Novel Salt-Cocrystals of Berberine Hydrochloride with Aliphatic Dicarboxylic Acids: Odd-Even Alternation in Physicochemical Properties

Lili Wang, Shuyu Liu, Jia Mei Chen, Yan Xiang Wang, Changquan Calvin Sun

Research output: Contribution to journalArticlepeer-review

Abstract

In this study, various structurally similar aliphatic dicarboxylic acids, namely, succinic acid, glutaric acid, adipic acid, and pimelic acid, were employed as coformers to obtain phase pure cocrystals with berberine chloride (BCl) by a slow solvent evaporation method. The structures of the four novel salt-cocrystals of BCl were determined by single crystal X-ray diffraction analysis and their solid-state properties were characterized. Compared with BCl·2H2O, all the cocrystals showed a higher melting point, improved powder dissolution and intrinsic dissolution rate (IDR), and lower hygroscopicity. It is noteworthy that the melting points and IDRs of these cocrystals exhibit an odd-even alternation with the carbon chain length of the acids.

Original languageEnglish (US)
Number of pages10
JournalMolecular pharmaceutics
Volume18
Issue number4
DOIs
StatePublished - Apr 5 2021

Bibliographical note

Funding Information:
This study was financially supported by the Postgraduate Research and Innovation Project of Shanghai University of Engineering Science (20KY0410) and the CAMS Initiative for Innovative Medicine (2016-I2M-1-011).

Publisher Copyright:
© 2021 American Chemical Society.

Keywords

  • aliphatic dicarboxylic acids
  • berberine chloride
  • intrinsic dissolution rate
  • melting point
  • odd-even alternation
  • salt-cocrystals

PubMed: MeSH publication types

  • Journal Article
  • Research Support, Non-U.S. Gov't

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