中国中药杂志

2015, v.40(19) 3859-3865

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沙棘膏中槲皮素、山柰素、异鼠李素血药浓度的HPLC-MS/MS测定及大鼠体内药代动力学研究
Determination of plasma concentration of quercetin,kaempferid and isorhamnetin in Hippophae rhamnoides extract by HPLC-MS / MS and pharmacokinetics in rats

刘宇;杨娟;陀扬凌;韦婷;曾勇;王平;孟宪丽;
LIU Yu;YANG Juan;TUO Yang-ling;WEI Ting;ZENG Yong;WANG Ping;MENG Xian-li;College of Pharmacy,Chengdu University of Traditional Chinese Medicine;

摘要(Abstract):

建立大鼠血浆中槲皮素、山柰素、异鼠李素的HPLC-MS/MS分析方法,用于沙棘膏中3种黄酮类成分在正常大鼠体内的药代动力学研究。该实验选用正常SD大鼠,单剂量灌胃沙棘膏(槲皮素26.35 mg·kg-1、山柰素4.040 mg·kg-1、异鼠李素31.37 mg·kg-1)后不同时间点采血,采用高效液相色谱-质谱连用(HPLC-MS/MS)系统进行槲皮素、山柰素、异鼠李素血药浓度测定,以kinetica 5.0.11软件,对数据进行二房室动力学拟合,计算主要药动学参数。经方法学考证,槲皮素、山柰素、异鼠李素的线性范围分别为7.500~600.0μg·L-1(R2=0.998 5),1.000~80.00μg·L-1(R2=0.998 5),10.00~800.0μg·L-1(R2=0.998 0),日内、日间精密度RSD≤14%,血浆样品冻融1次,-20℃放置15 d,室温放置6 h以及处理后的分析物-20℃放置24 h的稳定性均良好,符合生物样品分析要求。大鼠灌胃沙棘膏后的药代参数如下,槲皮素t1/2β(113.3±19.37)h,AUC0-t(12 542.14±3 504.05)μg·h·L-1,MRT0-∞(119.6±13.29)h,Cmax(164.6±27.33)μg·L-1,Tmax(5.199±0.840 3)h;山柰素t1/2β(79.85±17.15)h,AUC0-t(934.51±94.59)μg·h·L-1,MRT0-∞(81.50±13.75)h,Cmax(80.15±14.24)μg·L-1,Tmax(3.827±0.902 7)h;异鼠李素t1/2β(118.3±20.73)h,AUC0-t(26 067.77±4 124.60)μg·h·L-1,MRT0-∞(129.0±16.30)h,Cmax(269.6±29.32)μg·L-1,Tmax(6.513±1.450)h。该文所建立的灵敏、准确的HPLC-MS/MS检测方法适用于大鼠血浆中槲皮素、山柰素、异鼠李素成分的药代动力学研究。
To establish an HPLC-MS/MS method for the analysis of quercetin,kaempferid and isorhamnetin in rats plasma and study its pharmamacokinetics after an intragastrical administration of Hippophae rhamnoides extracts. Five healthy male Sprague-Dawley( SD) rats were given single doses of H. rhamnoides extracts( quercetin 26. 35 mg·kg- 1,kaempferid 4. 040 mg·kg- 1,isorhamnetin31. 37 mg·kg- 1),and then their orbital sinus blood samples were collected at different time points. The drug plasma concentration of the three flavonoids was determined by HPLC-MS / MS method. After that,the main pharmacokinetics parameters were calculated by using Kinetica 5. 0. 11 software. The methodological test showed that the linear concentration ranges of quercetin,kaempferid and isorhamnetin were 7. 500-600. 0 μg · L- 1( R2= 0. 998 5),1. 000-80. 00 μg · L- 1( R2= 0. 998 5) and 10. 00-800. 0 μg · L- 1( R2= 0. 998 0),respectively. The inner and inter-days precisions were both less than 14. 0%. The plasma samples showed a good stability and consistency with the requirement of biological sample analysis after the samples were frozen once and placed at- 20 ℃ for15 d and room temperature for 6 h and the treated analytes were placed at- 20 ℃ for 24 h. For quercetin,the pharmacokinetic parameter t1 /2β,AUC0-t,MRT0-∞,Cmaxand Tmaxwere( 113. 3 ± 19. 37) min,( 12 542. 14 ± 3 504. 05) μg·h·L- 1,( 119. 6 ± 13. 29) h,( 164. 6 ± 27. 33) μg·L- 1and( 5. 199 ± 0. 840 3) h,respectively. For kaempferid,the pharmacokinetic parameters t1 /2β,AUC0-t,MRT0-∞,Cmaxand Tmaxwere( 79. 85 ± 17. 15) min,( 934. 51 ± 94. 59) μg·h·L- 1,( 81. 50 ± 13. 75) h,( 80. 15 ± 14. 24) μg·L- 1and( 3. 827 ± 0. 902 7) h,respectively. For isorhamnetin,the pharmacokinetic parameters t1 /2β,AUC0-t,MRT0-∞,Cmaxand Tmax were( 118. 3 ± 20. 73) min,( 26 067. 77 ± 4 124. 60) μg·h·L- 1,( 129. 0 ± 16. 30) h,( 269. 6 ± 29. 32) μg·L- 1and( 6. 513 ±1. 450) h,respectively. The HPLC-MS / MS analysis method established in this study was proved to be sensitive and accurate and could be applied in the pharmacokinetic study of quercetin,kaempferid and isorhamnetin in rat plasma.

关键词(KeyWords): 沙棘膏;槲皮素;山柰素;异鼠李素;药代动力学;HPLC-MS/MS
Hippophae rhamnoides extract;quercetin;kaempferide;isorhamnetin;pharmacokinetics;HPLC-MS/MS

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基金项目(Foundation): 四川省科技计划项目(2013SZ0114,2014SZ0071)

作者(Author): 刘宇;杨娟;陀扬凌;韦婷;曾勇;王平;孟宪丽;
LIU Yu;YANG Juan;TUO Yang-ling;WEI Ting;ZENG Yong;WANG Ping;MENG Xian-li;College of Pharmacy,Chengdu University of Traditional Chinese Medicine;

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