目的 建立SD大鼠血浆中楤木皂苷A的LC-MS/MS分析方法,探讨楤木皂苷A在大鼠体内的药动学特征。方法 分别灌胃、静脉注射楤木皂苷A 50和5 mg·kg-1后,建立LC-MS/MS分析方法测定大鼠血浆中楤木皂苷A含量,运用DAS 3.0软件计算药动学参数。结果 楤木皂苷A在1.0~10 000.0 μg·L-1内线性良好(r>0.994 8),专属性,精密度和准确度,基质效应和提取回收率,以及稳定性均符合要求;SD大鼠灌胃楤木皂苷A 50 mg·kg-1和静脉注射楤木皂苷A 5 mg·kg-1,血浆中的t1/2分别为(8.65±3.22)和(2.00±0.21)h,AUC0-t分别为(277.14±101.00)和(21 194.59±4 385.13)ng·h·L-1,MRT0-t分别为(7.88±0.64)和(1.21±0.11)h,Vd/F分别为(2 229.99±1 013.97)和(0.71±0.20)L·kg-1,CL/F分别为(149.11±62.28)和(0.24±0.05)L·h-1·kg-1,灌胃给药ρmax为(32.68±10.74)μg·L-1,tmax达到(1.21±0.70)h,楤木皂苷A的口服绝对生物利用度约为0.14%。结论 本实验所建立的LC-MS/MS方法特异性强,灵敏度高,可用于楤木皂苷A的药动学研究。
Abstract
OBJECTIVE To develop a highly sensitive and specific LC-MS/MS method to explore the pharmacokinetic properties of araloside A. METHODS Araloside A was administered in a dose of 50 mg·kg-1 via gastric in fusion and 5 mg·kg-1 by intravenous injection in rats.Araloside A was analyzed by a validated LC-MS/MS method in plasma after intravenous and intragastric administration. The pharmacokinetic parameters were evaluated by software DAS 3.0. RESULTS The RESULTS of pharmacokinetic study showed that the linear range of araloside A was good in 1.0-10 000.0 μg·L-1(r>0.994 8). The specificity, precision and accuracy, matrix effect and extraction recovery rate and stability all meet the requirements. The main pharmacokinetic parameters for intragastric administration with araloside A 50 mg·kg-1 and intravenous injection of araloside A 5 mg·kg-1 were as follows:t1/2 was(8.65±3.22) and(2.00±0.21)h, AUC0-t was(277.14±101.00) and (21 194.59±4 385.13)ng·h·L-1, MRT0-t was (7.88±0.64) and (1.21±0.11)h, Vd/F was (2 229.99±1 013.97) and (0.71±0.20)L·kg-1, CL/F was(149.11±62.28) and (0.24±0.05) L·h-1·kg-1, respectively; ρmax was (32.68±10.74) μg·L-1 for intragastric administration and tmax reached(1.21±0.70) h, oral bioavailability of araloside A was about 0.14%. CONCLUSION The LC-MS/MS method established is specific and sensitive, and can be successfully applied in basic pharmacokinetic study of araloside A in rat plasma.
关键词
楤木皂苷A /
药动学 /
液质联用
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Key words
araloside A /
pharmacokinetics /
HPLC-MS/MS
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中图分类号：
R969.1
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参考文献
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脚注
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基金
国家自然科学基金项目资助(81703925);陕西省科技厅科技统筹项目资助(2013KTCQ03-12)
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