4.7 Article

Two Cocrystal Polymorphs of Palmatine Chloride with Racemic Hesperetin

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CRYSTAL GROWTH & DESIGN
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AMER CHEMICAL SOC
DOI: 10.1021/acs.cgd.1c01016

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  1. Natural Science Foundation of Fujian Province [2019J01758, 2020J01837]
  2. Research Projects of Minjiang University [MJY18003]

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Two polymorphic cocrystals of palmatine chloride with racemic hesperetin (Form I and Form II) were prepared and investigated, showing different supramolecular arrangements despite similar hydrogen-bonding interactions. Cocrystal formation decreases the solubility of palmatine chloride and improves the solubility of hesperetin, allowing for sustained release of palmatine chloride and enhanced release of hesperetin in pure water.
Two polymorphic cocrystals of palmatine chloride with racemic hesperetin (Form I and Form II) have been prepared and investigated systematically. Crystal structure analysis reveals that reliable O-H center dot center dot center dot Cl- hydrogen-bonding interactions exist in both cocrystal polymorphs. However, similar O-H center dot center dot center dot Cl- hydrogen-bonding interactions resulted in completely different supramolecular arrangements. Cocrystal Forms I and II are non-hygroscopic and show high stability against temperature, humidity, and light. The cocrystal formation greatly lowers the solubility of palmatine chloride, while the solubility of hesperetin has been improved. Sustained release of palmatine chloride and enhanced release of hesperetin from two cocrystal polymorphs in pure water were achieved.

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