目的 建立大鼠血浆中人参皂苷Rb1的LC-MS/MS定量分析方法, 分别考察单次静脉注射和口服给药后, 人参皂苷Rb1在大鼠体内的药动学特征。方法 大鼠灌胃和静脉注射后, 不同时间点眼底静脉丛取血, 建立LC-MS/MS分析方法测定大鼠体内Rb1含量, 运用PKSolver V2.0软件计算药动学参数。结果 Rb1在口服灌胃组大鼠体内的主要药动学参数ρmax、tmax、t1/2、AUC0~96 h分别为(2.01±0.93) μg·mL-1, (7.20±5.49) h, (25.91±15.84) h, (88.47±58.99) μg·h·mL-1。Rb1在静脉注射组大鼠体内的主要药动学参数ρmax、t1/2α、t1/2β、AUC0~96 h分别为(194.81±28.84) μg·mL-1, (0.18±0.05) h、(14.66±4.19) h、(1 671.16±388.91)μg·h·mL-1。结论 Rb1绝对生物利用度为0.62%, 说明Rb1口服给药吸收比较差, 而静脉注射因药物直接进入血管, 推荐临床给药优先选择。
Abstract
OBJECTIVE To develop a highly snsitive and specific LC-MS/MS method to explore the pharmacokinetic propeties of ginsenoside Rb1. METHODS Ginsenoside Rb1 dissolved in normal saline was administered in a dose of 100 mg·kg-1 via gastric in fusion and 10 mg·kg-1 by intravenous injection in rats.Plasma was collected from fundus oculi venous plexus and ginsenoside Rb1 was analyzed by a validated LC-MS/MS method in plasma after intravenous and oral administration. The pharmacokinetic parameters were evaluated by software PKSolver V2.0. RESULTS The main pharmacokinetic parameters of ginsenoside Rb1 after oral administration of 100 mg·kg-1 dosage were as follows: ρmax(2.01±0.93) μg·mL-1, tmax(7.20±5.49) h, t1/2(25.91±15.84) h, AUC0~96 h(88.47±58.99) μg·h·mL-1. The main pharmacokinetic parameters of ginsenoside Rb1 after intravenous administration of 10 mg·kg-1 dosage were as follows: ρmax(194.81±28.84) μg·mL-1, t1/2α(0.18±0.05) h, t1/2β(14.66±4.19) h, AUC0~96 h(1 671.16±388.91) μg·h·mL-1. CONCLUSION The ginsenoside Rb1 of orally administered was 0.62%, shows poor absolute bioavailability, and intravenous injection directly distribute into the blood vessels, can be the priority.
关键词
人参皂苷Rb1 /
药动学 /
LC-MS/MS
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Key words
ginsenoside Rb1 /
pharmacokinetics /
LC-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
科技部十二五重大新药创制专项(2011ZX09302-007-02);上海市自然科学基金资助项目(10ZR1423600);中国博士后科学基金特别资助(200902245)
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