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 ［2-15N］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 t1/2α=0.31 h, t1/2β=4.62 h, t1/2ka=0.10 h, tmax=0.34 h, cmax=18.74 ng.mL-1,K12=0.82 h-1, K21=0.38h-1,K10=0.29 h-1,Vb=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.