Pharmacokinetics of perlolyrine in rats by stable isotope dilution in conjunction with GC-MS.
OBJECTIVE
To determine the pharmacokinetics of perlolyrine in rats.


METHODS
The plasma concentration and pharmacokinetic parameters of perlolyrine were determined by gas chromatography-mass spectrometry (GC-MS) with selected ion (m/z 247 and m/z 248) and [2-(15) N] perlolyrine (m/z 248) as internal standard.


RESULTS
The concentration-time profile of perlolyrine after ig perlolyrine 2 mg.kg-1 fitted a two-compartment open model in rats. The pharmacokinetic parameters were T1/2 alpha = 0.33 h, T1/2 beta = 4.52 h, T1/2 (ka) = 0.14 h, Tmax = 0.35 h, Cmax = 18.84 micrograms/L, K12 = 0.88 h-1, K21 = 0.42 h-1, K10 = 0.32 h-1, V/F = 109.22 L.kg-1, AUC = 112.68 micrograms.h.L-1.


CONCLUSIONS
The method was constant, sensitive, and accurate. It provides a useful method for the determination of pharmacokinetics of perlolyrine which are important for clinical use of perlolyrine.
Tang
G H
GH
Department of Nuclear Medicine, Nan Fang Hospital, First Military Medical University, Guangzhou 510515, China. nfpet@fimmu.edu.cn
Jiang
G H
GH
Zheng
L F
LF
D000818:Animals; D002243:Carbolines / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D005663:Furans / Q000097:blood / Q000493:pharmacokinetics*; D008401:Gas Chromatography-Mass Spectrometry / Q000379:methods; D008297:Male; D009587:Nitrogen Isotopes; D051381:Rats; D017208:Rats, Wistar
D002243:Carbolines; D005663:Furans; D009587:Nitrogen Isotopes; C055781:perlolyrine