Modulating the Dissolution and Mechanical Properties of Resveratrol by Cocrystallization

被引：39

作者：

He, Hongyan ^{[1
,2
]}

Zhang, Qi ^{[1
]}

Li, Meiqi ^{[1
,2
]}

Wang, Jian-Rong ^{[1
]}

Mei, Xuefeng ^{[1
]}

机构：

[1] Chinese Acad Sci, Shanghai Inst Mat Med, Pharmaceut Analyt & Solid State Chem Res Ctr, Shanghai 201203, Peoples R China

[2] Univ Chinese Acad Sci, 19A Yuquan Rd, Beijing 100049, Peoples R China

来源：

CRYSTAL GROWTH & DESIGN | 2017年 / 17卷 / 07期

基金：

中国博士后科学基金; 中国国家自然科学基金;

关键词：

DRUG-DELIVERY SYSTEM; ORAL BIOAVAILABILITY; TABLETING PROPERTIES; SOLUBILITY; PARACETAMOL; ACID; PHARMACOKINETICS; TABLETABILITY; ENHANCEMENT; PERFORMANCE;

D O I：

10.1021/acs.cgd.7b00637

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Resveratrol (RSV), a dietary polyphenol found in red wine; has renewed interest in recent years due to a broad range of in vitro evidence that indicate cardioprotective effects. Herein; we have synthesized four RSV cocrystals with the objective to improve the physicochemical and mechanical properties. Single crystal structures were illustrated and comprehensive characterization of the cocrystals were performed. In addition, powder dissolution of RSV cocrystals in different buffer medium containing diffetent surfactants were conducted, and the result revealed that PVP K30 is an effective surfactant to maintain the supersaturation. Then phannacoldnetic experiments suggested that RSV cocrystals showed shorter T-max and RSV-NA exhibited higher C-max and AUC(0-24) values. Furthermore, RSV cocrystals exhibited superior mechanical properties compared to RSV pure component. These results may provide an alternative formulation for RSV.

引用

页码：3989 / 3996

页数：8

共 46 条

[1]

Aboarayes D. A., 2009, CRYSTAL ENG NUTRACEU

[2] Surfactant-mediated dissolution: Contributions of solubility enhancement and relatively low micelle diffusivity [J].