目的考察丹参酮ⅡA静脉乳剂在小鼠体内的药动学和组织分布特征。方法血浆和组织匀浆液经沉淀蛋白,以乙腈-0.01mol·L^-1枸橼酸水溶液(78:22)为流动相,经Diamonsil^TM C₁₈(4.6mm×150mm,5μm)分离,检测波长为270nm,吉非罗奇为内标,进行色谱分析。结果小鼠iv丹参酮ⅡA静脉乳剂20mg·kg^-1后,药-时曲线符合二室模型,其主要药动学参数为:t_1/2β2.48h,V_d16.23L·kg^-1,CL 4.54L·h^-1·kg^-1,AUC_0-∞ 4.404mg·h·L^-1。组织分布结果表明,在15min时,肺脏浓度最高,其次是脑、心脏、脾脏,肝脏和肾脏最低,随后浓度下降迅速,在1.5～4.0h内长期保持低浓度。结论丹参酮ⅡA静脉乳剂体内分布迅速,组织分布广泛,肺中浓度最高,且能通过血脑屏障,与丹参酮ⅡA磺酸钠在体内的组织分布有差异。

OBJECTIVE To investigate the pharmacokinetics and tissue distribution of TSⅡA emulsion.METHODS After the plasma protein and tissue homogenate were precipitated,the analysis was conducted on a DiamonsilTM C18(4.6 mm×150 mm,5 μm)column with mobile phase consisting of acetonitrile-0.01 mol·L^-1 Citric Acid solution(78∶22).Gemfibrozil was internal standard.The detective wavelength was 270 nm.RESULTS The concentration-time curve of TSⅡA emulsion was discribed by a two-compartment model.The main pharmacokinetic parameters were as follows:t_1/2β 2.48 h,V_d 16.23 L·kg^-1,CL 4.54 L·h^-1·kg^-1,AUC_0-∞ 4.404 mg·h·L^-1.In tissue distribution,the TS ⅡA concentration in the lung was the highest and those in the brain,heart,spleen,liver and kidney was lower sequentially.Then concentration descended rapidly,remaining at low level from 1.5 h to 4 h.CONCLUSION TSⅡA emulsion belongs to a short-half-life drug,distributed quickly and extensively.It has the ability to permeate blood brain barrier.It is different from TSⅡA sulfonic acid sodium in the tissue distribution.