马鞭草提取物在大鼠体内的组织分布及排泄研究

Study on tissue distributions and excretion of Verbena officinalis extract in rats

目的：建立马鞭草提取物中马鞭草苷、戟叶马鞭草苷在大鼠11种主要组织器官及尿液中的反相高效液相色谱（RPHPLC）分析方法,研究其在体内组织分布的规律特点及原形药物体内排泄情况。方法：50只SD大鼠随机分为5组,尾静脉注射给予8g生药/kg马鞭草提取物后,分别于5,15,30,60,120 min腹主动脉放血处死,时间点的选择包括药物的吸收相、分布相和消除相,迅速取出脑、心、肝、脾、肺、肾、胃、骨骼肌、小肠、生殖器（卵巢、子宫）、脂肪组织;另12只SD大鼠随机分为两组,尾静脉注射给予4g生药/kg马鞭草提取物后,收集给药前及给药后0~2 h、2~6 h、6~12 h、12~24h各尿液,RP-HPLC法测定各组织及尿液中马鞭草苷、戟叶马鞭草苷的浓度。结果：马鞭草苷和戟叶马鞭草苷在各组织的5个时间点上均有不同程度的药物浓度被检出,其中肾脏分布最高,其次为肺、生殖腺和肝脏。马鞭草苷和戟叶马鞭草苷以原形药物的形式经肾排泄,12 h马鞭草苷与戟叶马鞭草苷尿中原形药物累积排泄量分别占给药量的22.7%、32.6%。结论：马鞭草苷和戟叶马鞭草苷在大鼠体内分布快速而广泛,部分以原形药物的形式经尿排泄。

Objective： To establish an RP-HPLC method for the determination of 11 tissues and urine concentration of verbenalin and hastatoside in Verbena officinalis extract. The tissue distribution and excretion characteristics of verbenalin and hastatoside in rats were discussed. Methods： 25 SD rats were randomly divided into 5 groups,various tissues were obtained at 5,15,30,60,120 min after a single intravenous administration of 8g crude drug / kg V. officinalis extract; Other 6 SD rats,urine samples of different time periods were collected after a single intravenous administration of 4g crude drug / kg V. officinalis extract. The concentration of verbenalin and hastatoside in samples were subsequently determined by RP-HPLC. Results： Verbenalin and hastatoside were widely distributed in various tissues of rats. The distribution sequence of different tissues ranking from high to low was kidney,lung and reproductive organs. Verbenalin and hastatoside were excreted via the kidney as parent drug. After a 12 h,the accumulative excretion percentage of the parent drug of verbenalin and hastatoside in urine amounted to22. 7 %,32. 6 % respectively. Conclusion： Verbenalin and hastatoside were quickly distributed in all the tissues,part of parent drug were excreted via urine.