Resveratrol cocrystals with enhanced solubility and tabletability

Zhengzheng Zhou, Wanying Li, Wei Jhe Sun, Tongbu Lu, Henry H.Y. Tong, Calvin Sun, Ying Zheng

Research output: Contribution to journalArticlepeer-review

43 Scopus citations

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 languageEnglish (US)
Pages (from-to)391-399
Number of pages9
JournalInternational journal of pharmaceutics
Volume509
Issue number1-2
DOIs
StatePublished - 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.

Keywords

  • Cocrystal
  • Mechanical property
  • Resveratrol (RES)
  • Solubility
  • Tabletability

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