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Journal of ZheJiang University(Medical Science)  2011, Vol. 40 Issue (4): 395-401    DOI: 10.3785/j.issn.1008-9292.2011.04.009
    
Study on determination and pharmacokinetics of metabolites from Folium Mori extract in rats
JIANG Li-di,XUAN Gui-da,ZHAO Lan,ZHU Yan-fei,LOU Xue-fang
School of Medicine and Life Science,Zhejiang University City College,Hangzhou 310015,China
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Abstract  Objective: To establish a RP-HPLC method for simultaneous determination of total quercetin,kaempferol and isorhamnetin in rat plasma after oral administration of Folium Mori extract (FME).
Methods: After a single dose of FME (110 mg/kg) was taken,rat plasma samples were collected. The samples were hydrolyzed with hydrochloric acid (c=3.0 mol/L),the mixed solution was extracted with etheracetone mixture. The total quercetin,kaempferol and isorhamnetin in plasma samples were determined by HPLC,pharmacokinetic parameters were calculated by DAS 3.0 software.
Results: The method was linear over the concentration ranges of 0.0545-8.70,0.0954-14.7 and 0.0545-8.55 μg/ml for quercetin,kaempferol and isorhamnetin,respectively (r=0.9979,0.9993,0.9981). The absolute recoveries were 85.3%-86.1%,79.4%-86.7% and 62.8%-89.7%,respectively and the assay recoveries were all from 94.7% to 107%. The relative standard deviation (RSD) of intra-and inter-day were less than 9.5% and 9.8%,respectively. The main pharmacokinetic parameters were as follows: T1/2z was 92.7,67.9 and 54.2 h; Tmax was 0.400,0.400 and 3.87 h; AUC(0-∞) was 68.0,67.5 and 32.8 mg/h/L; MRT(0-∞) was 128,85.2 and 72.0 h for quercetin,kaempferol and isorhamnetin,respectively.
Conclusions: The method established in this study is accurate,reliable and reproducible,and can be applied for determination of total quercetin,kaempferol and isorhamnetin in rat plasma after oral administration of FME; the pharmacokinetic studies showed that the distribution of drugs is rapid and elimination is very slow.


Key wordsQuercetin/anal      Folium mori/chem      Naphthols/anal      Folium Mori extract;       HPLC      Kaempferol      Isorhamnetin      Pharmacokinetics     
Published: 25 July 2010
Cite this article:

. Study on determination and pharmacokinetics of metabolites from Folium Mori extract in rats. Journal of ZheJiang University(Medical Science), 2011, 40(4): 395-401.

URL:

https://www.zjujournals.com/med/10.3785/j.issn.1008-9292.2011.04.009     OR     https://www.zjujournals.com/med/Y2011/V40/I4/395


桑叶提取物在大鼠体内的代谢产物含量测定及其药动学研究

目的:建立大鼠血浆中槲皮素、山萘酚及异鼠李素总浓度的高效液相色谱法,并计算大鼠口服桑叶提取物(Folium Mori extract,FME)后血浆中主要代谢产物-槲皮素、山萘酚及异鼠李素的药动学参数。
方法:大鼠口服110 mg/kg桑叶提取物后,取其血浆并用3 mol/L盐酸水解,水解液经乙醚-丙酮混合液萃取,用HPLC法测定血浆中槲皮素、山萘酚及异鼠
李素总浓度,以DAS 3.0软件计算药动学参数。
结果:槲皮素、山萘酚和异鼠李素分别在
0.0545~8.70,0.0954~14.7和0.0545~8.55 μg/ml内呈良好线性关系,r分别为0.9979、0.9993、
0.9981;三者的绝对回收率分别在85.3%~86.1%、79.4%~86.7%、62.8%~89.7%内,方法回
收率均在94.7%~107%内。日内及日间精密度RSD分别小于9.5%及9.8%。以药动学软件
计算的药动学统计矩参数T1/2z 分别为 92.7,67.9和54.2 h ;Tmax 分别为 0.400、0.400
和3.87 h;AUC(0-∞)分别为68.0、67.5和32.8 mg·h-1·L-1;MRT(0-∞)分别为128、85.2和72.0 h。
结论:本法准确可靠,操作简便,重复性好,可用于同时测定桑叶提取物在大鼠体内的主要
代谢产物-槲皮素、山萘酚及异鼠李素的总浓度;同时,药动学研究显示,三者在大鼠体内
分布迅速,滞留久长。

关键词: 槲皮素/分析,  桑叶/化学,  萘酚类/分析,  桑叶提取物,  高效液相色谱法,  山萘酚,  异鼠李素,  药动学 
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