Influence of mefenamic acid on the intestinal absorption and metabolism of three bioactive flavones in Radix Scutellariae and potential pharmacological impact. (March 2014)

• Record Type: Journal Article
• Authors: Li, Chenrui; Fong, Sophia Yui Kau; Mei, Qibing; Lin, Ge; Zuo, Zhong
• Is Part Of: Pharmaceutical biology. Volume 52:Number 3(2014:Mar.)
• Page Start: 291
• Page End: 297
• Publication Date: 2014-03
• Subjects: Pharmacognosy -- Periodicals; Materia medica, Vegetable -- Periodicals; 615.321
• DOI: 10.3109/13880209.2013.834366
• Languages: English
• ISSNs: 1388-0209

Abstract

<abstract> <title>Abstract</title> <p> <italic>Context</italic>: Mefenamic acid (MEF) and the dried root of <italic>Scutellaria baicalensis</italic> Georgi (<italic>Radix Scutellariae</italic>, RS) share a high possibility of combined medication to treat inflammation.</p> <p> <italic>Objective</italic>: The present study investigates the impact of MEF on absorption/disposition of three major components in RS (baicalein, B; wogonin, W; oroxylin A, OA) and further pharmacological changes.</p> <p> <italic>Materials and methods</italic>: The apparent permeability (P<sub>app</sub>) and percentage of metabolism of B, W and OA at 10 μΜ were measured at the absence/presence of MEF (100 μΜ) in the Caco-2 cell monolayer model. A modified whole blood assay was employed to quantify prostaglandin E<sub>2</sub> (PGE<sub>2</sub>) 4, 6 and 8 h post-oral administration with water suspension of MEF at 40 mg/kg and RS at 200 mg/kg.</p> <p> <italic>Results</italic>: In the presence of MEF, P<sub>app</sub> of B, W and OA were increased from 1.69 ± 0.89 × 10<sup>−6</sup>, 1.57 ± 0.10 × 10<sup>−6</sup> and 3.09 ± 0.70 × 10<sup>−6 </sup>cm/sec to 5.24 ± 0.27 × 10<sup>−6</sup>, 6.08 ± 0.19 × 10<sup>−6</sup> and 4.13 ± 0.38 × 10<sup>−6</sup>, whereas their percentage of metabolism was decreased from 72.75 ± 2.44%, 73.27 ± 3.25% and 89.84 ± 2.99% to 21.11 ± 0.69%, 17.90 ± 5.55% and 45.44 ± 3.38%. PGE<sub>2</sub> level was much lower in the co-administration group (49.04 ± 2.03 pg/ml) than in the MEF group (73.13 ± 3.03 pg/ml) or RS group (494.37 ± 11.75 pg/ml) 4 h post MEF dosing, suggesting a synergic effect.</p> <p> <italic>Discussion and conclusion</italic>: Co-administration of MEF and RS could induce potential alterations in their pharmacokinetic profiles and anti-inflammatory effects.</p> </abstract>