本薬学会の論文
2007-03-01