川芎哚药代动力学参数的稳定同位素法测定

目的　测定川芎哚 (川芎III号碱 ,perlolyrine)的药动学参数。方法　以氘标川芎哚为内标准及GC MS的SIM(选择性离子监测 )为检测手段 ,定量测定大鼠体内川芎哚的含量及其药代动力学参数。结果　川芎哚在大鼠体内呈二室模型分布 ,其药代动力学参数为 :T1/ 2α=0 34h ,T1/ 2 β=4 5 9h ,T1/ 2 (Ka) =0 12h ,Tmax=0 36h ,Cmax=18 86μg·L-1,K12 =0 87h-1,K2 1=0 40h-1,K10 =0 31h-1,VB=10 7 86L·kg-1,AUC =99 6 8μg·h·L-1。结论　本法灵敏度高、特异性强和准确性好 ,为临床应用提供了科学依据。

Pharmacokinetics determination of perlolyrine by stable isotope dilution

AIM To determine pharmacokinetics parameters of perlolyrine in rats. METHODS The plasma concentration and pharmacokinetics parameters of perlolyrine were determined by means of GC MS with selected ion (m/z 247 and m/z 248) and deuterium labelled perlolyrine (m/z 248) as internal standard. RESULTS The concentration time profile of perlolyrine after oral administration of perlolyrine fitted a two-compartment open model in rats. The pharmacokinetics parameters were T 1/2α =0 34 h, T 1/2β = 4 59 h, T 1/2 ( K a)= 0 12 h, T max =0 36 h, C max =18 86 μg·L -1 , K 12 =0 87 h -1 , K 21 =0 40 h -1 , K 10 =0 31 h -1 , V B=107 86 L·kg -1 , AUC =99 68 μg·h -1 ·L -1 . CONCLUSION The method is constant, sensitive and accurate, which provides a scientific basis for clinical use of perlolyrine.