中国中药杂志

2014, v.39(02) 309-315

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玳玳黄酮提取物特征活性成分不同生理状态的药动学特性比较
Studies on pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in different physiological status

曾令军;陈丹;郑利;连赟芳;蔡韦炜;黄群;林伊莉;
ZENG Ling-jun;CHEN Dan;ZHENG Li;LIAN Yun-fang;CAI Wei-wei;HUANG Qun;LIN Yi-li;Department of Pharmacy,Fujian University of Traditional Chinese Medicine;

摘要(Abstract):

为探索玳玳黄酮提取物临床降血脂药效特性,该文研究比较了玳玳黄酮提取物特征活性成分在正常大鼠及高脂血症模型大鼠体内药动学特性。实验采用UPLC-MS建立血浆中玳玳黄酮提取物特征活性成分柚皮苷和新橙皮苷定量测定法,通过建立高脂血症大鼠模型,比较正常大鼠和高脂血症模型大鼠灌胃玳玳黄酮提取物后血浆中柚皮苷和新橙皮苷的药动学差异。实验结果表明,玳玳黄酮提取物中特征活性成分柚皮苷和新橙皮苷在不同生理状态下的药动学特性存在显著性差异,高脂血症模型大鼠口服玳玳黄酮提取物后柚皮苷和新橙皮苷最大血药浓度C max与正常大鼠相比均明显增大,半衰期t1/2和体内滞留时间MRT缩短,但AUC0-24 h变小,达峰时间t max无差异;进一步证实玳玳黄酮提取物在高脂血症病理状态下能更好的发挥降血脂活性,其中特征活性成分柚皮苷和新橙皮苷是玳玳黄酮提取物发挥生物活性的物质基础。
In order to explore the clinical hypolipidemic features of Daidai flavone extract,the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats were studied and compared. The study established the quantitative determination method of naringin and neohesperidin in plasma by UPLC-MS. Study compared the pharmacokinetics differences of naringin and noehesperidin in normal and hyperlipemia rats on the basis of establishment of hyperlipemia model. Results indicated that the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats showed significant differences. The C max of naringin and neohesperidin in hyperlipemia rats plasma after oral administration of Daidai flavone extract increased obviously,while t 1 /2,MRT and AUC 0-24 h decreased,compared to normal rats. But t max showed no differences to that of normal rats. The results further proved Daidai flavone extract would have better hypolipidemic effect in the hyperlipemia pathological status. And the characteristic active ingredients naringin and noehesperidin were the material base of Daidai flavone extract to express the hypolipidemic effect.

关键词(KeyWords): 玳玳黄酮提取物;UPLC-MS;高脂血症;药动学
Daidai flavone extract;UPLC-MS;hyperlipidaemia;pharmacokinetics

Abstract:

Keywords:

基金项目(Foundation): 福建省自然科学基金项目(2012J01386);; 福建省科技计划项目(2010Y2004);; 福建省发展和改革委员会产业技术开发项目(闽发改高技[2011]1598号)

作者(Author): 曾令军;陈丹;郑利;连赟芳;蔡韦炜;黄群;林伊莉;
ZENG Ling-jun;CHEN Dan;ZHENG Li;LIAN Yun-fang;CAI Wei-wei;HUANG Qun;LIN Yi-li;Department of Pharmacy,Fujian University of Traditional Chinese Medicine;

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