姜黄素-胡椒碱固体分散体的制备与生物利用度研究  

Preparation and bioavailability of curcumin/piperine solid dispersions

作　　者：黄容 陆昕怡 韩加伟 李俊松[1,2] 狄留庆 HUANG Rong;LU Xin-yi;HAN Jia-weil;LI Jun-song;DI Liu-qing(College of Pharmacy,Nanjing University of Chinese Medicine,Nanjing 210023,China;Jiangsu Engineering Research Center for Efficient Delivery System of TCM,Nanjing 210023,China)

机构地区：[1]南京中医药大学药学院,江苏南京210023 [2]江苏省中药高效给药系统工程技术研究中心,江苏南京210023

出　　处：《中草药》2018年第19期4528-4534,共7页Chinese Traditional and Herbal Drugs

摘　　要：目的将姜黄素(CUR)和胡椒碱(PIP)组合物制成固体分散体(SD),提高CUR、PIP口服吸收率。方法采用溶剂挥发法,以溶出度为指标,利用X射线衍射(XRD)和差示扫描量热分析(DSC)对姜黄素-胡椒碱固体分散体(CUR-PIP SD)进行表征,并运用体外超饱和溶出法对制得的SD进行体外评价。同时应用UPLC-MS/MS研究大鼠ig给药后CUR和PIP的药动学行为。结果体外溶出实验显示,与原料药相比,SD中CUR和PIP溶出度均得到较大提高。大鼠药动学实验结果显示,与原料药相比,SD中CUR的生物利用度提高至2.71倍(P<0.05),PIP提高至2.68倍(P<0.05)。结论以PVP K30为载体制备的SD能够有效地改善CUR和PIP的体外溶出度以及生物利用度。Objective Solid dispersion of curcumin and piperine compositions（CUR-PIP SD） was prepared to increase the in vitro dissolution rate and the oral bioavailability of CUR and PIP. Methods The CUR-PIP SD was prepared by a solvent evaporation method with dissolution rate as index. The characterization of CUR-PIP SD was evaluated by differential scanning calorimetry（DSC）, X-ray powder diffraction（XRD）, and the resulting SD was evaluated by in vitro dissolution assay. UPLC-MS/MS was used to determine the plasma concentrations of CUR and PIP in rats after ig administration. Results In vitro dissolution experiments showed that the dissolution rate of CUR and PIP in SD were both greatly improved compared with that of raw materials. Oral bioavailability of CUR in the SD was 2.71 times of that of the drug substance（P 0.05）, and PIP was increased to 2.68 times（P 0.05）. Conclusion The SD prepared with PVP K30 can effectively increase the in vitro dissolution and bioavailability of CUR and PIP.

关 键 词：姜黄素 胡椒碱 固体分散体 超饱和溶出法 生物利用度 溶剂挥发法 溶出度 UPLC-MS/MS 药动学 

分 类 号：R283.6[医药卫生—中药学]