LC-MS研究炒白芍提取物中芍药苷在大鼠体内的药代动力学

Pharmacokinetics study on paeoniflorin in Radix Paeoniae Alba extract by LC-MS

目的:建立LC-MS测定大鼠血浆中芍药苷含量的方法,并探讨其在大鼠体内的药动学行为。方法:大鼠灌胃不同剂量的炒白芍提取物后不同时间点采血,LC-MS法测定血药浓度,拟合药动学模型并计算相关药动学参数。结果:芍药苷在2.5～500μg·L-1(r=9994)线性关系良好。方法学考察均符合要求。大鼠灌胃炒白芍提取物0.2,0.4,0.8g·kg-1后,半衰期基本一致,AUC与给药剂量之间呈现良好的线性关系,属于线性动力学过程。结论:该法专属性强,灵敏度高,可用于芍药苷的体内定量分析,芍药苷在大鼠体内动力学过程符合一级吸收二室模型。

Objective： To develop a LC-MS method to determine paeoniflorin concentration in rats plasma. The method was applied to investigate pharmacokinetics of paeoniflorin in rats in vivo. Method： Blood samples were collected at different time after oral administration of Radix Paeoniae Alba extract at doses of O. 2, 0. 4, 0. 8 g · kg^-1. The paeoniflorin concentration in plasma was determined by LC-MS method. Pharmacokinetic parameters were fitted by WinNonlin 5.1 software package. Result： The linear range and the average recovery of paeoniflorin were 2. 5-500 μg · L^-1 （ r = 999 4）. and more than 80% （ n = 5 ）, respectively. The inner- and inter-days precision were both less than 15%. The T1/2 was similar. The relationship between dose and AUC showed good linearity. Conclusion： The method described in this report has high sensitivity and selectivity, and was suitable for pharmacokinetic study of paeoniflorin. The kinetic process of paeoniflorin in palsma showed two-compartment model after oral administration of Radix Paeoniae Alba extract at doses of 0.2, 0. 4, 0. 8 g · kg^-1 to rats.