Resveratrol cocrystals with enhanced solubility and tabletability

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• 作者：Zhengzheng Zhou^a ; ^b ; Wanying Li^a ; Wei-Jhe Sun^c ; Tongbu Lu^d ; Henry H.Y. Tong^e ; Changquan Calvin Sun^c ; ^{sunx0053@umn.edu" class="auth_mail" title="E-mail the corresponding author} ; Ying Zheng^a ; ^{yzheng@umac.mo" class="auth_mail" title="E-mail the corresponding author}
• 关键词：Resveratrol (RES) ; Cocrystal ; Solubility ; Tabletability ; Mechanical property
• 刊名：International Journal of Pharmaceutics
• 出版年：2016
• 出版时间：25 July 2016
• 年：2016
• 卷：509
• 期：1-2
• 页码：391-399
• 全文大小：1850 K

文摘

Two new 1:1 cocrystals of resveratrol (RES) with 4-aminobenzamide (RES-4ABZ) and isoniazid (RES-ISN) were synthesized by liquid assisted grinding (LAG) and rapid solvent removal (RSR) methods using ethanol as solvent. Their physiochemical properties were characterized using PXRD, DSC, solid state and solution NMR, FT-IR, and HPLC. Pharmaceutically relevant properties, including tabletability, solubility, intrinsic dissolution rate, and hygroscopicity, were evaluated. Temperature-composition phase diagram for RES-ISN cocrystal system was constructed from DSC data. Both cocrystals show higher solubility than resveratrol over a broad range of pH. They are phase stable and non-hygroscopic even under high humidity conditions. Importantly, both cocrystals exhibit improved solubility and tabletability compared with RES, which make them more suitable candidates for tablet formulation development.