黄芩苷磷脂复合物在动物体内的组织分布和抗肝损伤活性

Effect of Baicalin Phospholipids Complexion on Tissue Distribution and Antihepatitis Activity

目的研究黄芩苷磷脂复合物在大鼠体内的组织分布和在小鼠体内的抗肝损伤活性。方法建立一种新的HPLC方法,以黄芩苷及其与磷脂的物理混合物为对照,测定黄芩苷磷脂复合物在灌胃给药后不同时间在大鼠的心、肝、脾、肺、肾、胃、肠、脂肪、脑及血浆中的药物含量;采用四氯化碳致小鼠急性肝损伤的病理模型,设置黄芩苷和物理混合物两个给药对照组,考察黄芩苷磷脂复合物高、中、低3个剂量对小鼠血清中谷丙转氨酶(GPT)和谷草转氨酶(GOT)活性的影响。结果黄芩苷磷脂复合物在大鼠体内的分布特性与黄芩苷类似,在各脏器组织中均有分布,但在胃、肾脏和血浆中的分布相对较多;抗肝损伤活性实验结果表明,黄芩苷磷脂复合物随剂量增加其抑制酶活性的作用增强,复合物的低剂量对GPT的活性具有显著性降低作用,中、高剂量则有非常显著的降低作用。结论黄芩苷磷脂复合物增加了黄芩苷在胃肠中的吸收并增强了药效。

OBJECTIVE To investigate the effect of baicalin complexion with phospholipids on the tissue distribution of rats and antihepatitis activity in mice. METHODS A new HPLC method was established to determine the concentrations of baicalin in tissues and plasma of rat. Antihepatitis activity was evaluated by the effect of baicalin-phospholipid complex on glutamic oxalacetic transaminase （GOT） and glutamic pyryvic transaminase （GPF） in mice. RESULTS The baicalin concentrations in stomach, kidney and plasma after oral intake of the complex were higher than those of the free drug. Significant differences were found between the complex and the free drug in kidney concentration at 12 h, in plasma concentrations at 5 and 8 h. Signifieant differences were also found between the complex anti the physical mixture in plasma concentrations at 8 and 12 h after administration of drugs. The complex resulted in a more significant reduction in glutamic oxalacetic transaminase（GOT） and glutamic pyryvic transaminase （GPT）, while the equivalent dose of baicalin induced only a significant reduction in GPT, and some decrease in these enzymes after oral intake of the physical mixture. The same efficacy was obtained with a half dose of the complex and a full dose of baicalin. CONCLUSION The results suggest that baicalin-phospholipid complex increased the absorption from the stomach and the concentrations in rat rich-blood tissues by improving the amphiphilicity of baicalin. It can be concluded that the complex enhance the absorption of free drug in vivo and exhibited more activity than baicalin.