Resveratrol cocrystals with enhanced solubility and tabletability

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

doi:10.1016/j.ijpharm.2016.06.006

Resveratrol cocrystals with enhanced solubility and tabletability

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

Faculty of Health Sciences and Sports

Research output: Contribution to journal › Article › peer-review

99 Citations (Scopus)

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
Pages (from-to)	391-399
Number of pages	9
Journal	International Journal of Pharmaceutics
Volume	509
Issue number	1-2
DOIs	https://doi.org/10.1016/j.ijpharm.2016.06.006
Publication status	Published - 25 Jul 2016

Keywords

Cocrystal
Mechanical property
Resveratrol (RES)
Solubility
Tabletability

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10.1016/j.ijpharm.2016.06.006

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@article{c29ecde3707e4d30bc67134ae3c458a3,

title = "Resveratrol cocrystals with enhanced solubility and tabletability",

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.",

keywords = "Cocrystal, Mechanical property, Resveratrol (RES), Solubility, Tabletability",

author = "Zhengzheng Zhou and Wanying Li and Sun, {Wei Jhe} and Tongbu Lu and Tong, {Henry H.Y.} and Sun, {Changquan Calvin} and Ying Zheng",

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doi = "10.1016/j.ijpharm.2016.06.006",

language = "English",

volume = "509",

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journal = "International Journal of Pharmaceutics",

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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

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

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DO - 10.1016/j.ijpharm.2016.06.006

M3 - Article

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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 -

Resveratrol cocrystals with enhanced solubility and tabletability

Abstract

Keywords

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