用LC-MS/MS法测定大鼠血浆中大蒜皂苷PIEB的浓度及其体内药动学研究
投稿时间:2018-10-06  修订日期:2018-11-12  点此下载全文
引用本文:陈浩,李新方,孙渺,张钢,杨峰.用LC-MS/MS法测定大鼠血浆中大蒜皂苷PIEB的浓度及其体内药动学研究[J].药学实践杂志,2019,37(1):37~41
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作者单位E-mail
陈浩 解放军总医院海南分院药剂科, 海南 三亚 572013  
李新方 海军军医大学药学院, 上海 200433  
孙渺 海军军医大学药学院, 上海 200433  
张钢 陆军军医大学高原军事医学系高原医学教育部重点实验室, 重庆 400038  
杨峰 海军军医大学药学院, 上海 200433 yangfeng1008@126.com 
基金项目:全军后勤科研计划重大项目(AWS14L005)
中文摘要:目的 采用高效液相色谱-质谱(LC-MS/MS)法测定大鼠血浆中大蒜皂苷提取物中大蒜皂苷Proto-iso-eruboside-B(PIEB)的浓度,并研究其药动学特点。方法 采用Athena C18-WP色谱柱(50 mm×2.1 mm,3 μm),流动相为乙腈-水(含0.05%甲酸)体系,梯度洗脱,流速0.3 ml/min。大鼠分别给予低、中、高剂量大蒜皂苷总提取物灌胃及静脉注射单一剂量大蒜皂苷总提取物,给药后在不同的时间点眼眶取血,采用LC-MS/MS法测定血药浓度;采用InnaPhase Kinetica2000TM软件计算相关药动学参数。结果 大蒜皂苷提取物中的PIEB成分在10~2 430 ng/ml范围内具有良好的线性关系(r=0.999 1);方法学考察均符合要求;大鼠静脉给药大蒜皂苷总提取物(50 mg/kg)后,PIEB即刻在体内达到最大血药浓度,其t1/2为322 min左右,平均驻留时间(MRT)为270 min;口服灌胃低、中、高浓度大蒜皂苷总提取物后,PIEB的AUC、cmax等随给药剂量的增加而增大,大蒜皂苷提取物中的PIEB成分在大鼠体内的药动学过程符合线性药动学特征。结论 本方法操作简便、结果准确、重复性好,适用于测定大鼠血浆中大蒜皂苷PIEB的浓度。
中文关键词:大蒜皂苷PIEB  高效液相色谱-质谱  药动学  含量测定
 
Study on determination and pharmacokinetics of garlic saponins PIEB in the rat plasma by LC-MS/MS
Abstract:Objective To establish a method for concentration determination of garlic saponins PIEB in the rat plasma and study the pharmacokinetics of PIEB.Methods The separation was performed on a reverse phase Athena C18-WP (50 mm×2.1 mm, 3 μm), with the mobile phase consisted of elution of acetonitrile-water (contain 0.05% formic acid) at a flow rate of 0.3 ml/min.After intravenous and gavage administration, the blood samples of rats were collected in different time, and measured by LC-MS/MS.The pharmacokinetics parameters were calculated by Inna Phase Kinetica2000TM pharmacokinetics software.Results There was a good linearity of the calibration curves over the concentration range of 10-2 430 ng/ml (r=0.999 1), and the investigation of methodology all accorded with the demands.After intravenous administration of 50 mg/kg PIEB in rats, the maximum concentration of PIEB was achieved immediately.The t1/2 of PIEB was about 322 minutes and the MRT was 270 minutes.After oral administration of low, medium and high concentrations of garlic saponin, the AUC and cmax increased with the increasing of dosage, which were consistent with the features of linear pharmacokinetics.Conclusion The established method was simple, accurate and sensitive, which could be suitable for the contents determination of garlic saponins PIEB in the rat plasma.
keywords:garlic saponins PIEB  LC-MS/MS  pharmacokinetics  content determination
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