Version 1
: Received: 17 June 2024 / Approved: 18 June 2024 / Online: 19 June 2024 (02:42:05 CEST)
How to cite:
Masum, Z. U.; Spoors, P. G.; Burke, M. D.; Gupta, V. Identification of New Polymorphic Patterns for Elacestrant Dihydrochloride. Preprints2024, 2024061250. https://doi.org/10.20944/preprints202406.1250.v1
Masum, Z. U.; Spoors, P. G.; Burke, M. D.; Gupta, V. Identification of New Polymorphic Patterns for Elacestrant Dihydrochloride. Preprints 2024, 2024061250. https://doi.org/10.20944/preprints202406.1250.v1
Masum, Z. U.; Spoors, P. G.; Burke, M. D.; Gupta, V. Identification of New Polymorphic Patterns for Elacestrant Dihydrochloride. Preprints2024, 2024061250. https://doi.org/10.20944/preprints202406.1250.v1
APA Style
Masum, Z. U., Spoors, P. G., Burke, M. D., & Gupta, V. (2024). Identification of New Polymorphic Patterns for Elacestrant Dihydrochloride. Preprints. https://doi.org/10.20944/preprints202406.1250.v1
Chicago/Turabian Style
Masum, Z. U., Matt D Burke and Vivek Gupta. 2024 "Identification of New Polymorphic Patterns for Elacestrant Dihydrochloride" Preprints. https://doi.org/10.20944/preprints202406.1250.v1
Abstract
Extensive polymorphism screening of elacestrant dihydrochloride, an Active Pharmaceutical Ingredient (API), was conducted using various methods and solvents. The solubility assessment and polymorph screening of elacestrant dihydrochloride (referred to as elacestrant throughout the paper) utilized both crystalline and amorphous forms of the API as input material with 40 non-conventional solvents, employing slow cooling, maturation, and/or evaporation. Crystalline material underwent further screening via anti-solvent addition, polymer templating, and solvent-drop grinding. A total of 7 new polymorphs were identified. No solvated forms were identified, but some samples contained notable water content, tentatively classified as hydrated forms. Comprehensive solid-state characterization data for representative crystalline samples of each polymorph is presented. Polymorph A exhibited the highest melt (225-226 °C, onset). Thermal analysis of polymorphs B, C, D, E, F and G showed an endothermic-exothermic event (with an onset temperature between 136 and 184 °C), indicating a form conversion, followed by a melt at 205-222 °C (onset), consistent with the previously identified and most stable form of elacestrant. This suggests that these materials convert to the most stable form prior to melting. Pattern G does not show an endothermic-exothermic event, but after desolvation, the material melts at 222 °C (onset temperature).
Medicine and Pharmacology, Medicine and Pharmacology
Copyright:
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
