目的:研究大鼠静脉注射黄连生物碱提取物后,小檗碱在大鼠脑核团中的药代动力学特性。方法:HPLC法测定大鼠脑核团中小檗碱的浓度。结果:小檗碱在血浆中消除很快,t1/2β为1.13h;在脑核团中消除却很缓慢,t1/2/β为11~15h;在脑核团中分布较快,为2.5~4h达峰,且消除缓慢,在体内滞留时间较长。统计矩参数表明,体内平均滞留时间为19~22h。结论:小檗碱可以在这些脑核团蓄积。因此,仅靠血浆药代动力学来指导小檗碱的临床用药是远远不够的,尤其是治疗脑部疾病。本研究不仅可以阐明小檗碱脑部代谢规律,为定位其脑部药效靶点打下基础,也为其理论研究作了有益探索。
The study investigates the pharmacokinetic activities of berberine in rat cerebral nuclei that were intravenously administered with Coptidis Rhizoma extracts. In the study, HPLC was employed to determine the concentration of berberine in rat cerebral nuclei. Test results show that berberine stayed longer (t1/2β for 11-15 h) in cerebral nuclei than in plasma (t1/2β for 1.13 h). It reached the peak in cerebral nuclei at 2.5-4h and was eliminated slowly. It has also a relatively long residue time in the body. It is believed that berberine tends to accumulate in cerebral nuclei. In this context, plasma pharmacokinetics shall not be a sole criterion for clinical applications of berberine, especially in treating brain diseases. The finding, depicting the metabolic activities of berberine in brain, creates a fine ground for screening desired targets for the drug in brain, and for the future theoretical study in the area as well.