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Published on: July 4, 2014
Resveratrol cocrystals with enhanced solubility and tabletability
Zhengzheng Zhou1, Wanying Li2, Wei-Jhe Sun3
1State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macao; Hygiene Detection Center, Guangdong Provincial Key Laboratory of Tropical Disease Research, School of Public Health, Southern Medical University, Guangdong, Guangzhou 510515, China.
Two novel resveratrol cocrystals with 4-aminobenzamide and isoniazid were developed. These cocrystals demonstrate enhanced solubility and tabletability, making them promising for pharmaceutical tablet formulations.
Area of Science:
- Pharmaceutical Science
- Materials Science
- Crystallography
Background:
- Resveratrol (RES) is a polyphenol with potential health benefits but limited bioavailability.
- Developing novel formulations to improve RES solubility and delivery is crucial for therapeutic applications.
Purpose of the Study:
- To synthesize and characterize new resveratrol cocrystals with improved pharmaceutical properties.
- To evaluate the potential of these cocrystals for enhanced tablet formulation development.
Main Methods:
- Cocrystal synthesis using liquid-assisted grinding (LAG) and rapid solvent removal (RSR) with ethanol.
- Physicochemical characterization via PXRD, DSC, NMR, FT-IR, and HPLC.
- Evaluation of pharmaceutical properties: solubility, dissolution rate, tabletability, and hygroscopicity.
Main Results:
- Two new 1:1 cocrystals, RES-4ABZ and RES-ISN, were successfully synthesized.
- Both cocrystals exhibited significantly higher solubility and improved tabletability compared to pure resveratrol.
- The cocrystals demonstrated phase stability and were non-hygroscopic under high humidity.
Conclusions:
- The novel resveratrol cocrystals show enhanced solubility and tabletability, addressing key limitations of pure resveratrol.
- These RES cocrystals are promising candidates for developing advanced tablet formulations.
- The study highlights the utility of cocrystallization as a strategy for improving drug delivery and formulation characteristics.
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