Pharmacokinetics of perlolyrine in rats by stable isotope dilution in conjunction with GC-MS

AIM: To determine the pharmacokinetics of perlolyrine in rats. METHODS: The plasma concentration and pharmacokinetic parameters of perlolyrine were de termined by gas chromatography-mass spectrometry (GCMS) with selected ion ( m/z 247 and m/z 248) and [2-(15) N] perlolyrine (m/z 248) as internal stand ard. RESULTS: The concentration-time profile of perlolyrine after ig perlol yrine 2 mg kg(-1) fitted a two-compartment open model in rats. The pharmaco kinetic parameters were T1/2 alpha =0.33 h, T1/2 beta= 4.52 h, T1/2(ka) = 0 .14 h, T-max = 0.35 h, C-max = 18.&2 mu g/L, K-12 = 0.88 h(-1), K-21 = 0.4 2 h(-1), K-10 = 0.32 h(-1), V/F = 109.22 L . kg(-1), AUC = 112.68 mu g . h . L-1. CONCLUSION: The method was constant, sensitive, and accurate. It pro vides a useful method for the determination of pharmacokinetics of perlolyr ine which are important for clinical use of perlolyrine.