当归芍药散中阿魏酸和芍药苷的药代动力学研究

目的:探讨当归芍药散君药中的2个主要活性成分-阿魏酸和芍药苷的药代动力学。方法:昆明种小鼠一次性灌胃后,采用高效液相色谱法测定不同时间小鼠体内阿魏酸和芍药苷的血药浓度。用3P87药动力程序对血药浓度-时间数据进行拟合。结果:从灌胃小鼠血清中检测到阿魏酸和芍药苷两种成分,它们的主要药动学参数为:阿魏酸Ke(0.330±0.085)1/h,Ka(0.555±0.133)1/h,t_(1/2(ka))(1.249±0.365)h,t_(1/2(ke))(2.101±0.665)h,T_(peak)(2.606±0.586)h,C_(max)(6.372±1.510)mg·L~(-1),AUC(41.399±11.763)mg·h~(-1)·L~(-1);芍药苷:Ke(0.511±0.117)1/h,Ka(0.656±0.121)1/h,t_(1/2(Ka))(1.056±0.263)h,t_(1/2(Ke))(1.356±0.281)h,T_(peak)(2.062±0.396)h,C_(max)(3.401±0.879)mg·L~(-1),AUC(16.047±3.767)mg·h·L~(-1)。本研究为临床提供了有价值的实验数据。

Study on Pharmacokinetics of Ferulic Acid and Paeoniflorin in Angelic-Paeonia Root Powder

OBJECTIVE: To study pharmacokinetics of ferulic acid and paeoniflorin that are two chief active compounds in Angelic-Paeonia Root Powder (APRP). METHODS: After the mice were administered by APRP through ig, HPLC was used to determine ferulic acid and paeoniflorin concentration in serum at different times. 3P87 procedure was used to process concentration-time data. RESULTS: Ferulic acid and paeoniflorin were detected from serum in the mice. The pharmacokinetics parameters were: Ferulic acid: Ke = 0.330 +/- 0.085 1/h, Ka = 0.555 +/- 0.133 1/h, t1/2(ka) = 1.249 +/- 0.365 h, t1/2(ke) = 2.101 +/- 0.665 h, Tpeak = 2.606 +/- 0.586 h, Cmax = 6.372 +/- 1.510 mg.L-1, AUC = 41.399 +/- 11.763 mg.h-1.L-1; Paeoniflorin: Ke = 0.511 +/- 0.117 1/h, Ka = 0.656 +/- 0.121 1/h, t1/2(Ka) = 1.056 +/- 0.263 h, t1/2(Ke) = 1.356 +/- 0.281 h, Tpeak = 2.062 +/- 0.396 h, Cmax = 3.401 +/- 0.879 mg.L-1, AUC = 16.047 +/- 3.767 mg.L-1. The present research provided valuable data for rational clinical practice of APRP.