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1、人参茎叶总皂昔脂质体与水溶液在大鼠体内的血药浓度及药代动力学参数对比分析［摘要］该试验探讨人参茎叶❷皂背脂质体与水溶液在大鼠体内的血药浓度及药代动力学参数对比差异。通过大鼠静脉注射人参茎叶总皂昔水溶液和脂质体后，用高效液相色谱法检测血浆不同时间点的9种主要人参皂昔单体Rgl,Re,Rf,Rbl,Rg2,Rc,Rb2,Rb3,Rd的血药浓度,通过3p97软件拟合数据。大鼠静脉给药后，血浆中可测得9种目标皂背。水溶液的达峰时间一般在0.05〜0.0833h；脂质体的达峰时间一般在0.5h之后。经软件拟合
2、后，人参皂背Rgl,Re,Rf,Rg2,Rc,Rd,Rb3的水溶液均为二室模型，脂质体为一室模型;人参皂昔Rbl的水溶液和脂质体为三室模型;Rb2的水溶液为三室模型，脂质体为一室模型。9种皂昔脂质体的药-时曲线下面积均大于水溶液的曲线下面积，而且脂质体在体内停留时间较长，清除率较水溶液的清除率慢，半衰期一般也较水溶液长。研究结果显示通过静脉注射给药方式，对2种剂型的药动学参数进行对比，人参茎叶总皂昔脂质体与水溶液在大鼠体内的药动学显著不同，脂质体使药物在体内的浓度维持较长时间，降低了药物体内消除速度
3、，提高药物疗效。人参茎叶总皂昔脂质体与传统剂型相比，提高了药物的缓释长效，为今后研发人参皂背新剂型起到了重要意义。[关键词]人参茎叶总皂昔；药代动力学；脂质体；水溶液；静脉注射[Abstract]Theexperimentwasaimedtoinvestigatethedifferenceofplasmaconcentrationandpharmacokineticparametersbetweenliposomeandaqueoussolutionoftoatalginsenosideofgins
4、engstemsandleavesinrats,suchasginsenosidesRgLRe,Rf,RbLRg2,Rc,Rb2,Rb3,Rd.Afterintravenousinjectionofliposomeandaqueoussolutioninrats,thebloodwastakenfromthefemoralveintodetecttheplasmaconcentrationoftheabove9ginsenosidemonomersindifferenttimepointsbyusi
5、ngHPLC・Theconcentration-timecurvewasobtainedand3p97pharmacokineticsoftwarewasusedtogetthepharmacokineticparameters・Aftertheintravenousinjectionofginsenosidestorats,nineginsenosidesweredetectedinplasma.Ingeneral,amongtheseginsenosides,thepeaktimeoftheaq
6、ueoussolutionwasbetween0.05to0.0833h,andtheserumconcentrationpeakofliposomeusuallyappearedafter0.5h.Aftersoftwarefitting,theaqueoussolutionofginsenosidemonomersRgl,Re,Rf,Rg2,Rc,Rd,Rb3wastwo-compartmentmodel,andtheliposomeswereone-compartmentmodel；aqueo
7、ussolutionandliposomeofginsenosidemonomersRblwerethree-compartmentmodel；aqueoussolutionofginsenosidemonomersRb2wasthree-compartmentmodel,anditsliposomewasone-compartmentmodel.Areaunderthedrugtimecurveofthese9kindsofsaponinliposomeswaslargerthanthatofaq
8、ueoussolution,andtheretentiontimeoftheliposomeswaslongerthanthatoftheaqueoussolution；theremovalratewasslowerthanthatoftheaqueoussolution,andthehalf-lifewaslongerthanthatofthewatersolution.Theresultsfromtheexperimentshowedthatbyintraveno
