稳定同位素法研究川芎哚药代动力学

Pharmacokinetic study of perlolyrine in rats by means of stable isotope dilution

目的 测定川芎哚 (川芎Ⅲ号碱 ,perlolyrine)的药代动力学参数。方法 以 [2 15N]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 .31h ,t1/ 2 β=4.6 2h ,t1/ 2ka=0 .10h ,tmax=0 .34h ,cmax=18.74ng·mL-1,K12 =0 .82h-1,K2 1=0 .38h-1,K10 =0 .2 9h-1,Vb=10 8.16L·kg-1,AUC =98.5 4ng·h·mL-1。结论 本法灵敏度高、特异性强及重现性和准确性好 。

OBJECTIVE To determine the pharmacokinetic parameters of perlolyrine in rats.METHODS The plasma concentration and pharmacokinetic parameters of perlolyrine were determined by means of GC MS with selected ion (m/z 247 and m/z 248) and [2 15 N]perlolyrine(m/z 248) as the internal standard.RESULTS The concentration time profile of perlolyrine after oral administration of perlolyrine fitted a two compartment open model.The pharmacokinetic parameters were t 1/2α =0.31 h, t 1/2β =4.62 h, t 1/2ka =0.10 h, t max =0.34 h, c max =18.74 ng·mL -1 , K 12 =0.82 h -1 , K 21 =0.38h -1 , K 10 =0.29 h -1 , V b=108.16 L·kg -1 , AUC =98.54 ng·h·mL -1 ,respectively.CONCLUSION The method is constant,sensitive and accurate.It provided a scientific basis for the clinical use of perlolyrine.