复方抗病毒制剂中贯叶连翘对莪术油药动学的影响研究

Study on effect of Hypericum perforatum on pharmacokinetics of zedoary turmeric oil in compound antiviral preparation

目的:研究莪术油及自制的复方抗病毒制剂给药后莪术油在新西兰兔体内的药物动力学。方法:采用反相高效液相色谱法检测给药后血浆中莪术油的标志性成分吉马酮的含量。结果:莪术油与复方抗病毒制剂灌胃给药后吉马酮的药时曲线符合开放二室模型。单方莪术油的药动学参数t1/2α,t1/2β,Vd,CL,AUC,Ka分别为(1.52±0.59),(1.97±0.27)h,(47.59±2.29)L·kg-1,(176.77±7.65)L·h-1·kg-1,(5.70±0.70)mg·h·L-1,(0.97±0.11)h-1,复方中莪术油则为(0.41±0.03),(1.47±0.35)h,(75.21±5.21)L·kg-1,(287.79±6.39)L·h-1·kg-1,(3.91±0.53)mg·h·L-1,(5.14±1.26)h-1。两者的t1/2α,t1/2β,Vd,CL,AUC并没有显著性差异,而复方的吸收速率Ka显著高于单方(P<0.05)。结论:复方抗病毒制剂中贯叶连翘没有影响莪术油有效成分在新西兰兔体内的分布和消除,但提高了莪术油的吸收速度,缩短了药物吸收的时间,有利于药物在体内迅速发挥作用。

Objective： To study zedoary turmeric oil （ZTO） and the pharmacokinetics of its homemade compound antiviral preparation in New Zealand rabbits. Method： RP-HPLC was used to determinate the content of germacrone in rabbit plasma after oral administration. Result： After oral administration of ZTO and its homemade compound antiviral preparation, the plasma concentrationtime curve of germacrone is in conformity to two-compartment open model. The pharmacokinetic parameters of ZTO： t1/2α, tl/2β, Vd, CL, AUC andKawere （1.52±0.59）, （1.97±0.27） h, （47.59±2.29） L. kg-1, （176.77 ±7.65） L. h-1 · kg-1, （5.70± 0. 70） mg · h · L - 1 and （ 0. 97 ± 0. 11 ） h - 1, respectively, while those of compound preparation were （0. 41 -± 0. 03 ）, （ 1.47 ± 0. 35 ） h, （75.21 ±5.21） L · kg-1, （287.79±6.39） L · h-1 · kg-1, （3.91 ±0.53） mg · h · L-1 and （5. 14±1.26） h-1, respectively. There was no significant difference between the above two groups of pharmacokinetic parameters, expect that Ka of compound prepa- ration was significantly higher than that of ZTO （P 〈0. 05）. Conclusion： Hypericum petforatum in compound preparation doesn＇t impact the distribution and elimination of active ingredients of ZTO in New Zealand rabbits, but it improves the absorption speed, and shortens the time of drug absorption, which contributes to rapid efficacy of ZTO in rabbits.