TY - JOUR
T1 - Resveratrol cocrystals with enhanced solubility and tabletability
AU - Zhou, Zhengzheng
AU - Li, Wanying
AU - Sun, Wei Jhe
AU - Lu, Tongbu
AU - Tong, Henry H.Y.
AU - Sun, Changquan Calvin
AU - Zheng, Ying
N1 - Publisher Copyright:
© 2016 Elsevier B.V. All rights reserved.
PY - 2016/7/25
Y1 - 2016/7/25
N2 - 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.
AB - 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.
KW - Cocrystal
KW - Mechanical property
KW - Resveratrol (RES)
KW - Solubility
KW - Tabletability
UR - http://www.scopus.com/inward/record.url?scp=84975078635&partnerID=8YFLogxK
U2 - 10.1016/j.ijpharm.2016.06.006
DO - 10.1016/j.ijpharm.2016.06.006
M3 - Article
C2 - 27282539
AN - SCOPUS:84975078635
SN - 0378-5173
VL - 509
SP - 391
EP - 399
JO - International Journal of Pharmaceutics
JF - International Journal of Pharmaceutics
IS - 1-2
ER -