京尼平苷在大鼠体内药代动力学性别差异研究  

The influences of gender on pharmacokinetics of geniposide in rats

作　　者：佘丹[1] 苏晓纯[1] 何倩梅[1] 邱昆成 刘奕明[1] 

机构地区：[1]广州中医药大学附属广东省中医院,广州510120

出　　处：《中药药理与临床》2015年第3期50-52,共3页Pharmacology and Clinics of Chinese Materia Medica

基　　金：广东省科技厅资助项目"生物体内毒物代谢动力学实验技术平台"(2011B010500016)

摘　　要：目的:建立大鼠血浆中京尼平苷和京尼平快速液相色谱-串联质谱(LC-MS/MS)检测方法,考察毒性剂量下,性别差异对京尼平苷在大鼠体内的药代动力学特征的影响。方法:将大鼠分为雌雄两组,分别灌胃给与700 mg/kg的京尼平苷水溶液,收集各时间点的大鼠血浆,采用LC-MS/MS法测定血浆京尼平苷和京尼平浓度,通过DAS 2.1.1软件计算主要药代动力学参数。结果:大鼠灌胃京尼平苷后,体内京尼平苷主要的药代动力学参数为:雄性组AUC(0-t)为(17860±6886)μg·h/L,Cmax为(3059±1499)ng/ml,t1/2为(7.4±3.4)h;雌性组AUC(0-t)为(17197±7576)μg·h/L,Cmax为(3904±1062)ng/ml,t1/2为(5.3±2.9)h。结论:灌胃700mg/kg京尼平苷后,京尼平苷药动学特征不具性别差异,而京尼平的药动学特征可能存在性别差异。Objective： To establish a rapid, accurate, and reliable LC-MS/MS method for the simultaneous determination of geniposide and genipin in rat plasma and investigate the influence of gender on pharmacokinetics of geniposide and genipin in rats at a toxic dosage of geniposide. Methods： All rats were assigned to two groups： female group and male group, which were intragastric administration of geniposide at 700 mg/kg body weight by a single dose. The blood samples were collected from the ocular vein into heparinized tubes and pretreated by liquid- liquid extraction. Geniposide and genipin in plasma were determined by LC-MS/MS method, the data fitting and pharmacokinetic parameters calculation were carried out using the DAS 2.1.1 software program. Results： The pharmacokinetic parameters of geniposide in rat plasma af- ter oral administration of geniposide were AUC（0.t） ： （ 17860 ＋ 6886 ） μg · h/L, Cmax： （3058 ＋ 1499） ng/ml, t1/2 ： （7.4 ＋ 3.4） h for the male group and AUC（0-t） ： （ 17197 ＋-7576） μg · h/L, Cmax： （ 3904 ＋ 1062 ） ng/ml, t1/2 ： （5.3 ＋ 2.9） h for the female group, respective- ly. Conclusion： There was no influence of gender on pharmaeokineties of geniposide, where as some ones of genipin were existed in rats on pharmaeokinetics at 700 mg/kg body weight by a single dose.

关 键 词：京尼平苷 性别差异 LC-MS/MS 药代动力学 大鼠 

分 类 号：R285.5[医药卫生—中药学]