Biomolecules & Therapeutics

The Korean Society of Applied Pharmacology (한국응용약물학회)
권호 표지
DOI QR코드

DOI QR Code

Effect of Phenobarbital on the Pharmacokinetics of Rutaecarpine and its Metabolite in Rats

  • Published : 2008.09.30
Download PDF
⟨ Previous Next ⟩

Abstract

To investigate the possible interaction between rutaecarpine and phenobarbital in rats, phenobarbital in saline at 80 mg/kg was given ip to male SD rats for 3 consecutive days. Saline was given to control animals. One day after phenobarbital pre-treatment, rutaecarpine at 16 mg/kg was administered through penile vein. Blood was collected and analyzed by using HPLC. The pharmacokinetic parameters were determined with the non-compartmental model. Pre-treatment with phenobarbital significantly altered the pharmacokinetic profiles of rutaecarpine and its metabolite, 10-hydroxyrutaecarpine. The AUC of rutaecarpine was reduced to approximately 50% of control and the plasma half-life of rutaecarpine was significantly shortened when compared with control. In addition, the Cmax of 10-hydroxyrutaecarpine was increased approximately 160% of control. The AUC and the plasma half-life of 10-hydroxyrutaecarpine were decreased to 76.9% of control and to 82.7 min from 175.9 min, respectively. The results suggested that phenobarbital might accelerate the metabolism of rutaecarpine, thereby changing the pharmacokinetic parameters of rutaecarpine in male SD rats.

Keywords

References

  1. Chiou, W.F., Liao, J.P., and Chen, C.F. (1996) Comparative study of the vasodilatory effects of three quinazoline alkaloids isolated from Evodia rutaecarpa. J. Nat. Prod. 59, 374-378 https://doi.org/10.1021/np960161+
  2. Lee, S.H., Kim, S.I., Park, J.G., Lee, E.S., and Jahng, Y. (2001) A simple synthesis of rutaecarpine. Heterocycles 55, 1555-1559 https://doi.org/10.3987/COM-01-9244
  3. Lee, S.K., Kim, N.H., Lee, J., Kim, D.H., Lee, E.S., Choi, H.G., Chang, H.W., Jahng, Y., and Jeong, T.C. (2004a) Induction of cytochrome P450s by rutaecarpine and metabolism of rutaecarpine by cytochrome P450s. Planta Med. 70, 753-757 https://doi.org/10.1055/s-2004-827207
  4. Lee, S.K., Lee, D.W., Jeon, T.W., Jin, C.H., Kim, G.H., Jun, I.H., Lee, D.J., Kim, S.I., Kim, D.H., Jahng, Y., and Jeong, T.C. (2005) Characterization of the phase 2 metabolites of rutaecarpine in the rat by liquid chromatography-electrospray ionization tandem mass spectrometry. Xenobiotica 35, 1135-1145 https://doi.org/10.1080/00498250500363742
  5. Lee, S.K., Lee, J., Lee, E.S., Jahng, Y., Kim, D.H., and Jeong, T.C. (2004b) Characterization of in vitro metabolites of rutaecarpine in rat liver microsomes using liquid chromatography/ tandem mass spectrometry. Rapid Commun. Mass Spectrom. 18, 1073-1080 https://doi.org/10.1002/rcm.1448
  6. Moon, T.C., Murakami, M., Kudo, I., Son, K.H., Kang, S.S., and Chang, H.W. (1999) A new class of COX-2 inhibitor, rutaecarpine from Evodia rutaecarpa. Inflamm. Res. 48, 621-625 https://doi.org/10.1007/s000110050512
  7. Park, E.J., Cho, H.Y., and Lee, Y.B. (2005) Effect of cimetidine and phenobarbital on metabolite kinetics of omeprazole in rats. Arch. Pharm. Res. 28, 1196-1202 https://doi.org/10.1007/BF02972986
  8. Son, J.K., Park, J.G., and Jahng, Y. (2003) A simple synthesis of tryptanthrin. Heterocycl. Commun. 9, 621-624
  9. Ueng, Y.F., Yu, H.J., Lee, C.H., Peng, C., Jan, W.C., Ho, L.K., Chen, C.F., and Don, M.J. (2005) Identification of the microsomal oxidation metabolites of rutaecarpine, a main active alkaloid of the medicinal herb Evodia rutaecarpa. J. Chromatogr. A 1076, 103-109 https://doi.org/10.1016/j.chroma.2005.04.021
  10. Woo, H.G., Lee, C.H., Noh, M.S., Lee, J.J., Jung, Y.S., Baik, E.J., Moon, C.H., and Lee, S.H. (2001) Rutaecarpine, a quinazolinocarboline alkaloid, inhibits prostaglandin production in RAW264.7 macrophages. Planta Med. 67, 505-509 https://doi.org/10.1055/s-2001-16479

Cited by

  1. Simultaneous determination and pharmacokinetic analysis of seven alkaloids and two flavonoids from rat plasma by HPLC–DAD after oral administration of Wuzhuyu decoction vol.14, pp.4, 2012, https://doi.org/10.1080/10286020.2012.656093
  2. Detection and characterization of the metabolites of rutaecarpine in rats based on ultra-high-performance liquid chromatography with linear ion trap-Orbitrap mass spectrometer vol.55, pp.1, 2017, https://doi.org/10.1080/13880209.2016.1236392