青娥丸方有效成分药动学-药效学相关性研究  

Analysis on pharmacokinetics-pharmacodynamics correlation of effective ingredients of Qing'e wan

作　　者：刘玲[1,2] 翁泽斌[3] 王恒[1,2] 朱星宇[1,2] 陈志鹏[1,2] 吴丽[1,2] 李伟东[1,2] 

机构地区：[1]南京中医药大学江苏省中药炮制重点实验室国家教育部中药炮制规范化及标准化工程研究中心,江苏南京210046 [2]南京中医药大学药学院,江苏南京210046 [3]中国药科大学,江苏南京210009

出　　处：《中国中药杂志》2016年第23期4436-4441,共6页China Journal of Chinese Materia Medica

基　　金：浙江省重中之重一级学科--中药学学科科研开放基金项目;江苏省高校自然科学基金重点项目(11KJA360001);江苏省高校"青蓝工程"项目(2014)

摘　　要：研究青娥丸方中3种有效成分京尼平苷酸、补骨脂素、异补骨脂素在大鼠体内的药代动力学过程与其抗骨质疏松作用的相关性。该实验通过大鼠灌胃给药青娥丸生品与盐炙品后,选取不同时间点进行眼眶取血,采用UHPLC-MS/MS测定大鼠血浆中京尼平苷酸、补骨脂素和异补骨脂素的药物浓度,绘制药-时曲线;以成骨细胞的增殖率为药效学指标,采用MTT法测定不同时间点含药血清作用于成骨细胞后的增殖率,绘制时-效曲线。比较时-效曲线和药-时曲线可以发现,在成骨细胞的增殖率达到峰值时,京尼平苷酸和补骨脂素的血药浓度也在峰值附近,表明两者具有较好的相关性。而异补骨脂素的血药浓度峰值相对于药效峰值具有一定的滞后性。将青娥丸生品及盐炙品各成分的时-效曲线与药-时曲线进行拟合,进行相关性分析,发现盐炙品组各成分的相关性略高于生品组。上述实验结果表明,青娥丸中京尼平苷酸、补骨脂素的药-时曲线和时-效曲线具有良好的相关性,且与生品相比,青娥丸盐炙品中两者的相关性更高。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 effecttime 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 saltprocessed Qing’e wan was better than the raw one.

关 键 词：青娥丸 药动学 药效学 京尼平苷酸 补骨脂素 异补骨脂素 

分 类 号：R285.5[医药卫生—中药学]