代秋琼, 刘红斌, 崔佳丽, 赵高琼, 周艺佳, 梅晶, 王京昆. 三七提取物大鼠体内3种皂苷成分测定方法建立及药代动力学研究[J]. 云南大学学报(自然科学版), 2021, 43(1): 157-163. doi: 10.7540/j.ynu.20200210
引用本文: 代秋琼, 刘红斌, 崔佳丽, 赵高琼, 周艺佳, 梅晶, 王京昆. 三七提取物大鼠体内3种皂苷成分测定方法建立及药代动力学研究[J]. 云南大学学报(自然科学版), 2021, 43(1): 157-163. doi: 10.7540/j.ynu.20200210
DAI Qiu-qiong, LIU Hong-bin, CUI Jia-li, ZHAO Gao-qiong, ZHOU Yi-jia, MEI Jing, WANG Jing-kun. Establishment of a method for determination of three saponins composition from Panax notoginseng extract in rats and pharmacokinetic study[J]. Journal of Yunnan University: Natural Sciences Edition, 2021, 43(1): 157-163. DOI: 10.7540/j.ynu.20200210
Citation: DAI Qiu-qiong, LIU Hong-bin, CUI Jia-li, ZHAO Gao-qiong, ZHOU Yi-jia, MEI Jing, WANG Jing-kun. Establishment of a method for determination of three saponins composition from Panax notoginseng extract in rats and pharmacokinetic study[J]. Journal of Yunnan University: Natural Sciences Edition, 2021, 43(1): 157-163. DOI: 10.7540/j.ynu.20200210

三七提取物大鼠体内3种皂苷成分测定方法建立及药代动力学研究

Establishment of a method for determination of three saponins composition from Panax notoginseng extract in rats and pharmacokinetic study

  • 摘要: 对建立HPLC-MS/MS测定SD大鼠血浆中三七皂苷R1、人参皂苷Rg1、Rb1浓度的方法进行方法学验证,并研究三七提取物在SD大鼠体内的药代动力学. SD大鼠灌胃给予三七提取物1500 mg/kg后采集血样,HPLC-MS/MS测定血浆中Rg1、Rb1和R1的质量浓度,并利用DAS软件计算药动学参数. 建立的HPLC-MS/MS方法特异性良好,连续3批标准曲线相关系数均大于0.99(权重1/X2);血浆中3种成分的低、中、高3个质量浓度的日内精密度(RSD)均小于10%,准确度为88%~105%,日间精密度(RSD)均小于15%,准确度为93%~109%;冻融及室温稳定性良好,基质效应不影响测定. 采用非房室模型计算Rg1、Rb1和R1在大鼠体内的药代参数,结果表明,平均AUC0−tρmaxt1/2、MRT0−t的数值大小为Rb1>>Rg1>R1;平均Tmax的数值大小为Rb1>>R1>Rg1. 所建立的HPLC-MS/MS方法适用于三七提取物中Rg1、Rb1、R1在大鼠体内的药代动力学研究. Rg1、R1在大鼠体内具有相似的药代特征,吸收快、消除快;Rb1在大鼠体内的药代特征与Rg1、R1差别较大,吸收慢、消除慢;Rb1在大鼠体内的血浆暴露占绝对优势.

     

    Abstract: To verify the method of HPLC-MS/MS determination of notoginsenoside R1, Ginsenoside Rg1, Ginsenoside Rb1 in plasma of SD rats, the pharmacokinetics of Panax notoginseng extract in SD rats was studied. SD rats intragastrically administered Panax notoginseng extract of 1500 mg/kg had their blood collected for the determination of plasma concentration by HPLC-MS /MS, after which pharmacokinetic parameters were calculated by DAS software. The established HPLC-MS/MS method has good specificity, and the correlation coefficients of the three consecutive batches of standard curves are all greater than 0.99 (weighted 1/X2). The linearity of each component in certain concentration ranges was good. The RSD day precision of three components in plasma were less than 10% and the accuracy ranged from 88% to 105%. The diurnal precision (RSD) was less than 15% and the accuracy was between 93% to 109%. The stability of freeze-thaw and room temperature was good. The matrix effect does not affect the measurement effect. The non-compartmental model was used to calculate the pharmacokinetic parameters of Rg1, Rb1 and R1 in rats. The results showed that the average values of AUC0-t, ρmax, t1/2, and MRT0-t, Rb1>>Rg1>R1; average Tmax value of Rb1>> R1> Rg1. The established HPLC-MS/MS method is suitable for the pharmacokinetic study of Rg1, Rb1 and R1 in Panax notoginseng extract in rats. Rg1 and R1 have similar pharmacokinetic characteristics in rats, with rapid absorption and fast elimination; Rb1 pharmacokinetic characteristics in rats are very different from Rg1 and R1, with slow absorption and slow elimination; Rb1 exposure inplasma of rats take the absolute advantage.

     

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