메뉴 건너뛰기




Volumn 35, Issue 8, 2007, Pages 1275-1284

Asymmetric intestinal first-pass metabolism causes minimal oral bioavailability of midazolam in cynomolgus monkey

Author keywords

[No Author keywords available]

Indexed keywords

4 HYDROXYMIDAZOLAM; ALPHA HYDROXYMIDAZOLAM; DRUG METABOLITE; MIDAZOLAM; UNCLASSIFIED DRUG;

EID: 34547209778     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.106.013037     Document Type: Article
Times cited : (38)

References (38)
  • 1
    • 19444375003 scopus 로고    scopus 로고
    • Intestinal expression and metabolic activity of the CYP3A subfamily in female rats
    • Aiba T, Yoshinaga M, Ishida K, Takehara Y, and Hashimoto Y (2005) Intestinal expression and metabolic activity of the CYP3A subfamily in female rats. Biol Pharm Bull 28:311-315.
    • (2005) Biol Pharm Bull , vol.28 , pp. 311-315
    • Aiba, T.1    Yoshinaga, M.2    Ishida, K.3    Takehara, Y.4    Hashimoto, Y.5
  • 2
    • 0035478419 scopus 로고    scopus 로고
    • The drug efflux-metabolism alliance: Biochemical aspects
    • Benet LZ and Cummins CL (2001) The drug efflux-metabolism alliance: biochemical aspects. Adv Drug Deliv Rev 50 (Suppl 1):S3-S11.
    • (2001) Adv Drug Deliv Rev , vol.50 , Issue.SUPPL. 1
    • Benet, L.Z.1    Cummins, C.L.2
  • 3
    • 2442719906 scopus 로고    scopus 로고
    • Unmasking the dynamic interplay between efflux transporters and metabolic enzymes
    • Benet LZ, Cummins CL, and Wu CY (2004) Unmasking the dynamic interplay between efflux transporters and metabolic enzymes. Int J Pharm 277:3-9.
    • (2004) Int J Pharm , vol.277 , pp. 3-9
    • Benet, L.Z.1    Cummins, C.L.2    Wu, C.Y.3
  • 4
    • 0017184389 scopus 로고
    • A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
    • Bradford MM (1976) A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal Biochem 72:248-254.
    • (1976) Anal Biochem , vol.72 , pp. 248-254
    • Bradford, M.M.1
  • 5
    • 0036296060 scopus 로고    scopus 로고
    • Comparison of oral absorption and bioavailability of drugs between monkey and human
    • Chiou WL and Buehler PW (2002) Comparison of oral absorption and bioavailability of drugs between monkey and human. Pharm Res (N Y) 19:868-874.
    • (2002) Pharm Res (N Y) , vol.19 , pp. 868-874
    • Chiou, W.L.1    Buehler, P.W.2
  • 6
    • 0036175307 scopus 로고    scopus 로고
    • Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4
    • Cummins CL, Jacobsen W, and Benet LZ (2002) Unmasking the dynamic interplay between intestinal P-glycoprotein and CYP3A4. J Pharmacol Exp Ther 300:1036-1045.
    • (2002) J Pharmacol Exp Ther , vol.300 , pp. 1036-1045
    • Cummins, C.L.1    Jacobsen, W.2    Benet, L.Z.3
  • 7
    • 0345866819 scopus 로고    scopus 로고
    • CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: Studies with sirolimus and midazolam
    • Cummins CL, Jacobsen W, Christians U, and Benet LZ (2004) CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam. J Pharmacol Exp Ther 308:143-155.
    • (2004) J Pharmacol Exp Ther , vol.308 , pp. 143-155
    • Cummins, C.L.1    Jacobsen, W.2    Christians, U.3    Benet, L.Z.4
  • 8
    • 2342644210 scopus 로고    scopus 로고
    • Molecular and integrative physiology of intestinal peptide transport
    • Daniel H (2004) Molecular and integrative physiology of intestinal peptide transport. Annu Rev Physiol 66:361-384.
    • (2004) Annu Rev Physiol , vol.66 , pp. 361-384
    • Daniel, H.1
  • 9
    • 0027275566 scopus 로고
    • Physiological parameters in laboratory animals and humans
    • Davies B and Morris T (1993) Physiological parameters in laboratory animals and humans. Pharm Res (N Y) 10:1093-1095.
    • (1993) Pharm Res (N Y) , vol.10 , pp. 1093-1095
    • Davies, B.1    Morris, T.2
  • 11
    • 0029790347 scopus 로고    scopus 로고
    • Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cDNA-expressed human cytochrome P450
    • Ghosal A, Satoh H, Thomas PE, Bush E, and Moore D (1996) Inhibition and kinetics of cytochrome P4503A activity in microsomes from rat, human, and cDNA-expressed human cytochrome P450. Drug Metab Dispos 24:940-947.
    • (1996) Drug Metab Dispos , vol.24 , pp. 940-947
    • Ghosal, A.1    Satoh, H.2    Thomas, P.E.3    Bush, E.4    Moore, D.5
  • 13
    • 0032977985 scopus 로고    scopus 로고
    • Dose-dependent intestinal and hepatic first-pass metabolism of midazolam, a cytochrome P450 3A substrate with differently modulated enzyme activity in rats
    • Higashikawa F, Murakami T, Kaneda T, Kato A, and Takano M (1999) Dose-dependent intestinal and hepatic first-pass metabolism of midazolam, a cytochrome P450 3A substrate with differently modulated enzyme activity in rats. J Pharm Pharmacol 51:67-72.
    • (1999) J Pharm Pharmacol , vol.51 , pp. 67-72
    • Higashikawa, F.1    Murakami, T.2    Kaneda, T.3    Kato, A.4    Takano, M.5
  • 14
    • 0041856526 scopus 로고    scopus 로고
    • Application of compartmental modeling to an examination of in vitro intestinal permeability data: Assessing the impact of tissue uptake, P-glycoprotein, and CYP3A
    • Johnson BM, Charman WN, and Porter CJ (2003) Application of compartmental modeling to an examination of in vitro intestinal permeability data: assessing the impact of tissue uptake, P-glycoprotein, and CYP3A. Drug Metab Dispos 31:1151-1160.
    • (2003) Drug Metab Dispos , vol.31 , pp. 1151-1160
    • Johnson, B.M.1    Charman, W.N.2    Porter, C.J.3
  • 15
    • 3142628354 scopus 로고    scopus 로고
    • Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. I: Evaluation of cynomolgus monkeys as surrogates for humans
    • Kanazu T, Yamaguchi Y, Okamura N, Baba T, and Koike M (2004) Model for the drug-drug interaction responsible for CYP3A enzyme inhibition. I: evaluation of cynomolgus monkeys as surrogates for humans. Xenobiotica 34:391-402.
    • (2004) Xenobiotica , vol.34 , pp. 391-402
    • Kanazu, T.1    Yamaguchi, Y.2    Okamura, N.3    Baba, T.4    Koike, M.5
  • 16
    • 85009583484 scopus 로고    scopus 로고
    • Intestinal absorption of drugs mediated by drug transporters: Mechanisms and regulation
    • Katsura T and Inui K (2003) Intestinal absorption of drugs mediated by drug transporters: mechanisms and regulation. Drug Metab Pharmacokinet 18:1-15.
    • (2003) Drug Metab Pharmacokinet , vol.18 , pp. 1-15
    • Katsura, T.1    Inui, K.2
  • 18
    • 0026464616 scopus 로고
    • Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes
    • Kolars JC, Schmiedlin-Ren P, Schuetz JD, Fang C, and Watkins PB (1992b) Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes. J Clin Invest 90:1871-1878.
    • (1992) J Clin Invest , vol.90 , pp. 1871-1878
    • Kolars, J.C.1    Schmiedlin-Ren, P.2    Schuetz, J.D.3    Fang, C.4    Watkins, P.B.5
  • 19
    • 0029898197 scopus 로고    scopus 로고
    • Pharmacokinetics and bioavailability of midazolam after intravenous, subcutaneous, intraperitoneal and oral administration under a chronic food-limited regimen: Relating DRL performance to pharmacokinetics
    • Lau CE, Ma F, Wang Y, and Smith C (1996) Pharmacokinetics and bioavailability of midazolam after intravenous, subcutaneous, intraperitoneal and oral administration under a chronic food-limited regimen: relating DRL performance to pharmacokinetics. Psychopharmacology (Berl) 126:241-248.
    • (1996) Psychopharmacology (Berl) , vol.126 , pp. 241-248
    • Lau, C.E.1    Ma, F.2    Wang, Y.3    Smith, C.4
  • 20
    • 0036225166 scopus 로고    scopus 로고
    • Intestinal metabolism promotes regional differences in apical uptake of indinavir: Coupled effect of P-glycoprotein and cytochrome P450 3A on indinavir membrane permeability in rat
    • Li LY, Amidon GL, Kim JS, Heimbach T, Kesisoglou F, Topliss JT, and Fleisher D (2002) Intestinal metabolism promotes regional differences in apical uptake of indinavir: coupled effect of P-glycoprotein and cytochrome P450 3A on indinavir membrane permeability in rat. J Pharmacol Exp Ther 301:586-593.
    • (2002) J Pharmacol Exp Ther , vol.301 , pp. 586-593
    • Li, L.Y.1    Amidon, G.L.2    Kim, J.S.3    Heimbach, T.4    Kesisoglou, F.5    Topliss, J.T.6    Fleisher, D.7
  • 24
    • 4043163371 scopus 로고    scopus 로고
    • Transporter-mediated drug delivery: Recent progress and experimental approaches
    • Sai Y and Tsuji A (2004) Transporter-mediated drug delivery: recent progress and experimental approaches. Drug Discov Today 9:712-720.
    • (2004) Drug Discov Today , vol.9 , pp. 712-720
    • Sai, Y.1    Tsuji, A.2
  • 25
    • 33646818650 scopus 로고    scopus 로고
    • Marked species differences in the bioavailability of midazolam in cynomolgus monkeys and humans
    • Sakuda S, Akabane T, and Teramura T (2006) Marked species differences in the bioavailability of midazolam in cynomolgus monkeys and humans. Xenobiotica 36:331-340.
    • (2006) Xenobiotica , vol.36 , pp. 331-340
    • Sakuda, S.1    Akabane, T.2    Teramura, T.3
  • 26
    • 0030959377 scopus 로고    scopus 로고
    • Cytochrome P450-dependent drug oxidation activities in liver microsomes of various animal species including rats, guinea pigs, dogs, monkeys, and humans
    • Shimada T, Mimura M, Inoue K, Nakamura S, Oda H, Ohmori S, and Yamazaki H (1997) Cytochrome P450-dependent drug oxidation activities in liver microsomes of various animal species including rats, guinea pigs, dogs, monkeys, and humans. Arch Toxicol 71:401-408.
    • (1997) Arch Toxicol , vol.71 , pp. 401-408
    • Shimada, T.1    Mimura, M.2    Inoue, K.3    Nakamura, S.4    Oda, H.5    Ohmori, S.6    Yamazaki, H.7
  • 27
    • 0024571757 scopus 로고
    • The absolute oral bioavailability of selected drugs
    • Sietsema WK (1989) The absolute oral bioavailability of selected drugs. Int J Clin Pharmacol Ther Toxicol 27:179-211.
    • (1989) Int J Clin Pharmacol Ther Toxicol , vol.27 , pp. 179-211
    • Sietsema, W.K.1
  • 28
    • 0141569640 scopus 로고    scopus 로고
    • Influence of P-glycoprotein, transfer clearances, and drug binding on intestinal metabolism in Caco-2 cell monolayers or membrane preparations: A theoretical analysis
    • Tam D, Sun H, Pang KS (2003) Influence of P-glycoprotein, transfer clearances, and drug binding on intestinal metabolism in Caco-2 cell monolayers or membrane preparations: a theoretical analysis. Drug Metab Dispos 31:1214-1226.
    • (2003) Drug Metab Dispos , vol.31 , pp. 1214-1226
    • Tam, D.1    Sun, H.2    Pang, K.S.3
  • 29
    • 0030772347 scopus 로고    scopus 로고
    • Nonlinear intestinal absorption of 5-hydroxytryptamine receptor antagonist caused by absorptive and secretory transporters
    • Tamai I, Saheki A, Saitoh R, Sai Y, Yamada I, and Tsuji A (1997) Nonlinear intestinal absorption of 5-hydroxytryptamine receptor antagonist caused by absorptive and secretory transporters. J Pharmacol Exp Ther 283:108-115.
    • (1997) J Pharmacol Exp Ther , vol.283 , pp. 108-115
    • Tamai, I.1    Saheki, A.2    Saitoh, R.3    Sai, Y.4    Yamada, I.5    Tsuji, A.6
  • 30
    • 0029800447 scopus 로고    scopus 로고
    • Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier
    • Terao T, Hisanaga E, Sai Y, Tamai I, and Tsuji A (1996) Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier. J Pharm Pharmacol 48:1083-1089.
    • (1996) J Pharm Pharmacol , vol.48 , pp. 1083-1089
    • Terao, T.1    Hisanaga, E.2    Sai, Y.3    Tamai, I.4    Tsuji, A.5
  • 32
    • 0242585000 scopus 로고    scopus 로고
    • Midazolam exhibits characteristics of a highly permeable P-glycoprotein substrate
    • Tolle-Sander S, Rautio J, Wring S, Polli JW, and Polli JE (2003) Midazolam exhibits characteristics of a highly permeable P-glycoprotein substrate. Pharm Res (N Y) 20:757-764.
    • (2003) Pharm Res (N Y) , vol.20 , pp. 757-764
    • Tolle-Sander, S.1    Rautio, J.2    Wring, S.3    Polli, J.W.4    Polli, J.E.5
  • 33
    • 0029782485 scopus 로고    scopus 로고
    • Carrier-mediated intestinal transport of drugs
    • Tsuji A and Tamai I (1996) Carrier-mediated intestinal transport of drugs. Pharm Res (N Y) 13:963-977.
    • (1996) Pharm Res (N Y) , vol.13 , pp. 963-977
    • Tsuji, A.1    Tamai, I.2
  • 34
    • 20044365460 scopus 로고    scopus 로고
    • Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human
    • Ward KW, Nagilla R, and Jolivette LJ (2005) Comparative evaluation of oral systemic exposure of 56 xenobiotics in rat, dog, monkey and human. Xenobiotica 35:191-210.
    • (2005) Xenobiotica , vol.35 , pp. 191-210
    • Ward, K.W.1    Nagilla, R.2    Jolivette, L.J.3
  • 35
    • 2442680354 scopus 로고    scopus 로고
    • A comprehensive quantitative and qualitative evaluation of extrapolation of intravenous pharmacokinetic parameters from rat, dog, and monkey to humans. I. Clearance
    • Ward KW and Smith BR (2004) A comprehensive quantitative and qualitative evaluation of extrapolation of intravenous pharmacokinetic parameters from rat, dog, and monkey to humans. I. Clearance. Drug Metab Dispos 32:603-611.
    • (2004) Drug Metab Dispos , vol.32 , pp. 603-611
    • Ward, K.W.1    Smith, B.R.2
  • 36
    • 0342762062 scopus 로고    scopus 로고
    • The barrier function of CYP3A4 and P-glycoprotein in the small bowel
    • Watkins PB (1997) The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv Drug Deliv Rev 27:161-170.
    • (1997) Adv Drug Deliv Rev , vol.27 , pp. 161-170
    • Watkins, P.B.1
  • 37
    • 17644380257 scopus 로고    scopus 로고
    • Predicting drug disposition via application of BCS: Transport/ absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system
    • Wu CY and Benet LZ (2005) Predicting drug disposition via application of BCS: transport/ absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm Res (N Y) 22:11-23.
    • (2005) Pharm Res (N Y) , vol.22 , pp. 11-23
    • Wu, C.Y.1    Benet, L.Z.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.