Pharmacokinetics of Isofraxidin in Extracellular Fluids of Striatum in Rats Using Microdialysis-UPLC Method
基于微透析-UPLC技术的异嗪皮啶 大鼠脑纹状体细胞外液药动学研究

This study was aimed to observe the pharmacokinetic characteristics of isofraxidin in extracellular fluids of striatum in rats after oral administration of isofraxidin.Microdialysis and UPLC-MS analytical technology were employed in the study to detect the concentration of isofraxidin in microdialysis dialysate of extracellular fluids of striatum in rats,within 60 min after a single oral administration,with isofraxidin of 10 mg·kg-1 and 20 mg·kg-1,respectively.The results were revised by relative recovery in vivo.The pharmacokinetic parameters were calculated through non-compartment model method with software of WINONLIN 6.1 program.Main pharmacokinetic parameters of isofraxidin in extracellular fluids of striatum in rats after a single oral administration of isofraxidin at 10 mg·kg-1 and 20 mg·kg-1 were AUC0-∞(13973.88±1582.984) and(28059.76±4207.66) ng·min·mL-1;t1/2(16.68±0.49) and(17.41±2.88) min;Cmax(498.87±64.36) and(899.81±133.22) ng·mL-1.The tmax of both two groups was 15 min.Both the Cmax and tmax were measured.It is concluded that isofraxidin quickly permeates the blood-brain barrier and reaches the striatum.The maximal concentration of isofraxidin is 15 min after oral administration.And then the concentration decreases at a faster rate.It shows a significant dose-dependent phenomenon of the concentration of isofraxidin in extracellular fluids of striatum in rats.