Drug Molecule Diflunisal Forms Crystalline Inclusion Complexes with Multiple Types of Linear Polymers

作者：Zhong, Zhi; Guo, Canxiong; Yang, Xiaotong; Guo, Baohua; Xu, Jun^*; Huang, Yanbin^*

来源：Crystal Growth & Design, 2016, 16(3): 1181-1186.

DOI：10.1021/acs.cgd.6b00010

• CAMBRIDGE STRUCTURAL DATABASE
• X-RAY-DIFFRACTION
• SOLID-STATE NMR
• POLY(ETHYLENE OXIDE)
• CO-CRYSTALS
• CHEMICAL-SHIFTS
• PHARMACEUTICAL COCRYSTALS
• ANTIRETROVIRAL NEVIRAPINE
• SUPRAMOLECULAR SYNTHONS
• AROMATIC NANOCHANNELS

Co-crystals between drug molecules and coformers have shown great potential to optimize the stability and dissolution profiles of drugs. However, most of the coformers studied so far are small molecules. Here, we use diflunisal (DIF) as the model drug, and show that it could form co-crystals with multiple types of linear polymers in the form of crystalline inclusion complexes (ICs). These drug-polymer ICs were thoroughly characterized with single-crystal and powder XRD, solid-state NMR, DSC, and TGA, and showed similar channel structures, but their thermal properties changed with the type and molecular weight (MW) of the guest polymers. In addition, a strategy is proposed to identify the drug candidates with the potential to form ICs with polymers, which may help to expand the range of drug-polymer co-crystals.

• 出版日期2016-3
• 单位清华大学; 北京化工大学