Lu Sheng-Wen, Zhang Ai-Hua, Sun Hui, Yan Guang-Li, Han Ying, Wu Xiu-Hong, Wang Xi-Jun
National TCM Key Laboratory of Serum Pharmacochemistry, Key Lab of Chinmedomics, Department of Pharmaceutical Analysis, Heilongjiang University of Chinese Medicine, Heping Road 24, Harbin, 150040, China.
Biomed Chromatogr. 2013 Dec;27(12):1657-63. doi: 10.1002/bmc.2976. Epub 2013 Jul 15.
This study aimed to investigate the in vivo behaviors of the main components in traditional Chinese medicine (TCM) fomulae. The plasma pharmacokinetics, tissue distribution and excretion of the main component-schisandrin in rats after oral administration of a classical TCM prescription, shengmaisan (SMS), were studied by a developed and validated UPLC-MS/MS method. The separation of schisandrin was achieved on a UPLC HSS T3 column with a mobile phase consisting of acetonitrile and water at a flow rate of 0.5 mL/min by linear gradient elution. The MS/MS detection was carried out by monitoring the fragmentation of m/z 415.22 → 384.26 for schisandrin on a triple quadrupole mass spectrometer. The result showed that the method was suitable for the quantification of schisandrin in plasma, tissue and excreta samples with satisfactory selectivity, precision, accuracy, sensitivity, linearity and recovery. Pharmacokinetic results showed a rapid absorption phase with the mean Tmax of 0.17 h and a relatively slow elimination proceeding with a half-life (T1/2 ) of 5.24 ± 1.28 h. The tissue distribution showed the maximum concentration distributions of schisandrin after oral administration of SMS were in the order of small intestine > large intestine > lung > liver > kidney > spleen > heart > brain. Only 0.005-0.006% of schisandrin was recovered in feces and was not detected in urine.
本研究旨在探讨中药方剂主要成分的体内行为。采用已建立并验证的超高效液相色谱-串联质谱(UPLC-MS/MS)方法,研究了经典中药方剂生脉散(SMS)灌胃给药后大鼠体内主要成分五味子醇甲的血浆药代动力学、组织分布及排泄情况。五味子醇甲在UPLC HSS T3柱上分离,流动相为乙腈和水,流速0.5 mL/min,采用线性梯度洗脱。在三重四极杆质谱仪上通过监测五味子醇甲m/z 415.22 → 384.26的碎片进行串联质谱检测。结果表明,该方法适用于血浆、组织和排泄物样品中五味子醇甲的定量分析,具有良好的选择性、精密度、准确度、灵敏度、线性和回收率。药代动力学结果显示吸收相迅速,平均达峰时间(Tmax)为0.17 h,消除相对较慢,半衰期(T1/2)为5.24 ± 1.28 h。组织分布显示,灌胃给予SMS后五味子醇甲的最大浓度分布顺序为小肠>大肠>肺>肝>肾>脾>心>脑。粪便中仅回收了0.005 - 0.006%的五味子醇甲,尿液中未检测到。