大黄黄芩药对配伍在内毒素血症大鼠体内的药动学比较研究  

Effect of Compatibility of Rheum officinale Bailland Scutellaria baicalensis Georgion Pharmacokinetics of Rhein and Baicalin in Endotoxemia Rats

作　　者：张艳[1] 李红[1] 李帆帆[1] 王平[1] 孟宪丽[1] 

机构地区：[1]成都中医药大学药学院,四川成都611137

出　　处：《成都中医药大学学报》2015年第4期19-22,共4页Journal of Chengdu University of Traditional Chinese Medicine

基　　金：国家自然科学基金项目(编号:81274111)

摘　　要：目的:研究大黄、黄芩单用及配伍后水煎液中大黄酸和黄芩苷在内毒素血症大鼠体内的药动学差异。方法:采用尾静脉注射内毒素(LPS)5 mg/kg制备大鼠内毒素血症模型,单次灌胃大黄水煎液(1.54 g/kg)、黄芩水煎液(0.77 g/kg)及大黄-黄芩水煎液(2.31 g/kg)后不同时间点采血,分离血清,高效液相色谱-荧光(HPLC-FLD)法测定大黄酸血药浓度,高相液相色谱-质谱(HPLC-MS)法测定黄芩苷血药浓度,以Kinetica软件计算药动学参数并进行比较分析。结果:黄芩苷在单味药及药对中,吸收均呈现明显双峰现象。与单味药给药组比较,大黄-黄芩配伍应用后,药对中大黄酸、黄芩苷Cmax、AUC均有增加,T1/2和MRT均有所延长。结论:大黄-黄芩配伍后大黄酸与黄芩苷消除减缓,生物利用度均有所增加;配伍可能通过提高有效成分的体内含量及延长其作用时间而达到协同增效的作用。Objective： To investigate the effect of compatibility of Rheum offtcinale BaiU and Scutellaria baicalensis Georgi on pharmacokinetics of rhein and baicalin in endotoxemiarats. Methods： The model rats wereinjected intravenously with lipopolysaccha- ride （LPS, 5mg/kg） . Three groups of rats were orally administeredrespectively with three decoctions including decoction of Rheum of- ficina/e Baill （ 1.54 g/kg）, decoction of Scutellaria baicalensis Georgi （0. 77 g/kg） and blenddecoction ofRheum officinale Baill and Scutellaria baicalensis Georgi （2. 31 g/kg） . The bloods were sampled at different time points to determine the drug concentration of rhein and baicalin in serum by HPLC-FLD and I-IPLC-MS separately. Main pharmacokinetic parameters were calculated by Kinetica 5.0 software. Results： The pharmacokinetic parameters showed that Cmaxand AUC of rhein and baicalin were both obviously increased, Tl/2 and MRT were both obviously prolonged when Rheum offtcinale Baill was combined with Scutellaria baicalensis Georgi. Conclusion： The elimination process of rhein and baicalin were remarkably prolongedand the bioavailability significantlyenhanced after compatibili- ty. The effect of decoction which decocted together was more prominent than which used separately.

关 键 词：大黄 黄芩 大黄酸 黄芩苷 高效液相色谱法 药动学 

分 类 号：R285.5[医药卫生—中药学] R284.1[医药卫生—中医学]