Journal of Pharmaceutical Investigation
- Volume 28 Issue 2
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- Pages.73-80
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- 1998
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- 2093-5552(pISSN)
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- 2093-6214(eISSN)
Metabolite Kinetics of Trimebutine to N-monodesmethyl Trimebutine in Rats
트리메부틴의 N-모노데스메칠 트리메부틴으로의 대사동태
- Lee, Yong-Bok (College of Pharmacy, Chonnam National University) ;
- Chang, Woo-Ik (R & D Center. Dae Woong Pharmaceutical Co.. Ltd.) ;
- Koh, Ik-Bae (College of Pharmacy, Chonnam National University)
- Published : 1998.06.20
Abstract
In order to elucidate the effect of N-demethylation on the in vivo metabolite kinetics, especially hepatic first-pass effect of trimebutine(TMB), the N-demethylation of TMB to N-monodesmethyl trimebutine(N-TMB) was studied in rats. TMB(10 mg/kg) and N-TMB(10 mg/kg) were injected into the femoral and the portal vein, respectively. And the pharmacokinetic parameters were obtained from the plasma concentration-time profiles of TMB and N-TMB determined by the simultaneous analysis using high-performance liquid chromatography. It was supposed that these drugs were almost metabolized in vivo because the urinary and biliary excreated amounts of TMB and N-TMB were lower than 0.1% of the administered dose. According to the hepatic biotransformation model and metabolic pathways of TMB proposed, it was found that the fraction of systemic clearance of TMB which formed N-TMB in liver
Keywords
- Metabolite kinetics;
- Trimebutine;
- N-monodesmethyl trimebutine;
- Sequential hepatic first-pass metabolism;
- N-demethylation