Liu Ling, Weng Ze-Bin, Wang Heng, Zhu Xing-Yu, Chen Zhi-Peng, Wu Li, Li Wei-Dong
Jiangsu Key Laboratory of Chinese Medicine Processing, Nanjing University of Chinese Medicine, Engineering Center for Standardization of Traditional Chinese Medicine Processing under State Ministry of Education, Nanjing 210046, China.
Pharmacy College of Nanjing University of Chinese Medicine, Nanjing 210046, China.
Zhongguo Zhong Yao Za Zhi. 2016 Dec;41(23):4436-4441. doi: 10.4268/cjcmm20162323.
To study the pharmacokinetics of three active ingredients in Qing'e wan, namely geniposidic acid, psoralen and isopsoralen, in rats, in order to investigate their correlation in the anti-osteoporotic effect. The rats were taken blood from their eye sockets at different time points after being orally administered with raw and salt-processed Qing'e wan. Geniposidic acid, psoralen and isopsoralen in rats plasma were determined by means of UHPLC-MS/MS to draw the concentration-time curve. The proliferation rate of osteoblasts was taken as the pharmacodynamic index, and determined by MTT method to draw effect-time curve. In comparison between the effect-time curve and the concentration-time curve, the blood concentrations of geniposidic acid and psoralen were close to the peak when the cell proliferation rate reached its peak, indicating a good correlation between them. The peak blood concentration of isopsoralen was slightly lagging behind the peak of efficacy. According to the correlation analysis after fitting the effect-time curve and the concentration-time curve, salt-processed Qing'e wan had a better correlation than the raw one. The above experimental results showed that the effect-time curve and the concentration-time curve of geniposidic acid and psoralen had a good correlation, and the correlation of salt-processed Qing'e wan was better than the raw one.
为研究青娥丸中3种活性成分（即京尼平苷酸、补骨脂素和异补骨脂素）在大鼠体内的药代动力学，以探讨它们在抗骨质疏松作用中的相关性。大鼠口服生品和盐炙品青娥丸后，于不同时间点从眼眶取血。采用超高效液相色谱-串联质谱法测定大鼠血浆中京尼平苷酸、补骨脂素和异补骨脂素的含量，绘制浓度-时间曲线。以成骨细胞增殖率作为药效学指标，采用MTT法测定并绘制效应-时间曲线。比较效应-时间曲线和浓度-时间曲线发现，当细胞增殖率达到峰值时，京尼平苷酸和补骨脂素的血药浓度接近峰值，表明二者具有良好的相关性。异补骨脂素的血药浓度峰值略滞后于药效峰值。对效应-时间曲线和浓度-时间曲线拟合后的相关性分析结果显示，盐炙品青娥丸的相关性优于生品。上述实验结果表明，京尼平苷酸和补骨脂素的效应-时间曲线与浓度-时间曲线具有良好相关性，且盐炙品青娥丸的相关性优于生品。
