助剂对小鼠吸收黄连总生物碱的影响及药代动力学的研究

Effect of additives on absorption of Coptis chinensis total alkaloids and pharmacokinetics in mice

目的:筛选促进小鼠吸收黄连总生物碱的助剂,研究黄连总生物碱的药代学。方法:黄连总生物碱与助剂按1∶1配成制剂,灌胃小鼠后收集小鼠粪便和灌胃后眼眶采血,HPLC测定粪便和血液中总生物碱含量。结果:明胶使药根碱、黄连碱、小檗碱和总生物碱的吸收均提高约30%;聚山梨醇酯和阿拉伯树胶对小檗碱的吸收无影响,而抑制其他3种生物碱和总碱的吸收;卵磷脂几乎不影响各生物碱的吸收。总生物碱在血液中的达峰时间分别为2 h(Cmax1=5.9 mg.L-1)和5.0 h(Cmax2=3.4 mg.L-1),AUC为17.6 mg.h.L-1,消除半衰期t1/2为5.2 h;添加明胶后,总生物碱的达峰时间分别为1.5 h(Cmax1=7.6 mg.L-1)和4.8 h(Cmax2=8.5 mg.L-1),AUC增大为31.1 mg.h.L-1,消除半衰期t1/2为6.2 h。结论:明胶可以加快小鼠对黄连总生物碱的吸收,延长消除半衰期,增加血药浓度和生物利用度。

Objective:To evaluate the effect of additives on absorption of Coptis chinensis total alkaloid and their pharmacokinetics in mice.Method:The mice were fed with the mixture of C.chinensis total alkaloids and additives(1:1).And then the feces and orbital blood were taken to detect the content of total alkaloids by HPLC and their pharmacokinetics.Result:Glutin could make the absorption of jatrorrhizine,coptisine,berberine and total alkaloids increased by 30%.Tween 80 and arabic gum did not affect the absorptio...