Application of a sensitive and specific LC-MS/MS method for determination of chinensinaphthol methyl ether in rat plasma for a bioavailability study

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• 作者：Shujun Zhou ; Feng Qiu ; Zhanqi Tong ; Shihai Yang ; Meihua Yang
• 关键词：Justicia procumbens ; Chinensinaphthol methyl ether ; Bioavailability ; LC&ndash ; MS/MS ; Rat
• 刊名：Journal of Chromatography B, Analytical Technologies in the Biomedical and Life Sciences
• 出版年：2012
• 出版时间：15 August, 2012
• 年：2012
• 卷：903
• 期：Complete
• 页码：75-80
• 全文大小：295 K

文摘

Chinensinaphthol methyl ether (CME) is a potential pharmacologically active ingredient isolated from the dried plants of Justicia procumbens L. (Acanthaceae). A sensitive and specific LC-MS/MS method was developed and validated for the analysis of CME in rat plasma using buspirone as the internal standard (IS). The analyte was extracted with ethyl acetate and chromatographed on a reverse-phase Agilent Zorbax-C18 110 ? column (50 mm ¡Á 2.1 mm, 3.5 ¦Ìm). Elution was achieved with a gradient mobile phase consisting of water and acetonitrile both containing 0.1 % formic acid at a flow rate of 0.40 mL/min. The analytes were monitored by tandem-mass spectrometry with positive electrospray ionization. The precursor/product transitions (m/z) in the positive ion mode were 394.5 ¡ú 346.0 and 386.1 ¡ú 122.0 for CME and IS, respectively. The assay was shown to be linear over the range of 0.50-500 ng/mL, with a lower limit of quantification of 0.50 ng/mL. The method was shown to be reproducible and reliable with the inter- and intra-day accuracy and precision were within ¡À15 % . The assay has been successfully used for pharmacokinetic evaluation of CME after intravenous and oral administration of 1.80 mg/kg CME in rats. The oral absolute bioavailability (F) of CME was estimated to be 3.2 ¡À 0.2 % with an elimination half-life (t_1/2) value of 2.4 ¡À 0.8 h, suggesting its poor absorption and/or strong metabolism in vivo.