| 黄连生物碱中小檗碱在大鼠脑核团中的药代动力学研究 |
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| 引用本文： | 王明玮,王雪莉,邢东明,雷帆,杜力军.黄连生物碱中小檗碱在大鼠脑核团中的药代动力学研究[J].世界科学技术,2009,11(3):361-364. |
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| 作者姓名： | 王明玮 王雪莉 邢东明 雷帆 杜力军 |
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| 作者单位： | 王明玮(新疆军区西安第二干休所医务室,西安,710100);王雪莉,邢东明,雷帆,杜力军(清华大学生物科学与技术系药物药理研究室,北京,100084) |
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| 基金项目： | 国家自然科学基金资助项目(90713043):用数学模型对石榴叶总鞣质及其主要活性成分对脂肪细胞作用的综合评价;负责人:杜力军，国家自然科学基金资助项目(30801523):石榴叶总酚成分对脑缺血过程中PPARγ转录活性的影响及其脑保护作用研究;负责人:雷帆 |
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| 摘 要： | 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。
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| 关 键 词： | 小檗碱 脑核团 HPLC |
Pharmacokinetics of Berberine in Rat Cerebral Nuclei Following Intravenous Administration of Coptidis Rhizoma Extract |
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| Institution: | Wang Mingwei, Wang Xueli, Xing Dongming, Lei Fan, Du Lijun (1.Medical Service, Xi ＇an Second Sanatorium, Xi＇an 710100, China;2. Laboratory of Pharmaceutical Sciences, Department of Biological Sciences and Biotechnology, Tsinghua University, Beijing 100084, China) |
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| Abstract: | 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. |
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| Keywords: | HPLC |
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