E2101, a novel antispastic drug, was found to exist in at least two polymorphs that were confirmed by X-ray powder diffraction (XRD). These two species are designated forms I and II. The physicochemical and thermodynamic properties of these polymorphs were characterized by variable temperature XRD,
Solid-state characterization of a novel chemotherapeutic drug
โ Scribed by A. Marini; V. Berbenni; G. Bruni; A. Maggioni; P. Cofrancesco; C. Sinistri; A. Orlandi; M. Villa
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- English
- Weight
- 311 KB
- Volume
- 92
- Category
- Article
- ISSN
- 0022-3549
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โฆ Synopsis
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 80 degrees and 90 degrees C 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 150 degrees C causes decomposition of the anhydrous form and (above 190 degrees C) amorphization of the solid residue occurs.
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