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聚乙烯吡咯烷酮与姜黄素/α-葡萄糖基甜菊糖苷二元复合物的杂交改善了姜黄素的口服吸收和光化学稳定性。

Hybridization of polyvinylpyrrolidone to a binary composite of curcumin/α-glucosyl stevia improves both oral absorption and photochemical stability of curcumin.

作者信息

Kadota Kazunori, Okamoto Daiki, Sato Hideyuki, Onoue Satomi, Otsu Shigeyuki, Tozuka Yuichi

机构信息

Osaka University of Pharmaceutical Sciences, 4-20-1 Nasahara, Takatsuki, Osaka 569-1094, Japan.

Department of Pharmacokinetics and Pharmacodynamics, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.

出版信息

Food Chem. 2016 Dec 15;213:668-674. doi: 10.1016/j.foodchem.2016.07.025. Epub 2016 Jul 6.

Abstract

The tri-component system curcumin/α-glucosyl stevia (Stevia-G)/polyvinylpyrrolidone (PVP) was developed to improve the oral bioavailability and physicochemical properties of curcumin (CUR). The tri-component CUR formulation with Stevia-G and PVP was prepared with freeze-drying. The tri-component CUR system exhibited 13,000-fold higher solubility of CUR than the equilibrium solubility of CUR for 24h, indicating a stable tri-composite structure involving CUR. CUR could be converted into an amorphous form in the presence of Stevia-G and PVP by freeze-drying. The photo-degradation of CUR in the tri-component system was negligible even under an amorphous state of CUR. After oral administration in rats, the oral absorption of the tri-component CUR formulation (20mgCUR/kg) was 6.7-fold higher than that of crystalline CUR. The tri-component CUR formulation would therefore be a promising option to improve physicochemical properties and oral absorption of CUR.

摘要

开发了姜黄素/α-葡萄糖基甜菊糖苷(甜菊糖苷-G)/聚乙烯吡咯烷酮(PVP)三组分体系,以提高姜黄素(CUR)的口服生物利用度和理化性质。采用冷冻干燥法制备了含甜菊糖苷-G和PVP的三组分CUR制剂。三组分CUR体系中CUR的溶解度比CUR 24小时的平衡溶解度高13000倍,表明存在涉及CUR的稳定三复合结构。通过冷冻干燥,在甜菊糖苷-G和PVP存在下,CUR可转变为无定形形式。即使在CUR处于无定形状态下,三组分体系中CUR的光降解也可忽略不计。大鼠口服给药后,三组分CUR制剂(20mg CUR/kg)的口服吸收率比结晶CUR高6.7倍。因此,三组分CUR制剂有望成为改善CUR理化性质和口服吸收的选择。

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