In this study the single-crystal X-ray structure of the solvated species (nifedipine)2. 1,4-dioxane is reported for the first time. Included solvent molecules are located in isolated cavities in the crystal, yielding a very stable solvate. Desolvation of this species involves complete disruption of
Crystal forms of LY334370 HCl: Isolation, solid-state characterization, and physicochemical properties
✍ Scribed by Susan M. Reutzel-Edens; Rita L. Kleemann; Peggy L. Lewellen; Alfio L. Borghese; Luc J. Antoine
- Publisher
- John Wiley and Sons
- Year
- 2003
- Tongue
- English
- Weight
- 297 KB
- Volume
- 92
- Category
- Article
- ISSN
- 0022-3549
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✦ Synopsis
LY334370 HCl, a 5HT1f agonist investigated for the treatment of migraines, was identified in five crystal forms: three anhydrates (I-III), a dihydrate, and an acetic acid solvate. The identification and characterization of these crystal forms by optical microscopy, differential scanning calorimetry, thermogravimetric and moisture sorption analyses, solid-state NMR spectroscopy, and X-ray crystallography (Form I only) are presented. Physical properties, including hygroscopicity, solubility, and intrinsic dissolution rate, were assessed for Form I and the dihydrate, the two most viable crystal forms for commercial development. Surprisingly, anhydrous Form I was found to be the thermodynamically most stable crystal form in water, dissolving six times slower than the dihydrate, a difference that correlates well with the rank order of aqueous solubility.
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Ranitidine hydrochloride (RAN-HCl), a known anti-ulcer drug, is the product of reaction between HCl and ranitidine base (RAN-B). RAN-HCl has been extensively studied; however this is not the case of the RAN-B. The solid state characterization of RAN-B polymorphs has been carried out using different