淫羊藿总黄酮在骨质疏松大鼠体内的药动学行为  

Pharmacokinetic behaviors of total flavonoids from Epimedii Folium in osteoporotic rats in vivo

作　　者：刘聪燕[1] 高霞[1] 陈彦[1] 黄萌萌[1] 瞿鼎[1] 

机构地区：[1]南京中医药大学附属中西医结合医院江苏省中医药研究院中药组分与微生态研究中心,江苏南京210028

出　　处：《中成药》2017年第8期1595-1600,共6页Chinese Traditional Patent Medicine

基　　金：国家自然科学基金(81173557)

摘　　要：目的研究淫羊藿Epimedii Folium总黄酮在骨质疏松大鼠体内的药动学行为。方法 12只大鼠分为模型组和假手术组,双侧卵巢摘除法复制骨质疏松大鼠模型。灌胃总黄酮(500 mg/kg)后,HPLC-DAD法测定13个时间点(0.083、0.25、0.5、0.75、1、2、3、4、6、8、12、24、48 h)总黄酮原型苷(朝藿定A、朝藿定B、朝藿定C、淫羊藿苷)及其代谢产物(箭藿苷A、箭藿苷B、2″-O-鼠李糖基淫羊藿次苷Ⅱ、宝藿苷Ⅰ、淫羊藿苷元)的血药浓度,绘制药-时曲线,计算药动学参数。结果总黄酮原型苷及其代谢产物在2组大鼠体内的药-时曲线均呈双峰。与假手术组相比,模型组的整合AUC和Cmax均显著降低(P<0.01),t1/2显著延长(P<0.01)。结论在大鼠骨质疏松状态下,淫羊藿总黄酮的体内吸收和代谢显著变慢,从而影响其药效发挥。AIM To investigate the pharmacokinetic behaviors of total flavonoids from Epimedii Folium in osteoporotic rats in vivo. METHODS Twelve rats were divided into model group and sham group,after which the osteoporotic rat model was established by removing bilateral ovaries. After intragastric administration with total flavonoids（ 500 mg/kg）,HPLC-DAD was applied to detecting the plasma concentrations of total flavonoids＇ prototype glycosides（ epimedin A,epimedin B,epimedin C,icariin） and their metabolites（ sagittatoside A,sagittatoside B,2″-O-rhamnosylicariside Ⅱ,baohuoside I,icaritin） at thirteen time points（ 0. 083,0. 25,0. 5,0. 75,1,2,3,4,6,8,12,24 and 48 h）,then the plasma concentration-time curves were drawn,followed by the calculation of pharmacokinetic parameters. RESULTS Doubled peaks were observed in the plasma concentration-time curves of total flavonoids＇ prototype glycosides and their metabolites in both groups. Compared with the sham group,the integrated AUC and Cmaxin the model group were significantly decreased（ P〈0. 01）,as well as the prolonged t1/2（ P〈0. 01）. CONCLUSION The in vivo absorption and metabolism of total flavonoids from Epimedii Folium are much slower in the state of osteoporosis,thus affects the efficacy.

关 键 词：淫羊藿 总黄酮 药动学行为 骨质疏松大鼠 

分 类 号：R969.1[医药卫生—药理学]