范汇森1,2,闫秋莹1,张海彬1,2,程海波1,3,沈卫星1,王振中2*,孙东东1,3*.UPLC-MS/MS法测定大鼠血浆中紫草氰苷、格列风内酯浓度[J].南京中医药大学学报(社会科学版),2018,34(1):91-95. |
UPLC-MS/MS法测定大鼠血浆中紫草氰苷、格列风内酯浓度 |
Determination of Lithospermoside and Griffonilide in Rat Plasma by UPLC-MS/MS |
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DOI: |
中文关键词: 天葵子 紫草氰苷 格列风内酯 UPLC-MS/MS 药物代谢动力学 |
英文关键词: Semiaquilegiae radix lithospermoside griffonilide UPLC-MS/MS pharmacokinetics |
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中文摘要: |
目的 建立使用UPLC-MS/MS法测定大鼠血浆中紫草氰苷、格列风内酯浓度的方法,并研究其药物代谢动力学特征。方法 采用Aglient C18色谱柱(100 mm×2.1 mm,1.8 μm),流动相为乙腈(A)-0.1%甲酸水溶液(B),梯度洗脱(0~1 min,5%~20%B;1~2 min,20%~60%B;2~6 min,60%~70%B;6~6.5 min,70%~5%B;6.5~7.5 min,5%B),流速0.3 mL/min,柱温35 ℃。大鼠灌胃给药量为4 g/(kg·d),使用液质联用色谱法测定给药后不同时间点紫草氰苷和格列风内酯的血药浓度,通过DAS2.0软件模拟计算,得出相应的药物代谢动力学参数。结果 在大鼠血浆中,紫草氰苷在0.701 9~140.4 ng/mL,格列风内酯在1.120~240.4 ng/mL内线性关系良好,两者日内、日间精密度和准确度RSD均小于15%,回收率在87.22%~107.75%之间。紫草氰苷和格列风内酯在体内吸收均较迅速,0.5 h达到最高血药浓度,并且消除速率较快,24 h基本消除。结论 经方法学检验,此方法准确、稳定,可用于紫草氰苷和格列风内酯的药物代谢动力学研究。 |
英文摘要: |
OBJECTIVE To establish an UPLC-MS/MS method for the determination of lithospermoside and griffonilide in rat plasma and study its pharmacokinetic characteristics. METHODS The separation was performed on Aglient C18 column (100 mm×2.1 mm,1.8 μm) with acetonitrile (A) and 0.1% aqueous formic acid (B) as the gradient elution mobile phase (0~1 min,5%~20%B;1~2 min, 20%~60%B;2~6 min,60%~70%B;6~6.5 min,70%~5%B;6.5~7.5 min,5%B), the flow rate was 0.3 mL/min, the column temperature was set at 35 ℃ and the injection volume was 3 μL. UPLC-MS/MS was used to detected the concentration of lithospermoside and griffonilide in rat plasma after oral administration of Semiaquilegiae Radix. The pharmacokinetics parameters of lithospermoside and griffonilide were calculated by DAS 2.0 software. RESULTS Good linearity was found in lithospermoside and griffonilide within linear range from 0.701 9 ~ 140.4 ng/mL and 1.120 2 ~ 240.4 ng/mL, respectively. The RSD of accuracy and intra-/inter-day precision were less than 15%. The recovery of the method was ranged from 87.22% to 107.75%. Lithospermoside and griffonilide were absorbed rapidly, the highest plasma concentration reached at 0.5 h, and the drug removed from body very fast and eliminated completely in 24 h. CONCLUSION This method is accuracy and stability for the study on pharmacokinetics of lithospermoside and griffonilide in rat plasma. |
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