Rapid Quantification of Astilbin in Rat Plasma by Liquid Chromatography-tandem Mass Spectrometry and Its Application to Pharmacokinetic Study

doi:10.1007/s40242-013-3166-8

Chemical Research in Chinese Universities ›› 2013, Vol. 29 ›› Issue (6): 1078-1082.doi: 10.1007/s40242-013-3166-8

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Rapid Quantification of Astilbin in Rat Plasma by Liquid Chromatography-tandem Mass Spectrometry and Its Application to Pharmacokinetic Study

YIN Lei^1,2, ZHANG Yun-hui¹, ZHAO Sen¹, CHENG Long-mei¹, SHI Mei-yun¹, YANG Yan^1,3,4, SUN Yan-tong^2,5, LIU Xi-dong¹, FAWCETT J. Paul⁶

1. School of Life Sciences, Jilin University, Changchun 130012, P. R. China;
2. Clinical Pharmacology Center, Research Institute of Translational Medicine, the First Hospital of Jilin University, Changchun 130061, P. R. China;
3. National Engineering Laboratory for AIDS Vaccine, Jilin University, Changchun 130012, P. R. China;
4. Key Laboratory for Molecular Enzymology and Engineering, the Ministry of Education, Jilin University, Changchun 130012, P. R. China;
5. School of Pharmaceutical Sciences, Jilin University, Changchun 130021, P. R. China;
6. School of Pharmacy, University of Otago, Dunedin 9054, New Zealand

Received:2013-04-10 Revised:2013-06-24 Online:2013-12-01 Published:2013-07-02
Contact: YANG Yan, SUN Yan-tong E-mail:yyan@jlu.edu.cn;sunyt@jlu.edu.cn
Supported by:
Supported by the National Natural Science Foundation of China(No.81102383), the Science and Technology Major Specialized Projects for "Significant New Drugs Creation" of the 12th Five-year Plan of China(No.2012ZX09303-015) and the National Key Technology R&D Program of the Ministry of Science and Technology, China(No.2012BAI30B00).

Abstract

Abstract:

Astilbin is a potential immunosuppressive agent with minor cytotoxicity. Its oral bioavailability is supposed to be rather low and therefore a sensitive analytical method is required for its pharmacokinetic study after oral administration. A simple, sensitive and rapid liquid chromatography-tandem mass spectrometry(LC-MS/MS) method was developed and validated for the determination of astilbin in rat plasma. Plasma samples were subjected to liquid-liquid extraction with ethyl acetate and separated by reversed phase high performance liquid chromatography(HPLC) with methanol-0.01%(volume fraction) formic acid(50:50, volume ratio) as mobile phase. Quantitive determination was achieved on negative LC-MS/MS by a multiple reaction moitoring method with transitions m/z 449.1→150.9(quantifier) and m/z 449.1→284.9(qualifier) for astilbin and m/z 128.9→42.0 for internal standard(IS). A lower limit of quantification(LLOQ) of ng/mL was achieved within a short cycle time of 3.4 min. The method was successfully applied to a pharmacokinetic study involving oral and intravenous administrations of 6 mg/kg astilbin to six rats.

Key words: Astilbin, Liquid chromatography-tandem mass spectrometry(LC-MS/MS), Pharmacokinetics, Rat, Plasma

YIN Lei, ZHANG Yun-hui, ZHAO Sen, CHENG Long-mei, SHI Mei-yun, YANG Yan, SUN Yan-tong, LIU Xi-dong, FAWCETT J. Paul. Rapid Quantification of Astilbin in Rat Plasma by Liquid Chromatography-tandem Mass Spectrometry and Its Application to Pharmacokinetic Study[J]. Chemical Research in Chinese Universities, 2013, 29(6): 1078-1082.

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Rapid Quantification of Astilbin in Rat Plasma by Liquid Chromatography-tandem Mass Spectrometry and Its Application to Pharmacokinetic Study

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