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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 screen auxiliaries that promote the absorption of total alkaloids from Coptis chinensis in mice and study the pharmacokinetics of total alkaloids in Coptis chinensis. Methods: The total alkaloids and adjuvants of Rhizoma Coptidis were administrated into 1:1 preparations. Mice were collected after gavage and blood was collected from the eyelids after intragastric administration. The contents of total alkaloids in feces and blood were determined by HPLC. Results: Gelatin increased the absorption of jatrorrhizine, coptisine, berberine and total alkaloids by approximately 30%; polysorbate and gum arabic had no effect on the absorption of berberine, while inhibiting the other three alkaloids and Total alkali absorption; Lecithin hardly affects the absorption of alkaloids. The peak time for the total alkaloids in the blood was 2 h (Cmax1=5.9 mg.L-1) and 5.0 h (Cmax2=3.4 mg.L-1), and the AUC was 17.6 mg.hL-1. The elimination half-life t1 /2 was 5.2 h; after adding gelatin, the peak time of total alkaloids was 1.5 h (Cmax1=7.6 mg.L-1) and 4.8 h (Cmax2=8.5 mg.L-1), respectively, and the AUC increased to 31.1. mg.hL-1, elimination half-life t1/2 is 6.2 h. Conclusion: Gelatin can accelerate the absorption of total alkaloids in Coptis chinensis, prolong the elimination of half-life, increase blood concentration and bioavailability.