Kadota Kazunori, Okamoto Daiki, Sato Hideyuki, Onoue Satomi, Otsu Shigeyuki, Tozuka Yuichi
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.
Food Chem. 2016 Dec 15;213:668-674. doi: 10.1016/j.foodchem.2016.07.025. Epub 2016 Jul 6.
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.
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。