The pharmacokinetics of raloxifene and its interaction with apigenin in rat

Molecules

Volumn 15, Issue 11, 2010, Pages 8478-8487

  Chen, Yan ^a   Jia, Xiaobin ^a   Chen, Jian ^a   Wang, Jinyan ^a   Hu, Ming ^b  

^a KEY LABORATORY OF NEW DRUG DELIVERY SYSTEM OF CHINESE MATERIA MEDICA   (China)

^b UNIVERSITY OF HOUSTON   (United States)

Author keywords

Apigenin; Flavonoid; Interaction; Pharmacokinetics; Raloxifene; Rats

Indexed keywords

APIGENIN; RALOXIFENE;

ANIMAL; ARTICLE; DRUG INTERACTION; FEMALE; MALE; RANDOMIZATION; RAT; WISTAR RAT;

ANIMALS; APIGENIN; DRUG INTERACTIONS; FEMALE; MALE; RALOXIFENE; RANDOM ALLOCATION; RATS; RATS, WISTAR;

EID: 78649472328     PISSN: None     EISSN: 14203049     Source Type: Journal    
DOI: 10.3390/molecules15118478     Document Type: Article

References (22)

1. Scott, J.A.; Da Camara, C.C.; Early, J.E. Raloxifene: A selective estrogen receptor modulator. Am. Fam. Physician 1999, 60, 1131-1138.
2. Delmas, P.D.; Bjarnason, N.H.; Mitlak, B.H.; Ravoux, A.C.; Shah, A.S.; Huster, W.J.; Draper, M.; Christiansen, C. Effect of raloxifene on bone mineral density, serum cholesterol concentrations and uterine endometrium in postmenopausal women. New Engl. J. Med. 1997, 337,1641-1647.
3. Snyder, K.R.; Sparano, N.; Malinowski, J.M. Raloxifene hydrochloride. Am. J. Health-Syst. Pharm. 2000, 57, 1669-1678.
4. Lindstrom, T.D.; Whitaker, N.G.; Whitaker, G.W. Disposition and metabolism of a new benzothiophene antiestrogen in rats, dogs and monkeys. Xenobiotica 1984, 14, 841-847.
5. Heringa, M. Review on raloxifene: Profile of a selective estrogen receptor modulator. Int. J. Clin. Pharmacol. Ther. 2003, 41, 331-345.
6. Hochner-Celnikier, D. Pharmacokinetics of raloxifene and its clinical application. Eur. J. Obst. Gyn. Rep. Bio. 1999, 85, 23-29.
7. Jeong, E.J.; Liu, Y.; Lin, H.M.; Hu, M. Species-and disposition model-dependent metabolism of raloxifene in gut and liver: Role of UGT1A10. Drug Metab. Dispos. 2005, 33, 785-794.
8. Dalvie, D.; Kangm P.; Zientek, M.; Xiangm C.; Zhou. S.; Obach, R.S. Effect of intestinal glucuronidation in limiting hepatic exposure and bioactivation of raloxifene in humans and rats. Chem. Res. Toxicol. 2008, 21, 2260-2271.
9. Dodge, J.A.; Lugar, C.W.; Cho, S.; Short, L.L.; Sato, M.; Yang, N.N.; Spangle, L.A.; Martin, M.J.; Phillips, D.L.; Glasebrook, A.L. Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity. J. Steroid Biochem. Mol. Biol. 1997, 61, 97-106.
10. Middleton, J.E.; Kandaswami, C.; Theoharides, T.C. The effects of plant flavonoids on mammalian cells: Implications for inflammation, heart disease, and cancer. Pharmacol. Rev. 2000, 52, 673-751.
11. Leszek, O.; Joanna, F.; Waldemar, J.; Grzegorz, G.; Katarzyna, K. Differential effects of genistein, estradiol and raloxifene on rat osteoclasts in vitro. Pharmacol. Rep. 2005, 57, 352-359.
12. Mizuma, T. Intestinal glucuronidation metabolism may have a greater impact on oral bioavailability than hepatic glucuronidation metabolism in humans: A study with raloxifene, substrate for UGT1A1, 1A8, 1A9, and 1A10. Int. J. Pharm. 2009, 13, 140-141.
13. Setchell, K.D.; Brown, N.M.; Desai, P.B.; Zimmer-Nechimias, L.; Wolfe, B.; Jakate, A.S.; Creutzinger, V.; Heubi, J.E. Bioavailability, disposition, and dose-response effects of soy isoflavones when consumed by healthy women at physiologically typical dietary intakes. J. Nutr. 2003, 133, 1027-1035.
14. Liu, Y.; Hu, M. Absorption and metabolism of flavonoids in the Caco-2 cell culture model and a perfused rat intestinal model. Drug Metab. Dispos. 2002, 31, 370-377.
15. Jeong, E.J.; Lin, H.; Hu, M. Disposition mechanisms of raloxifene in the human intestinal Caco-2 model. J. Pharmacol. Exp. Ther. 2004, 310, 376-385.
16. Kemp, D.C.; Fan, P.W.; Stevens, J.C. Charavterization of raloxifene glucuronidation in vitro: Contribution of intestinal metabolism to presysystemic clearance. Drug Metab. Dispos. 2002, 30, 694-700.
17. Chen, J.; Lin, H.; Hu, M. Metabolism of flavonoids via enteric recycling: Role of intestinal disposition. J. Pharmcol. Exp. Ther. 2003, 304, 1228-1235. (Pubitemid 36254436)
18. Chang, J.H.; Kochansky, C.J.; Shou, M. The Role of P-glycoprotein in the Bioactivation of Raloxifene. Drug Metab. Dispos. 2006, 34, 2073-2078.
19. Hu, M.; Chen, J.; Lin, H. Metabolism of flavonoids via enteric recycling: Mechanistic studies of disposition of apigenin in the Caco-2 cell culture model. J. Pharmacol. Exp.Ther. 2003, 307, 314-321.
20. Liu, Y.; Hu, M. Absorption and Metabolism of Flavonoids in the Caco-2 Cell Culture Model and a Perfused Rat Intestinal Model. Drug Metab. Dispos. 2002, 30, 370-377.
21. Kim, A.R.; Lim, S.J.; Lee, B.J. Metabolic inhibition and kinetics of raloxifene by pharmaceutical excipients in human liver microsomes. Int. J. Pharm. 2009, 23, 37-44.
22. Pathak, S.M.; Udupa, N. Pre-clinical Evidence of Enhanced Oral Bioavailability of the PGlycoprotein Substrate Talinolol in Combination with Morin. Biopharm. Drug Dispos. 2010, 31, 202-214.