Solid-state characterization of a novel chemotherapeutic drug

We present the results of a thermal, spectroscopic, diffractometric, and microscopic study of a novel DNA intercalator synthesized by Novuspharma S.p.A. (code name BRR 2778, purity by high-performance liquid chromatography: 99.4%). We found that the form that is stable at room temperature contains 1.5 water molecules per unit of formula (or about 4.7% in mass): this water is reversibly lost in two stages below 80degrees and 90degreesC in dry and wet nitrogen atmosphere, respectively. The hydrated compound is a pseudo-polymorph and dehydration is accompanied by a structural change that modifies the diffraction pattern without changing the shape of the microcrystals. Annealing above 150degreesC causes decomposition of the anhydrous form and (above 190degreesC) amorphization of the solid residue occurs. (C) 2003 Wiley-Liss, Inc. and the American Pharmaceutical Association J Pharm Sci 92:577-584, 2003.