桔梗石油醚提取物对酒石酸泰乐菌素在小鼠体内的药代动力学及组织分布的影响  

Effect of petroleum ether extract from Platycodon grandiflorum roots on pharmacokinetics and tissue distribution of tylosin tartrate in mice after oral administration

作　　者：陈雯[1] 李英伦[1] 叶刚[1] 施飞[1] 

机构地区：[1]四川农业大学动物医学院,四川雅安625014

出　　处：《湖南农业大学学报（自然科学版）》2015年第2期177-183,共7页Journal of Hunan Agricultural University(Natural Sciences)

基　　金：国家自然科学基金项目(31272599)

摘　　要：以酒石酸泰乐菌素为靶标药物,探究药物中加入桔梗石油醚提取物对小鼠血浆中的药代动力学特征及组织分布的影响。采用高效液相色谱法测定不同时间点小鼠血浆及心脏、肝、肺、肾中酒石酸泰乐菌素的浓度,运用PKsolver程序及SPSS19.0统计软件处理数据,用非房室模型分析药代动力学参数。结果表明:酒石酸泰乐菌素的血–药时曲线呈现多峰;与对照组(药物未加桔梗石油醚提取物)相比,桔梗石油醚提取物组(桔梗组)消除半衰期和达峰时间均变短,达峰浓度降低;药时曲线下面积减少,而表观分布容积增加;平均滞留时间缩短,而药物清除率增大;组织分布图显示,与对照组相比,桔梗石油醚组小鼠心脏中的药物浓度明显比肺、肝、肾中药物浓度高,说明桔梗石油醚提取物改变了酒石酸泰乐菌素在小鼠体内的组织分布。综合分析,桔梗石油醚提取物对酒石酸泰乐菌素在小鼠体内的药代动力学特征有较大影响,表现为加快了药物的吸收速度,但减轻了吸收程度;使药物在体内分布更广泛,却加快了其在体内的消除速度。Tylosin tartrate was used as a target drug in this study to investigate the influence of petroleum ether extract from Platycodon grandiflorum roots on the pharmacokinetics and its distribution character in tissue of mice by oral administration. The concentrations of tylosin tartrate in mice plasma and tissue at different time were determined using high performance liquid chromatography. The pharmacokinetic data was calculated by Pkslover program and analyzed by SPSS19.0 software and non compartment model. The result showed that the curve of time-concentration from tylosin tartrate in blood exhibited multiple peaks, compared with control group, half-life time（t1/2）became shorter, peak concentration and peak time decreased, area under the curve（AUC）and mean residence time（TMR）decreased as well, however, numerical value of apparent volume of distribution（Vz） and clearance（Cl） increased; It was showed that the concentration of the drug in heart was in the highest among tissues. In general, petroleum ether extract from Platycodon grandiflorum roots could significantly influence on the pharmacokinetic parameters of tylosin tartrate in healthy mice, including on speeding up drug absorption, relieving the degree of absorption, diffusing drug in bodies, and accelerating its rate of clearance.

关 键 词：小鼠 桔梗石油醚提取物 酒石酸泰乐菌素 高效液相色谱 药代动力学 组织分布 

分 类 号：S859.79[农业科学—临床兽医学]