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• W4224310514 abstract "The structural resemblance strategy is an often-employed principle to guide the discovery of novel pharmaceutical cocrystals and salts. Here, baricitinib (BAR) was selected as a model compound due to the existence of abundant heterocyclic nitrogen sites (proton acceptor sites) to form crystalline complexes with four structurally similar and pharmaceutically acceptable C4-dicarboxylic acids, maleic acid (MAL), fumaric acid (FUM), succinic acid (SUC), and l-tartaric acid (TAR). Crystal structures, intermolecular interactions, and physicochemical properties of each resulting form were analyzed to demonstrate the similarity and diversity. BAR–MAL and BAR–TAR are two salts with stoichiometric ratios of 2:2 and 2:1, respectively. BAR–FUM and BAR–SUC are isostructural cocrystals with a stoichiometric ratio of 1:0.5. All of these new solid-state forms demonstrated excellent phase stability against hydration, reduced hygroscopicity, and slight solubility improvements, supporting their usage as alternative forms of BAR for generic drug development." @default.
• W4224310514 created "2022-04-26" @default.
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• W4224310514 date "2022-04-25" @default.
• W4224310514 modified "2023-10-18" @default.
• W4224310514 title "Similarity and Diversity: Cocrystallization of Baricitinib with Four C4-Dicarboxylic Acids" @default.
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• W4224310514 doi "https://doi.org/10.1021/acs.cgd.2c00067" @default.
• W4224310514 hasPublicationYear "2022" @default.
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