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

Dezhi Yang; Junzi Cao; Lingtai Jiao; Shiying Yang; Li Zhang; Yang Lu; Guanhua Du

doi:10.1021/acsomega.0c00692

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

ACS Omega. 2020 Apr 6;5(14):8283-8292. doi: 10.1021/acsomega.0c00692. eCollection 2020 Apr 14.

Authors

Dezhi Yang¹, Junzi Cao¹, Lingtai Jiao¹, Shiying Yang¹, Li Zhang¹, Yang Lu¹, Guanhua Du²

Affiliations

¹ Beijing City Key Laboratory of Polymorphic Drugs, Center of Pharmaceutical Polymorphs, Institute of MateriaMedica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.
² Beijing City Key Laboratory of Drug Target and Screening Research, National Center for Pharmaceutical Screening, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China.

Abstract

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.