Solubility and Stability Advantages of a New Cocrystal of Berberine Chloride with Fumaric Acid

BBC
is a drug with a variety of activities but poor solubility. Cocrystal
technology is an effective method to improve the solubility and stability
of this type of compound. In this work, the cocrystal of BBC with
fumaric acid was obtained at a stoichiometric ratio of 2:1. Studies
on stabilities and solubilities were carried out using BBC dihydrate
and tetrahydrate as reference materials. Results showed that this
new cocrystal did not only significantly improve the dissolution rate
of BBC but also highly improved the stability in high humidity and
temperature. Given that the cocrystals formed by BBC as the host molecule
were few, different techniques were applied for characterization and
structural analyses. Moreover, theoretical calculations were performed
on weak interactions, such as hydrogen bonding and π–π
stacking interactions, which provided the research data for the study
of this kind of cocrystal.