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目的:测定黄连生物碱在大鼠体内的药代动力学、组织分布,及药根碱、黄连碱、巴马汀、小檗碱4种生物碱在大鼠体内的转化。方法:大鼠分别灌胃黄连总碱、小檗碱,采用反相高效液相色谱法测定大鼠的血浆、组织、胃肠道中黄连4种生物碱的含量。结果:小檗碱在大鼠体内的血药浓度出现2个峰值,达峰时间分别2,5h,其中血药浓度分别为Cmax3.7,2.8mg.L-1;小檗碱在大鼠血液中可以转化为药根碱;给大鼠灌胃黄连总生物碱后,小檗碱在大鼠胃中的浓度单调下降,而黄连碱、巴马汀和药根碱逐渐增加,表明在大鼠的胃中小檗碱可转化为药根碱;小檗碱和巴马汀主要分布在动物的肺部,其次分布在肝脏中,而药根碱和黄连碱主要分布在动物的肝脏中,其次分布在肺部。结论:小檗碱可以转化为药根碱,根据胃肠道推进实验部分解释了小檗碱在血液中出现2次峰值的原因。
OBJECTIVE: To determine the pharmacokinetics and tissue distribution of Coptis alkaloids in rats and the conversion of four alkaloids (jatrorrhizine, berberine, palmatine and berberine) in rats. Methods: The rats were respectively gavaged with berberine and berberine. The contents of four alkaloids of Coptis in plasma, tissue and gastrointestinal tract of rats were determined by RP-HPLC. Results: Berberine plasma concentration in rats showed two peaks, peak time 2,5h, respectively, which plasma concentrations were Cmax3.7,2.8 mg.L-1; berberine in rat blood Can be transformed into jatrorrhizine; berberine concentration in rat stomach decreased monotonously, and berberine, jatrorrhizine and jatrorrhizine increased gradually after intragastric administration of berberine alkaloids in rats, indicating that in rat Berberine in the stomach can be converted to jatrorrhizine; berberine and palmatine are mainly distributed in the lungs of animals, followed by the liver, and jatrorrhizine and jianlian base are mainly distributed in the liver of animals, followed by distribution In the lungs. CONCLUSIONS: Berberine can be converted to jatrorrhizine, and the reason why berberine appears twice in the blood is explained according to the experiment of gastrointestinal propulsion.