治郁颗粒活性成分大鼠体内分布的研究

Active ingredient of Zhiyu Particles distribution in rats

目的观察采用经典强迫游泳试验确定治郁颗粒的最佳给药剂量及高效液相色谱法,以芍药苷的含量为内标物,研究治郁颗粒活性成分栀子苷在大鼠体内各组织脏器中的分布。方法以4种剂量小鼠灌胃给予治郁颗粒混悬液,以4 min内累计不动时间为考察指标,确定药物的最佳给药剂量。治郁颗粒混悬液0.02 g/mL灌胃给予大鼠,给药剂量为0.10 mL/kg体质量,连续给药4 d。结果确定药物的浓度为0.02 g/mL为最佳给药浓度,即小鼠剂量为0.2 g/kg体质量,换算成人的服用量为每日4.4 g/60 kg。大鼠末次给药45min后,各组织及血液中均检出栀子苷,各脏器中栀子苷含量大小顺序为肝>肾>肺>脾>血>心>脑,其中脑组织栀子苷含量为(1.223±0.277)μg/g。结论该方法稳定、可行,方中活性成分栀子苷能通过血脑屏障,为治郁颗粒的抗抑郁机制提供了理论依据。

Objective Using the forced swimming test to determine the optimum dosage of Zhiyu Particles, using high per- formance liquid chromatography, with paeoniflorin as internal standard, to study the jasminoidin distribution in rats, that was active ingredient of Zhiyu particles. Methods With 4 different dosages mice were orally administered Zhiyu Particles, sus- pension, 4 rain motionless time as the indexes, determine the best concentration. With 0.02 g＂ mL Zhiyu Particles, suspen- sion, administered at a dose of 0.10 mL-kg bw, was best, the mice at a dose of 0.2 g· kg bw, dose conversion of 4.4 g/60 （ kg· d） for continuous administration for 4 Days. Results The drug concentration of 0.02 g· mL adult. 45 min after the last administration, the organization of jasminoidin was detected, the order is kidney 〉 kidney 〉 lungs 〉 spleen 〉 blood 〉 heart 〉 brain, the content of jasminoidin in brain tissue was （ 1. 223 ±0. 277） μg/g, to prove the active ingredients in the prescrip- tion can pass the blood-brain barrier. Conclusion the result provides a theoretical basis for antidepressant mechanism of Zhiyu Particles.