Yang Lei, Sun Zhen, Zu Yuangang, Zhao Chunjian, Sun Xiaowei, Zhang Zhonghua, Zhang Lin
Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, 150040 Harbin, PR China.
Key Laboratory of Forest Plant Ecology, Ministry of Education, Northeast Forestry University, 150040 Harbin, PR China.
Food Chem. 2012 May 1;132(1):319-25. doi: 10.1016/j.foodchem.2011.10.083. Epub 2011 Oct 31.
The objective of the study was to prepare ursolic acid (UA) nanoparticles using the supercritical anti-solvent (SAS) process and evaluate its physicochemical properties and oral bioavailability. The effects of four process variables, pressure, temperature, drug concentration and drug solution flow rate, on drug particle formation during SAS process, were investigated. Particles with mean particle size ranging from 139.2±19.7 to 1039.8±65.2nm were obtained by varying the process parameters. The UA was characterised by scanning electron microscopy, X-ray diffraction, Fourier-transform infrared spectroscopy, thermal gravimetric analysis, specific surface area, dissolution test and bioavailability test. It was concluded that physicochemical properties and bioavailability of crystalline UA could be improved by physical modification, such as particle size reduction and generation of amorphous state using SAS process. Further, SAS process was a powerful methodology for improving the physicochemical properties and bioavailability of UA.
本研究的目的是采用超临界抗溶剂（SAS）工艺制备熊果酸（UA）纳米颗粒，并评估其理化性质和口服生物利用度。研究了压力、温度、药物浓度和药物溶液流速这四个工艺变量对SAS过程中药物颗粒形成的影响。通过改变工艺参数，获得了平均粒径范围为139.2±19.7至1039.8±65.2nm的颗粒。通过扫描电子显微镜、X射线衍射、傅里叶变换红外光谱、热重分析、比表面积、溶出度试验和生物利用度试验对UA进行了表征。得出结论，通过物理改性，如使用SAS工艺减小粒径和生成无定形状态，可以改善结晶UA的理化性质和生物利用度。此外，SAS工艺是一种改善UA理化性质和生物利用度的有效方法。
