具栖冬青苷在大鼠体内的药动学  

Pharmacokinetics of pedunculosid in rat

作　　者：赵文珠 居文政[2,3] 臧雨馨 孙冰婷 谈恒山[4] 

机构地区：[1]南京市江宁区中医医院药剂科,江苏南京211100 [2]南京中医药大学药学院,江苏南京210029 [3]南京中医药大学附属医院临床药理科,江苏南京210029 [4]南京军区总医院,江苏南京210002

出　　处：《中国新药与临床杂志》2016年第1期46-49,共4页Chinese Journal of New Drugs and Clinical Remedies

基　　金：江苏省中医药领军人才项目(LJ200906);江苏高校优势学科建设工程资助项目2010;中药新药临床评价研究技术平台(南京)建设(2012ZX09303009-002)重大新药创制

摘　　要：目的建立测定大鼠血浆中具栖冬青苷浓度的液相质谱联用(LC-MS)法。方法雄性SD大鼠8只,尾静脉注射具栖冬青苷2.86 mg·只^(-1),于指定时间眼眶采血,并用LC-MS法测定血浆中具栖冬青苷的浓度。色谱柱为ZORBAX SB-C_(18)柱(2.1 mm×150 mm,5μm),以乙腈和0.1%甲酸+2 mmol·L^(-1)醋酸铵水溶液(80∶20,V/V)为流动相。离子化方式为电喷雾(ESI),负离子方式检测,具栖冬青苷[M-H]^+,m/z 649.6,替硝唑[M-H]^+,m/z 248.1。采用DAS 2.0软件对其药动学参数进行统计分析。结果具栖冬青苷在大鼠体内呈二室模型分布,主要药动学参数:tβ为(5.20±0.14)h,CL为(51.07±0.22)L·h^(-1)·kg^(-1),ρmax为(22.68±0.72)μg·L^(-1),V_d为(2 355.69±1.68)L·kg^(-1)。结论该方法灵敏度较高,可用于具栖冬青苷在大鼠血浆中的检测及药动学分析。AIM To establish a liquid chromatography- mass spectrometric （LC- MS） method for determination of pedunculosid concentration rat plasma. METHODS Eight male SD rats were injected with pedunculosid 2.86 mg per rat through the tail vein. Plasma samples were collected from orbit at a specified time. And to determine the plasma concentration of pedunculosid in rat by LC-MS. The column was ZORBAX SB-C18 （2.1 mm ×150 mm, 5 μm）. The mobile phase was acetonitrile and the solution of 0.1% formic acid and 2 mmol·L^-1 ammonium acetate （80 ： 20, V/V）. The ionization mode was electrospray, and the mode of detection was negative, pedunculosid [M-H]^＋, m/z 649.6, tinidazole [M-H]^＋, m/z 248.1. DSA 2.0 software was used for statistical analysis of its pharmacokinetic parameters. RESULTS Pedunculosid was two-compartment model in rat, and the main pharmacokinetic parameters： t1/2β was （5.20 ±0.14） h, CL was （51.07 ±0.22） L·h^-1·kg^-1, ρmax was （22.68 ± 0.72） μg·L^-1 and Va was （2 355.69 ±1.68） L·kg^-1. CONCLUSION The method has high sensitivity and it can be used to detect the concentration of pedunculosid in rat plasma and analyze its pharmacokinetic parameters.

关 键 词：具栖冬青苷 色谱法 液相 药动学 

分 类 号：R969.1[医药卫生—药理学]