Abstract
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.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 391-399 |
| Number of pages | 9 |
| Journal | International journal of pharmaceutics |
| Volume | 509 |
| Issue number | 1-2 |
| DOIs | |
| State | Published - Jul 25 2016 |
Bibliographical note
Funding Information:The authors thank Mr. Shan-Yue Guan at the Instrumental Analysis & Research Center of Sun Yat-Sen University for colleting the solution and solid state NMR data. Financial support from the Macao Science and Technology Development Fund ( 112/2013/A3 ) and Matching Grant from University of Macau ( MRG031/ZY/2015/ICMS ) are gratefully acknowledged. W-J. Sun was supported by a David Grant and Marilyn Grant Fellowship in Physical Pharmacy, Department of Pharmaceutics at the University of Minnesota.
Publisher Copyright:
© 2016 Elsevier B.V. All rights reserved.
Keywords
- Cocrystal
- Mechanical property
- Resveratrol (RES)
- Solubility
- Tabletability