大鼠灌胃给予维血宁颗粒后虎杖苷血药浓度测定及药动学研究

摘要

OBJECTIVE: To establish an RP-HPLC method for the determination of polydatin in rat plasma and its pharmacoki-netic study in vivo after ig. METHODS: The analysis was performed on a Diamonsil C18(200 mm×4.6 mm,5 μm) column, with the acetonitrile-water(20:80, V/V)as the mobile phase. The flow rate was 1 mL-min-1, and the detective wave length was set at 303 nm. The Weixuening granule was administrated by i.g, and blood samples were collected a different time and detected. The data were calculated by DAS2.0 software. RESULTS: The primary pharmacokinetic parameters of polydatin were as follows: tmax= (0.403±0.063) h,Cmax=( 1.715 ±0.097) mg-L-1,Ka:.= (6.894±3.275) h-1,t1/2a= (0.202 ±0.142) h-1,t12β=(2.484± 1.624) h-1,CL/ F= (32.229±22.027) L ? h-1-kg-1, V1/F= (14.447 ± 12.013) L-kg-1,AUC(0~t)=(1.511±0.550) mg-h-L-1 and AUC(0~∞)= (1.955± 0.765) mg-h-L-1. CONCLUSION: The pharmacokinetie behavior of polydatin in rats was fitted to two-compartment open model, and it is distributed and eliminated quickly in vivo.%目的:建立大鼠血浆中虎杖苷浓度的反相高效液相色谱(RP-HPLC)测定方法.方法:色谱柱为DiamonsilC18(200 mm×4.6 mm,5μm),流动相为乙腈-水(20∶80,V/V),流速为1.0 mL·min-1,柱温为35℃,检测波长为303 nm.大鼠ig维血宁颗粒后,测定不同时间血药浓度.采用DAS2.0药动学软件对血药浓度-时间数据进行拟合,计算相应药动学参数.结果:大鼠灌胃给予维血宁颗粒后,虎杖苷在大鼠体内药动学主要参数为:tmax=(0.403±0.063)h,Cmax=(1.715±0.097)mg·L-1,Ka=(6.894±3.275)h-1,t1/2α=(0.202±0.142)h,t1/2β=(2.484±1.624)h,CL/F=(32.229±22.027)L·h-1·kg-1,V1/F=(14.447±12.013)L·kg-1,AUC(0～t)=(1.511±0.550)mg·h·L-1,AUC(0-∞)=(1.955±0.765)mg·h·L-1.结论:虎杖苷在大鼠体内的药动学过程符合二室模型,进入体内分布迅速,代谢消除速度也较快.