Study on determination and pharmacokinetics of garlic saponins PIEB in the rat plasma by LC-MS/MS
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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。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.
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Key words:
- garlic saponins PIEB /
- LC-MS/MS /
- pharmacokinetics /
- content determination
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[1] XIAO J,XING F,LIU Y,et al.Garlic-derived compound S-allylmercaptocysteine inhibits hepatocarcinogenesis through targeting LRP6/Wnt pathway[J].Acta Pharm Sin B, 2018,8(4):575-586. [2] HASSANZADEH H,ALIZADEH M,REZAZAD BARI M. Formulation of garlic oil-in-water nanoemulsion:antimicrobial and physicochemical aspects[J].IET Nanobiotechnol,2018,12(5):647-652. [3] SHABANI E,SAYEMIRI K,MOHAMMADPOUR M.The effect of garlic on lipid profile and glucose parameters in diabetic patients:A systematic review and meta-analysis[J].Prim Care Diabet,2018. [4] KANG J S,KIM S O,KIM G Y,et al.An exploration of the antioxidant effects of garlic saponins in mouse-derived C2C12 myoblasts.[J].Int J Mol Med,2016,37(1):149-156. [5] 周思敏,郑善军,张钢.大蒜总皂苷对小鼠耐缺氧作用的实验研究[J].中国病理生理杂志,2015(10):1897. [6] 柏冬,王瑞海,刘丽梅.大蒜皂苷对照品制备及比色法测定大蒜皂苷提取物中总皂苷含量[J].中国中医药信息杂志,2012,19(9):55-58. [7] 张家伟,王晓明,潘桂湘,等.UPLC-MS/MS法测定大鼠灌服稳心颗粒后血浆中3个皂苷成分及其药动学研究[J].辽宁中医杂志,2016(8):1717-1720. [8] 宋兴良,梁恕坤,赵翊萌,等.柱前衍生化-HPLC法测定大蒜中甾体皂苷的含量[J].中国药房,2016,27(3):361-364. [9] 周梦娣,何功浩,倪伟,等.LC-MS/MS法测定大鼠血浆中丫蕊花皂苷G的浓度及其体内药动学研究[J].华西药学杂志,2018,33(3):279-282. [10] 刘继华,卢丹,刘金平,等.大鼠肌内注射20(S)-人参皂苷Rg3的药动学研究[J].中国药学杂志,2007,42(14):1087-1090. -
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