title: Quantification of trans-3,4,5,4'-Tetramethoxystilbene in rat plasma by HPLC: application to pharmacokinetic study.
abstract: A simple HPLC method was established to quantify trans-3,4,5,4'-tetramethoxystilbene (MR-4 or DMU-212) in rat plasma. Chromatographic separation was obtained with a reversed-phase HPLC column through an 11 min gradient delivery of a mixture of acetonitrile and water at a flow rate of 1.5 mL/min at 50 °C. The limit of quantification was 15 ng/mL. The intra- and interday precisions in terms of relative standard deviation were <9% at all concentrations. Similarly, the accuracy was good, and the bias rates ranged within ±7%. The pharmacokinetic profiles of MR-4 were subsequently assessed in rats using 2-hydroxypropyl-β-cyclodextrin as a dosing vehicle. Upon intravenous administration, MR-4 displayed moderate clearance (46.5 ± 7.6 mL/min/kg) and terminal elimination half-life (154 ± 80 min). However, the absolute oral bioavailability of MR-4 was low (6.31 ± 3.30%). Future investigation on MR-4 as a chemotherapeutic agent should be focused on colorectal cancers.
authors.affiliation: Department of Pharmacy, National University of Singapore , 10 Kent Ridge Crescent, Singapore 119260.
authors.forename: Hai-Shu
authors.initials: HS
authors.lastname: Lin
authors.forename: Wei
authors.initials: W
authors.lastname: Zhang
authors.forename: Mei Lin
authors.initials: ML
authors.lastname: Go
authors.forename: Corrado
authors.initials: C
authors.lastname: Tringali
authors.forename: Carmela
authors.initials: C
authors.lastname: Spatafora
authors.forename: Paul C
authors.initials: PC
authors.lastname: Ho
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000970:Antineoplastic Agents; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D006207:Half-Life; D007275:Injections, Intravenous; D008297:Male; D051381:Rats; D017207:Rats, Sprague-Dawley; D015203:Reproducibility of Results; D013267:Stilbenes / Q000097:blood* / Q000493:pharmacokinetics*
chemical_list: C482492:3,4,5,4'-tetramethoxystilbene; D000970:Antineoplastic Agents; D013267:Stilbenes