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.
Highlights
Tangeretin (40,5,6,7,8-pentamethoxyflavone, TAN, Figure 1a) is one of the most abundant polymethoxyflavones present in the peel of various citrus fruits [1,2]
To our results generated from this study will facilitate further investigations on the medicinal potentials of knowledge, this is the first assessment on the intravenous pharmacokinetics and F of TAN
The results generated from this study will facilitate further investigations on the medicinal potentials of TAN
Summary
Tangeretin (40 ,5,6,7,8-pentamethoxyflavone, TAN, Figure 1a) is one of the most abundant polymethoxyflavones present in the peel of various citrus fruits [1,2]. Pharmacokinetic profiling is an integral step in drug discovery and development. The physiological reference of the in vitro pharmacological effects of a drug candidate depends on its in vivo pharmacokinetic profile. The measurement of the level of a drug candidate and its active metabolite in biological matrices over time helps to build a better correlation between its dosing regimen and its pharmacological responses. The pharmacokinetic profiling of TAN has been attempted before [27,28,29], due to the lack of an intravenous pharmacokinetic study, many important kinetic
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