Crystal forms of LY334370 HCl: isolation, solid-state characterization, and physicochemical properties

Journal of Pharmaceutical Sciences
S M Reutzel-EdensLuc J Antoine

Abstract

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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Citations

Feb 24, 2006·The Analyst·Robin K Harris
Jul 14, 2010·Journal of Pharmaceutical Sciences·Brian SamasBrian P Chekal
Mar 17, 2005·Journal of Pharmaceutical Sciences·Madhu Pudipeddi, Abu T M Serajuddin
Apr 23, 2009·Journal of Pharmaceutical Sciences·Rositza I PetrovaJ Michael Williams
Apr 27, 2010·International Journal of Pharmaceutics·Tommi Virtanen, Sirkka L Maunu
Jun 16, 2015·Molecular Pharmaceutics·Doris E BraunSusan M Reutzel-Edens
Nov 3, 2010·The Journal of Pharmacy and Pharmacology·Fang TianJukka Rantanen
Dec 29, 2004·International Journal of Pharmaceutics·Kunikazu MoribeKeiji Yamamoto
Feb 15, 2015·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·C SaalK Seemann

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