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http://dx.doi.org/10.5487/TR.2008.24.3.195

Effects of Oral Rutaecarpine on the Pharmacokinetics of Intravenous Chlorzoxazone in Rats  

Bista, Sudeep R. (College of Pharmacy, Yeungnam University)
Lee, Sang-Kyu (Bioanalysis and Biotransformation Research Center, KIST)
Thapa, Dinesh (College of Pharmacy, Yeungnam University)
Kang, Mi-Jeong (College of Pharmacy, Yeungnam University)
Seo, Young-Min (College of Pharmacy, Yeungnam University)
Kim, Ju-Hyun (College of Pharmacy, Yeungnam University)
Kim, Dong-Hyeon (College of Pharmacy, Yeungnam University)
Jahng, Yurng-Dong (College of Pharmacy, Yeungnam University)
Kim, Jung-Ae (College of Pharmacy, Yeungnam University)
Jeong, Tae-Cheon (College of Pharmacy, Yeungnam University)
Publication Information
Toxicological Research / v.24, no.3, 2008 , pp. 195-199 More about this Journal
Abstract
It has been reported that hepatic microsomal cytochrome P450(CYP) 2E1 is responsible for the metabolism of chlorzoxazone(CZX) to 6-hydroxychlorzoxazone. The present study was undertaken to assess the possible interaction of rutaecarpine, an alkaloid originally isolated from the unripe fruit of Evodia rutaecarpa, with CZX. Male Spraque-Dawley rats were administered with 80 mg/kg/day of oral rutaecarpine for three consecutive days. Twenty four hr after the pre-treatment with rutaecarpine, the rats were treated with 20 mg/kg of intravenous CZX. Rat hepatic microsomes isolated from rutaecarpine-treated rats showed greater(50% increase) activity of p-nitrophenol hydroxylase(a marker of CYP2E1) when compared with the control rats. Compared with control rats, the AUC of CZX was significantly smaller(84% decrease) possibly due to significantly faster CL(646% increase) in rats pretreated with rutaecarpine. This could be, at least partially, due to induction of CYP2E1 by rutaecarpine.
Keywords
Rutaecarpine; Chlorzoxazone; Interaction; Pharmacokinetics; CYP2E1; In vivo;
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Times Cited By KSCI : 4  (Citation Analysis)
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