胡黄连苷Ⅰ和胡黄连苷Ⅱ在大鼠体内的药物动力学  

Pharmacokinetics of picroside Ⅰ and picroside Ⅱ in rats

作　　者：张卫平[1] 孙小成[2] 王静 王浩[2] 王金辉[1] 

机构地区：[1]沈阳药科大学中药学院,辽宁沈阳110016 [2]吉林大学药物代谢研究中心,吉林长春130012

出　　处：《沈阳药科大学学报》2013年第9期724-728,748,共6页Journal of Shenyang Pharmaceutical University

基　　金：国家科技支撑计划基金资助项目(2012BAI30B02)

摘　　要：目的研究胡黄连苷Ⅰ和胡黄连苷Ⅱ在大鼠体内的药物动力学特征及胡黄连苷Ⅱ的绝对生物利用度。方法采用大鼠尾静脉注射和灌胃给药两种方式,利用LC-MS/MS法同时测定大鼠血浆中胡黄连苷Ⅰ和胡黄连苷Ⅱ的质量浓度,进行房室模型拟合并计算其主要药物动力学参数。结果大鼠尾静脉注射给予胡黄连总苷32mg·kg-1后,胡黄连苷Ⅰ和苷Ⅱ的t1/2β分别为(0.70±0.03)h和(0.63±0.25)h,AUC0t-为(1 379.74±122.82)μg·h·L-1和(16 221.01±562.50)μg·h·L-1。灌胃给予等量总苷后,胡黄连苷Ⅱ的绝对生物利用度仅为0.99%。结论胡黄连苷Ⅰ和苷Ⅱ在大鼠体内消除迅速,两者的药物动力学过程均符合二室模型。Objective To study the pharmacokinetic properties of picroside Ⅰand picroside Ⅱ after intrave- nous administration of total glycoside of Picrorhiza scrophulariiflora Pennell in Wistar rats, and to study the absolute bioavailability of picroside Ⅱ. Methods Wistar rats were given 32 mg. kg-1of total glycoside of Picrorhiza scrophulariiflora Pennell by oral and intravenous means respectively, the concentrations of picro- side Ⅰ and picroside 11 were determined simultaneously by LC-MS/MS method in rat plasma. Main phar- macokinetic parameters were estimated after compartmental fitted using the DAS 3.0 software. Results After intravenous administration of 32 mg. kg- 1 total glycoside of Picrorhiza scrophulariiflora Pennell to 6 rats, the main pharmacokinetic parameters were as follows： tl/2B （ O. 70 ± 0. 03 ） h and （ 0. 63 ± 0. 25 ） h, AUC0., （ 1 379. 74 ± 122.82） μg·h·L-1 and （ 16 221.01 ± 562.50 ） μg·h·L-1 After oral administration of the same dosage,the absolute bioavailability of picroside Ⅱ was only 0. 99% ,the concentration of picroside Ⅰ was under the LLOQ. Conclusions Picroside Ⅰ and picrosideⅡ are eliminated rapidly in rats. The concen- tration-time curves of picroside Ⅰand picroside Ⅱ are confirmed to be two-compartment open models.

关 键 词：胡黄连苷Ⅰ 胡黄连苷Ⅱ LC—MS MS 药物动力学 生物利用度 

分 类 号：R97[医药卫生—药品] R917[医药卫生—药学]