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Volumn 368, Issue 1-2, 2009, Pages 37-44

Metabolic inhibition and kinetics of raloxifene by pharmaceutical excipients in human liver microsomes

Author keywords

Inhibition of hepatic metabolism; Metabolic factors; Metabolic kinetics; Pharmaceutical excipients; Raloxifene

Indexed keywords

CREMOPHOR; DODECYL SULFATE SODIUM; GELUCIRE; MACROGOL 6000; POLIDOCANOL; POLOXAMER; POLYOXYETHYLENE OLEYL ETHER; POLYSORBATE 80; POVIDONE DERIVATIVE; RALOXIFENE; TWEEN; UNCLASSIFIED DRUG; URIDINE DIPHOSPHATE GLUCURONIC ACID;

EID: 58949099347     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ijpharm.2008.09.049     Document Type: Article
Times cited : (23)

References (30)
  • 2
    • 0030430033 scopus 로고    scopus 로고
    • Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes
    • Bourrié M., Meunier V., Berger Y., and Fabre G. Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes. J. Pharmacol. Exp. Ther. 277 (1996) 321-332
    • (1996) J. Pharmacol. Exp. Ther. , vol.277 , pp. 321-332
    • Bourrié, M.1    Meunier, V.2    Berger, Y.3    Fabre, G.4
  • 3
    • 0742324810 scopus 로고    scopus 로고
    • In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam
    • Bravo Gonzalez R.C., Huwyler J., Boess F., Walter I., and Bittner B. In vitro investigation on the impact of the surface-active excipients Cremophor EL, Tween 80 and Solutol HS 15 on the metabolism of midazolam. Biopharm. Drug Dispos. 25 (2004) 37-49
    • (2004) Biopharm. Drug Dispos. , vol.25 , pp. 37-49
    • Bravo Gonzalez, R.C.1    Huwyler, J.2    Boess, F.3    Walter, I.4    Bittner, B.5
  • 4
    • 33747041999 scopus 로고    scopus 로고
    • Developments in the pharmacotherapeutic management of osteoporosis
    • Close P., Neuprez A., and Reginster J.Y. Developments in the pharmacotherapeutic management of osteoporosis. Expert Opin. Pharmacother. 7 (2006) 1603-1615
    • (2006) Expert Opin. Pharmacother. , vol.7 , pp. 1603-1615
    • Close, P.1    Neuprez, A.2    Reginster, J.Y.3
  • 5
    • 2442671307 scopus 로고    scopus 로고
    • Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo
    • Cornaire G., Woodley J., Hermann P., Cloarec A., Arellano C., and Houin G. Impact of excipients on the absorption of P-glycoprotein substrates in vitro and in vivo. Int. J. Pharm. 278 (2004) 119-131
    • (2004) Int. J. Pharm. , vol.278 , pp. 119-131
    • Cornaire, G.1    Woodley, J.2    Hermann, P.3    Cloarec, A.4    Arellano, C.5    Houin, G.6
  • 6
    • 4744341196 scopus 로고    scopus 로고
    • Interaction of non-ionic surfactants with hepatic CYP in Prochilodus scrofa
    • da Silva M.E., and Meirelles N.C. Interaction of non-ionic surfactants with hepatic CYP in Prochilodus scrofa. Toxicol. In vitro 18 (2004) 859-867
    • (2004) Toxicol. In vitro , vol.18 , pp. 859-867
    • da Silva, M.E.1    Meirelles, N.C.2
  • 7
    • 0029962074 scopus 로고    scopus 로고
    • Glucuronidation of amines and hydroxylated xenobiotics and endobiotics catalyzed by expressed human UGT1. 4 protein
    • Green M.D., and Tephly T.R. Glucuronidation of amines and hydroxylated xenobiotics and endobiotics catalyzed by expressed human UGT1. 4 protein. Drug Metab. Dispos. 24 (1996) 356-363
    • (1996) Drug Metab. Dispos. , vol.24 , pp. 356-363
    • Green, M.D.1    Tephly, T.R.2
  • 9
    • 0019772163 scopus 로고
    • Effects of detergents and organic solvents on rat liver microsomal UDP-glucuronosyltransferase activity towards phenolic substrates
    • Illing H.P., and House E.S. Effects of detergents and organic solvents on rat liver microsomal UDP-glucuronosyltransferase activity towards phenolic substrates. Xenobiotic 11 (1981) 709-718
    • (1981) Xenobiotic , vol.11 , pp. 709-718
    • Illing, H.P.1    House, E.S.2
  • 10
    • 0035994868 scopus 로고    scopus 로고
    • Excipient crystallinity and its protein-structure-stabilizing effect during freeze-drying
    • Izutsu K., and Kojima S. Excipient crystallinity and its protein-structure-stabilizing effect during freeze-drying. J. Pharm. Pharmacol. 54 (2002) 1033-1039
    • (2002) J. Pharm. Pharmacol. , vol.54 , pp. 1033-1039
    • Izutsu, K.1    Kojima, S.2
  • 11
    • 3042681890 scopus 로고    scopus 로고
    • Disposition mechanisms of raloxifene in the human intestinal Caco-2 model
    • Jeong E.J., Lin H., and Hu M. Disposition mechanisms of raloxifene in the human intestinal Caco-2 model. J. Pharmacol. Exp. Ther. 310 (2004) 376-385
    • (2004) J. Pharmacol. Exp. Ther. , vol.310 , pp. 376-385
    • Jeong, E.J.1    Lin, H.2    Hu, M.3
  • 12
    • 0036453655 scopus 로고    scopus 로고
    • An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine
    • Johnson B.M., Charman W.N., and Porter C.J. An in vitro examination of the impact of polyethylene glycol 400, Pluronic P85, and vitamin E d-alpha-tocopheryl polyethylene glycol 1000 succinate on P-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine. AAPS PharmSci 4 (2002) E40
    • (2002) AAPS PharmSci , vol.4
    • Johnson, B.M.1    Charman, W.N.2    Porter, C.J.3
  • 13
    • 0032586721 scopus 로고    scopus 로고
    • i in a competitive enzyme-inhibition model: comparisons among three methods of data analysis
    • i in a competitive enzyme-inhibition model: comparisons among three methods of data analysis. Drug Metab. Dispos. 27 (1999) 756-762
    • (1999) Drug Metab. Dispos. , vol.27 , pp. 756-762
    • Kakkar, T.1    Boxenbaum, H.2    Mayersohn, M.3
  • 14
    • 0036266936 scopus 로고    scopus 로고
    • Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance
    • Kemp D.C., Fan P.W., and Stevens J.C. Characterization of raloxifene glucuronidation in vitro: contribution of intestinal metabolism to presystemic clearance. Drug Metab. Dispos. 30 (2002) 694-700
    • (2002) Drug Metab. Dispos. , vol.30 , pp. 694-700
    • Kemp, D.C.1    Fan, P.W.2    Stevens, J.C.3
  • 15
    • 0037423299 scopus 로고    scopus 로고
    • Expression and characterization of recombinant human UDP-glucuronosyltransferases (UGTs). UGT1A9 is more resistant to detergent inhibition than other UGTs and was purified as an active dimeric enzyme
    • Kurkela M., García-Horsman J.A., Luukkanen L., Mörsky S., Taskinen J., Baumann M., Kostiainen R., Hirvonen J., and Finel M. Expression and characterization of recombinant human UDP-glucuronosyltransferases (UGTs). UGT1A9 is more resistant to detergent inhibition than other UGTs and was purified as an active dimeric enzyme. J. Biol. Chem. 278 (2003) 3536-3544
    • (2003) J. Biol. Chem. , vol.278 , pp. 3536-3544
    • Kurkela, M.1    García-Horsman, J.A.2    Luukkanen, L.3    Mörsky, S.4    Taskinen, J.5    Baumann, M.6    Kostiainen, R.7    Hirvonen, J.8    Finel, M.9
  • 16
    • 0021674554 scopus 로고
    • Disposition and metabolism of a new benzothiophene antiestrogen in rats, dogs and monkeys
    • Lindstrom T.D., Whitaker N.G., and Whitaker G.W. Disposition and metabolism of a new benzothiophene antiestrogen in rats, dogs and monkeys. Xenobiotica 14 (1984) 841-847
    • (1984) Xenobiotica , vol.14 , pp. 841-847
    • Lindstrom, T.D.1    Whitaker, N.G.2    Whitaker, G.W.3
  • 17
    • 0030778114 scopus 로고    scopus 로고
    • Structure and function of uridine diphosphate glucuronosyltransferases
    • Meech R., and Mackenzie P.I. Structure and function of uridine diphosphate glucuronosyltransferases. Clin. Exp. Pharmacol. Physiol. 24 (1997) 907-915
    • (1997) Clin. Exp. Pharmacol. Physiol. , vol.24 , pp. 907-915
    • Meech, R.1    Mackenzie, P.I.2
  • 18
    • 0037255847 scopus 로고    scopus 로고
    • Pharmacokinetics of selective estrogen receptor modulators
    • Morello K.C., Wurz G.T., and DeGregorio M.W. Pharmacokinetics of selective estrogen receptor modulators. Clin. Pharmacokinet. 42 (2003) 361-372
    • (2003) Clin. Pharmacokinet. , vol.42 , pp. 361-372
    • Morello, K.C.1    Wurz, G.T.2    DeGregorio, M.W.3
  • 19
    • 38349165563 scopus 로고    scopus 로고
    • Effect of pharmaceutical excipients upon aqueous stability of rabeprazole sodium
    • Ren S., Park M.-J., Sah H., and Lee B.-J. Effect of pharmaceutical excipients upon aqueous stability of rabeprazole sodium. Int. J. Pharm. 350 (2008) 197-204
    • (2008) Int. J. Pharm. , vol.350 , pp. 197-204
    • Ren, S.1    Park, M.-J.2    Sah, H.3    Lee, B.-J.4
  • 20
    • 46249095516 scopus 로고    scopus 로고
    • In vitro metabolic stability of moisture-sensitive rabeprazole in human liver microsomes and its modulation by pharmaceutical excipients
    • Ren S., Park M.-J., Kim A., and Lee B.-J. In vitro metabolic stability of moisture-sensitive rabeprazole in human liver microsomes and its modulation by pharmaceutical excipients. Arch. Pharm. Res. 31 (2008) 406-413
    • (2008) Arch. Pharm. Res. , vol.31 , pp. 406-413
    • Ren, S.1    Park, M.-J.2    Kim, A.3    Lee, B.-J.4
  • 21
    • 0035478758 scopus 로고    scopus 로고
    • Chitosan and its derivatives as intestinal absorption enhancers
    • Thanou M., Verhoef J.C., and Junginger H.E. Chitosan and its derivatives as intestinal absorption enhancers. Adv. Drug Deliv. Rev. 50 (2001) S91-101
    • (2001) Adv. Drug Deliv. Rev. , vol.50
    • Thanou, M.1    Verhoef, J.C.2    Junginger, H.E.3
  • 22
    • 0022378446 scopus 로고
    • UDP-glucuronosyltransferase(s) activities towards natural substrates in rat liver microsomes. Kinetic properties and influence of triton X-100 activation
    • Thomassin J., Boutin J.A., and Siest G. UDP-glucuronosyltransferase(s) activities towards natural substrates in rat liver microsomes. Kinetic properties and influence of triton X-100 activation. Pharmacol. Res. Commun. 17 (1985) 1005-1015
    • (1985) Pharmacol. Res. Commun. , vol.17 , pp. 1005-1015
    • Thomassin, J.1    Boutin, J.A.2    Siest, G.3
  • 24
    • 23144451233 scopus 로고    scopus 로고
    • Effect of hydroxypropyl beta-cyclodextrin complexation on aqueous solubility, stability, and corneal permeation of acyl ester prodrugs of ganciclovir
    • Tirucherai G.S., and Mitra A.K. Effect of hydroxypropyl beta-cyclodextrin complexation on aqueous solubility, stability, and corneal permeation of acyl ester prodrugs of ganciclovir. AAPS PharmSciTech 4 (2003) E45
    • (2003) AAPS PharmSciTech , vol.4
    • Tirucherai, G.S.1    Mitra, A.K.2
  • 25
    • 0031808472 scopus 로고    scopus 로고
    • Glucuronidation of 3′-azido-3′-deoxythymidine (zidovudine) by human liver microsomes: relevance to clinical pharmacokinetic interactions with atovaquone, fluconazole, methadone, and valproic acid
    • Trapnell C.B., Klecker R.W., Jamis-Dow C., and Collins J.M. Glucuronidation of 3′-azido-3′-deoxythymidine (zidovudine) by human liver microsomes: relevance to clinical pharmacokinetic interactions with atovaquone, fluconazole, methadone, and valproic acid. Antimicrob. Agents Chemother. 42 (1998) 1592-1596
    • (1998) Antimicrob. Agents Chemother. , vol.42 , pp. 1592-1596
    • Trapnell, C.B.1    Klecker, R.W.2    Jamis-Dow, C.3    Collins, J.M.4
  • 26
    • 0034128936 scopus 로고    scopus 로고
    • Human UDP-glucuronosyltransferases: metabolism, expression, and disease
    • Tukey R.H., and Strassburg C.P. Human UDP-glucuronosyltransferases: metabolism, expression, and disease. Annu. Rev. Pharmacol. Toxicol. 40 (2000) 581-616
    • (2000) Annu. Rev. Pharmacol. Toxicol. , vol.40 , pp. 581-616
    • Tukey, R.H.1    Strassburg, C.P.2
  • 27
    • 0033588485 scopus 로고    scopus 로고
    • In vitro inhibition of simvastatin metabolism in rat and human liver by naringenin
    • Ubeaud G., Hagenbach J., Vandenschrieck S., Jung L., and Koffel J.C. In vitro inhibition of simvastatin metabolism in rat and human liver by naringenin. Life Sci. 65 (1999) 1403-1412
    • (1999) Life Sci. , vol.65 , pp. 1403-1412
    • Ubeaud, G.1    Hagenbach, J.2    Vandenschrieck, S.3    Jung, L.4    Koffel, J.C.5
  • 28
    • 0035668586 scopus 로고    scopus 로고
    • Effect of carrier excipient and processing on stability of indorenate hydrochloride/excipient mixtures
    • Villalobos-Hernandez J.R., and Villafuerte-Robles L. Effect of carrier excipient and processing on stability of indorenate hydrochloride/excipient mixtures. Pharm. Dev. Technol. 6 (2001) 551-561
    • (2001) Pharm. Dev. Technol. , vol.6 , pp. 551-561
    • Villalobos-Hernandez, J.R.1    Villafuerte-Robles, L.2
  • 29
    • 0026644535 scopus 로고
    • Drug metabolism by cytochromes P450 in the liver and small bowel. Gastroenterol
    • Watkins P.B. Drug metabolism by cytochromes P450 in the liver and small bowel. Gastroenterol. Clin. North Am. 21 (1992) 511-526
    • (1992) Clin. North Am. , vol.21 , pp. 511-526
    • Watkins, P.B.1
  • 30
    • 33644842869 scopus 로고    scopus 로고
    • Integration of hepatic drug transporters and phase II metabolizing enzymes: mechanisms of hepatic excretion of sulfate, glucuronide, and glutathione metabolites
    • Zamek-Gliszczynski M.J., Hoffmaster K.A., Nezasa K., Tallman M.N., and Brouwer K.L. Integration of hepatic drug transporters and phase II metabolizing enzymes: mechanisms of hepatic excretion of sulfate, glucuronide, and glutathione metabolites. Eur. J. Pharm. Sci. 27 (2006) 447-486
    • (2006) Eur. J. Pharm. Sci. , vol.27 , pp. 447-486
    • Zamek-Gliszczynski, M.J.1    Hoffmaster, K.A.2    Nezasa, K.3    Tallman, M.N.4    Brouwer, K.L.5


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