کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
7626581 | 1494582 | 2018 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
A simple and sensitive HPLC-MS/MS method for quantification of eggmanone in rat plasma and its application to pharmacokinetics
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آنالیزی یا شیمی تجزیه
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چکیده انگلیسی
Allosteric phosphodiesterase 4 (PDE4) inhibitors are highly sought after due to their important anti-inflammatory and anti-cancer therapeutic effects. We recently identified Eggmanone, an extraordinarily selective allosteric PDE4 inhibitor displaying favorable drug properties. However, a specific analytic method of Eggmanone in serum and its pharmacokinetics have not been reported yet. In this study, we developed a rapid and sensitive high performance liquid chromatography-mass spectrometric (HPLC-MS/MS) method to determine Eggmanone concentrations in rat plasma. This assay method was validated in terms of specificity, linearity, sensitivity, accuracy, precision, matrix effect, recovery and stability, and was applied to a pharmacokinetic study in rats following intravenous injection of Eggmanone at doses of 1 and 3â¯mg/kg. The lower limit of quantification (LLOQ) of this assay was 5â¯ng/mL and the linear calibration curve was acquired with R2â¯>â¯0.99 between 5 and 1000â¯ng/m. The intra-day and inter-day precision was evaluated with the coefficient of variations less than 11.09%, whereas the mean accuracy ranged from 98.38% to 105.13%. The assay method exhibited good recovery and negligible matrix effect. The samples were stable under all the experimental conditions. The plasma concentrations of Eggmanone were detected and quantified over 24â¯h with the terminal elimination half-live of 3.57â¯Â±â¯1.80â¯h and 5.92â¯Â±â¯3.34â¯h for the low dose (1â¯mg/kg) and high dose (3â¯mg/kg) respectively. In summary, the present method provides a robust, fast and sensitive analytical approach for quantification of Eggmanone in plasma and was successfully applied to a pharmacokinetic study in rats.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 153, 10 May 2018, Pages 37-43
Journal: Journal of Pharmaceutical and Biomedical Analysis - Volume 153, 10 May 2018, Pages 37-43
نویسندگان
Chen Xie, Ana Ramirez, Zhijun Wang, Moses S.S. Chow, Jijun Hao,