LIU Ya-min, CHEN Qing, YANG Yan-jiao, et al. Pharmacokinetics Analysis of Brucine and Strychnine from Rebiqing Tablets in Rats[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(6): 79-83.
LIU Ya-min, CHEN Qing, YANG Yan-jiao, et al. Pharmacokinetics Analysis of Brucine and Strychnine from Rebiqing Tablets in Rats[J]. Chinese journal of experimental traditional medical formulae, 2016, 22(6): 79-83. DOI: 10.13422/j.cnki.syfjx.2016060079.
Objective: To calculate pharmacokinetic parameters of brucine and strychnine in rats after oral administration of Rebiqing tablets and Strychni Semen Pulveratum
and compare their pharmacokinetic characteristics in plasma. Method: UPLC-MS/MS was employed to determine contents of brucine and strychnine in rat plasma with Agela Venusil ASB C18column (2.1 mm×50 mm
3 μm)
taking acetonitrile-0.15% formic acid (60: 40) as mobile phase at 0.1 mL·min-1.Column temperature was 35 ℃.Internal standard was clenbuterol hydrochloride
UPLC-MS/MS was performed with electrospray ionization (ESI) and operated in positive mode in multiple reaction monitoring (MRM).Reaction selected ions were m/z 395.22-243.97 for brucine
m/z 335.14-183.96 for strychnine and m/z 277.11-202.87 for internal standard.Samples were extracted from rat plasma by liquid-liquid extraction.Pharmacokinetic parameters were calculated by DAS 2.1 software. Result: Main pharmacokinetic parameters of brucine in Rebiqing tablets and Strychni Semen Pulveratum were as follows:tmax of (27±11)
(40±12) min
Cmax of (5.6±1.2)
(4.5±1.7) μg·L-1
AUC0-t of (922±96)
(710±126) μg·min·L-1
CL/F of (4 596±306)
(87±34) L·min-1·kg-1;parameters of strychnine in them were (30±9)
(42±14) min
(27.3±10.8)
(15.9±7.0) μg·L-1
(3 957±651)
(2 031±256) μg·min·L-1 and (880 ±84)
(49±10) L·min-1·kg-1
respectively. Conclusion: Pharmacokinetic behavior of brucine and strychnine are well fitted to two-compartment model in rats.Compared with Strychni Semen Pulveratum
Rebiqing tablets can significantly improve oral bioavailability
accelerate absorption and elimination rate of brucine and strychnine.