目的建立大鼠血浆中丹参酮ⅡA和隐丹参酮的HPLC-UV检测法,并研究丹参脂溶性成分在大鼠体内的药动学?方法以吉非罗齐为内标,血浆样品经简单的甲醇沉淀蛋白后,上清液直接进样测定?大鼠尾iv丹参醇提取物(以丹参酮ⅡA计为5 m g/只),测定各时点丹参酮ⅡA和隐丹参酮的血药浓度,绘制药-时曲线,采用3p87计算药动学参数?结果大鼠尾iv丹参醇提取物后,丹参酮ⅡA的主要药动学参数分别为:t1/2α为(0.088±0.024)h,t1/2β为(2.1±0.7)h;VC为(0.8±0.6)L;CL为(2.0±1.1)L/h-1;AUC0-4和AUC0-∞分别为(2.2±0.9)m g.h/L和(3.4±1.7)m g.h/L?结论丹参醇提取物iv给药后,丹参酮ⅡA的药-时曲线符合二室模型,血浆中丹参酮ⅡA迅速下降,表观分布容积大;隐丹参酮在血浆中消除快,药动学参数不易获得?

Objective To study the stability of ligustillde and the inclusion process in β-cyclodextrin to avoid its isomerization,Methods The content of ligustilide dropped severely even if it was kept away from layer and air under room temperature.The inclusion process with peyelodextrin was carried out on orthogonal design.The optimum conditions were determined and inclusion complex was made sure by many ways.Results The validated trials by DCS,IR,and GC could exhibit the obvious difference between mixture and inclusion complex which showed the form of a new phase,because of β-cyelodextrin and drugs in the molecular capsules.Conclusion Inclusion process with β-cyclodextrin Call improve stability of ligustilide that is unstable in normal situation.