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Paek, In Bok,Kim, Sung Yeon,Kim, Maeng Sup,Kim, John,Lee, Gwansun,Lee, Hye Suk Taylor Francis 2007 Journal of toxicology and environmental health. Pa Vol.70 No.15
<P> HM-30181, 4-oxo-4H-chromene-2-carboxylic acid [2-(2-{4-[2-(6,7-dimethoxy-3,4-dihydro-1H-isoquinolin-2-yl)-ethyl]-phenyl}-2H-tetrazol-5-yl)-4,5-dimethoxy-phenyl]-amide, is a new P-glycoprotein inhibitor with the potential to increase the cytotoxic activity of orally coadministered paclitaxel. This study was performed to characterize human cytochrome P-450 (CYP) enzymes involved in the metabolism of HM-30181 to 4- or 5-O-desmethyl-HM-30181 (M2) and 6- or 7-O-desmethyl-HM-30181 (M3) and to investigate the inhibitory potential of HM-30181 on CYP enzymes in human liver microsomes. CYP3A4 was identified as the major isozyme responsible for the O-demethylation of HM-30181 to M2 and M3 based on the correlation analysis, chemical inhibition and immuno-inhibition study and metabolism in cDNA-expressed human CYP isozymes. HM-30181 itself had no inhibitory effects on CYPs 1A2, 2A6, 2C8, 2C9, 2C19, 2D6, and 3A4 in human liver microsomes, suggesting the possibility that the pharmacokinetics of HM-30181 could be changed with coadministration of known CYP3A4 inducers or inhibitors.</P>
Pharmacokinetics of a ginseng saponin metabolite compound K in rats
Paek, In Bok,Moon, Ya,Kim, John,Ji, Hye Young,Kim, Soon Ai,Sohn, Dong Hwan,Kim, Jae Baek,Lee, Hye Suk John Wiley Sons, Ltd. 2006 BIOPHARMACEUTICS AND DRUG DISPOSITION Vol.27 No.1
<P>The absorption, dose-linearity and pharmacokinetics of compound K, a major intestinal bacterial metabolite of ginsenosides, were evaluated in vitro and in vivo. Using the Caco-2 cell monolayers, compound K showed moderate permeability with no directional effects, thus suggesting passive diffusion. After intravenous dose (i.v.; 1, 2, and 10 mg/kg), no significant dose-dependency was found in Cl (17.3–31.3 ml/min/kg), V<SUB>ss</SUB> (1677–2744 ml/kg), dose-normalized AUC (41.8–57.8 µg·min/ml based on 1 mg/kg) and t<SUB>1/2</SUB>. The extent of urinary excretion was minimal for both i.v. and oral doses. The extent of compound K recovered from the entire gastrointestinal tract at 24h were 24.4%–26.2% for i.v. doses and 54.3%–81.7% for oral doses. Following oral administration (doses 5–20 mg/kg), dose-normalized AUC (based on 5 mg/kg) was increased at the 20 mg/kg dose (85.3 µg·min/ml) compared with those at lower doses (4.50–10.5 µg·min/ml). Subsequently, the absolute oral bioavailability (F) was increased from 1.8%–4.3% at the lower doses to 35.0% at the 20 mg/kg dose. The increased F could be related to the saturation of carrier-mediated hepatic uptake and esterification of compound K with fatty acids in the liver. Copyright © 2005 John Wiley & Sons, Ltd.</P>
Moon, Ya,Paek, In-Bok,Kim, Hui-Hyun,Ji, Hye-Young,Lee, Hye-Won,Park, Hyoung-Geun,Lee, Hye-Suk The Pharmaceutical Society of Korea 2004 Archives of Pharmacal Research Vol.27 No.9
A rapid, sensitive and selective hydrophilic interaction liquid chromatography-tandem mass spectrometric(HILIC-MS/MS) method for the determination of tiapride in human plasma was developed. Tiapride and internal standard, metoclopramide were extracted from human plasma with dichloromethane at basic pH and analyzed on an Atlantis HILIC silica column with the mobile phase of acetonitrile-ammonium formate (190 mM, pH 3.0) (94:6, v/v). The ana-Iytes were detected using an electrospray ionization tandem mass spectrometry in the multi-ple-reaction-monitoring mode. The standard curve was linear (r=0.999) over the concentration range of 1.00-200 ng/mL. The coefficient of variation and relative error for intra- and inter-assay at three QC levels were 6.4∼8.8% and -2.0∼3.6%, respectively. The recoveries of tiapride ranged from 96.3 to 97.4%, with that of metoclopramide (internal standard) being 94.2%. The lower limit of quantification for tiapride was 1.00 ng/mL using 1 00 $\mu$L of plasma sample.