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Pharmaceutics 2018, 10(1), 3; doi:10.3390/pharmaceutics10010003

Determination of Tangeretin in Rat Plasma: Assessment of Its Clearance and Absolute Oral Bioavailability

Department of Pharmacy, Faculty of Science, National University of Singapore, 18 Science Drive 4, Singapore 117543, Singapore
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Author to whom correspondence should be addressed.
Received: 6 November 2017 / Revised: 9 December 2017 / Accepted: 24 December 2017 / Published: 29 December 2017
(This article belongs to the Special Issue Preclinical Pharmacokinetics and Bioanalysis)
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Abstract

Tangeretin (TAN) is a dietary polymethoxylated flavone that possesses a broad scope of pharmacological activities. A simple high-performance liquid chromatography (HPLC) method was developed and validated in this study to quantify TAN in plasma of Sprague-Dawley rats. The lower limit of quantification (LLOQ) was 15 ng/mL; the intra- and inter-day assay variations expressed in the form of relative standard deviation (RSD) were all less than 10%; and the assay accuracy was within 100 ± 15%. Subsequently, pharmacokinetic profiles of TAN were explored and established. Upon single intravenous administration (10 mg/kg), TAN had rapid clearance (Cl = 94.1 ± 20.2 mL/min/kg) and moderate terminal elimination half-life (t1/2 λz = 166 ± 42 min). When TAN was given as a suspension (50 mg/kg), poor but erratic absolute oral bioavailability (mean value < 3.05%) was observed; however, when TAN was given in a solution prepared with randomly methylated-β-cyclodextrin (50 mg/kg), its plasma exposure was at least doubled (mean bioavailability: 6.02%). It was obvious that aqueous solubility hindered the oral absorption of TAN and acted as a barrier to its oral bioavailability. This study will facilitate further investigations on the medicinal potentials of TAN. View Full-Text
Keywords: tangeretin; high performance liquid chromatography; clearance; absolute oral bioavailability tangeretin; high performance liquid chromatography; clearance; absolute oral bioavailability
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Elhennawy, M.G.; Lin, H.-S. Determination of Tangeretin in Rat Plasma: Assessment of Its Clearance and Absolute Oral Bioavailability. Pharmaceutics 2018, 10, 3.

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