Yang Dezhi, Cao Junzi, Jiao Lingtai, Yang Shiying, Zhang Li, Lu Yang, Du Guanhua
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.
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.
ACS Omega. 2020 Apr 6;5(14):8283-8292. doi: 10.1021/acsomega.0c00692. eCollection 2020 Apr 14.
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.
BBC是一种具有多种活性但溶解度较差的药物。共晶技术是提高这类化合物溶解度和稳定性的有效方法。在本研究中，以2:1的化学计量比获得了BBC与富马酸的共晶。以BBC二水合物和四水合物作为参考物质进行了稳定性和溶解度研究。结果表明，这种新型共晶不仅显著提高了BBC的溶解速率，而且在高湿度和高温下的稳定性也有很大提高。鉴于以BBC作为主体分子形成的共晶较少，采用了不同技术进行表征和结构分析。此外，还对氢键和π-π堆积相互作用等弱相互作用进行了理论计算，为这类共晶的研究提供了研究数据。
