黄连共存成分对木兰花碱在大鼠胆汁、尿、粪中排泄的影响  

Influence of coexisting components in Coptidis Rhizoma on excretion of magnoflorine in rat bile, urine, and feces

作　　者：薛宝娟[1,2] 赵雯雯 孙秀蕊 张哲 陈建华 张玉杰 XUE Bao-juan;ZHAO Wen-wen;SUN Xiu-rui;ZHANG Zhe;CHEN Jian-hua;ZHANG Yu-jie(Schoo of Chinese Materia Medica,Bejing University of Chinese Medicine,Bejing 102488,China;Monitoring and Statistical Research Center,National Administration of Traditional Chinese Medicine,Beijing 100027,China)

机构地区：[1]北京中医药大学中药学院,北京102488 [2]国家中医药管理局监测统计中心,北京100027

出　　处：《中国中药杂志》2022年第14期3908-3914,共7页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金面上项目(81673680)。

摘　　要：木兰花碱是黄连中一种重要的阿朴菲型生物碱,前期实验表明,黄连共存成分可明显改变木兰花碱的药代动力学特征,为阐释木兰花碱与黄连共存成分相互作用具体环节,该实验考察了黄连共存成分对木兰花碱在大鼠胆汁、尿液、粪便中排泄的影响。大鼠分别灌胃30 mg·kg^(-1)木兰花碱(ig)、黄连水提液(含30 mg·kg^(-1)木兰花碱)(ig)及静脉注射10 mg·kg^(-1)木兰花碱(iv),观察24 h大鼠胆汁、尿液和粪便木兰花碱的排泄情况。结果显示,大鼠静脉注射木兰花碱24 h胆汁和尿液中木兰花碱排泄率分别为0.90%、37.11%,尿液为静注木兰花碱主要排泄途径。大鼠灌胃给药木兰花碱和黄连水提液后,粪便为木兰花碱主要排泄途径,排泄率分别为8.77%、6.18%。黄连水提液组中大鼠胆汁、尿液和粪便的排泄率分别为木兰花碱单体组的77.78%、79.44%、70.47%。结果表明,大鼠胆汁、尿液和粪便中木兰花碱的累积排泄率整体水平不高,提示木兰花碱在大鼠体内存在显著代谢;黄连共存成分对木兰花碱在胆汁、尿液和粪便排泄均有一定的抑制作用,与黄连水提液中木兰花碱药代动力学中消除速率降低结果一致,此现象说明药物之间存在相互作用。该实验为木兰花碱的新药开发和黄连临床合理应用提供参考依据。Magnoflorine is an important aporphine alkaloid in Coptidis Rhizoma. As reported previously, coexisting components in Coptidis Rhizoma can change the pharmacokinetic characteristics of magnoflorine. To illustrate the interactional links of magnoflorine with its coexisting components in Coptidis Rhizoma, the present study investigated the influence of coexisting components in Coptidis Rhizoma on the excretion of magnoflorine in rat bile, urine, and feces. The rats were dosed with magnoflorine(30 mg·kg) and water decoction of Coptidis Rhizoma(equivalent to 30 mg·kgmagnoflorine) via intragastric administration, and magnoflorine(10 mg·kg) by intravenous administration, respectively, and the excretion of magnoflorine in rat bile, urine, and feces in 24 h was observed. The excretion rates of magnoflorine in bile and urine in 24 h were 0.90% and 37.11% respectively after intravenous administration of magnoflorine, which suggested that urination was the main excretive way of magnoflorine. The excretion rates of magnoflorine in feces were 8.77% and 6.18% respectively after intragastric administration of magnoflorine and water decoction of Coptidis Rhizoma, which indicated that defecation was the main excretion route of magnoflorine. The cumulative excretion rates of magnoflorine in the bile, urine, and feces in the Coptidis Rhizoma water decoction group were 77.78%, 79.44%, and 70.47% of those in the magnoflorine group. The results showed that the cumulative excretion rates of magnoflorine in rat bile, urine, and feces were not high, suggesting that magnoflorine was metabolized significantly in rats. The coexisting components of Coptidis Rhizoma could inhibit the excretion of magnoflorine in rat bile, urine, and feces, which was consistent with the decrease in the elimination rate of magnoflorine in the pharmacokinetics of Coptidis Rhizoma water decoction. It indicated interactions between drugs. This study is expected to provide references for the development of magnoflorine-containing new drugs and rational clinical

关 键 词：黄连 木兰花碱 相互作用 排泄 胆汁 尿液 粪便 

分 类 号：R285.5[医药卫生—中药学]