Separate evaluation of intestinal and hepatic metabolism of three benzodiazepines in rats with cannulated portal and jugular veins: comparison with the profile in non-cannulated mice

References

• Amidon GL, Sinko PJ, Fleisher D. (1988). Estimating human oral fraction dose absorbed: a correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds. Pharmaceut Res 5:651–4.
   PubMed Web of Science ®Google Scholar
• Artursson P, Karlsson J. (1991). Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem Biophys Res Comm 175:880–5.
   PubMed Web of Science ®Google Scholar
• Avdeef A, Nielsen P, Tsinman O. (2004). PAMPA − a drug absorption in vitro model. 11. Matching the in vivo aqueous boundary layer by individual-well stirring in microtiter plates. Eur J Pharmaceut Chem 22:365–74.
   Google Scholar
• Bailey DG, Spence JD, Munoz C, Arnold JM. (1991). Interaction of citrus juices with felodipine and nifedipine. Lancet 2:268–9.
   Google Scholar
• Benet LZ, Izumi T, Zhang Y. Silverman JA, Wacher VJ. (1999). Intestinal MDR transport proteins and cytochrome P450 enzymes as barriers to oral drug delivery. J Contr Rel 1:25–31.
   Google Scholar
• Berggren S, Gall C, Wollnitz N, Ekelund M, Karlbom U, Hoogstraate J, Schrenk D, Lennernäs H. (2007). Gene and protein expression of P-glycoprotein, MRP1, MRP2, and CYP3A4 in the small and large human intestine. Mol Pharmaceut 4:252–7.
   PubMed Web of Science ®Google Scholar
• Cao X, Gibbs ST, Fang L, Miller HA, Landowski CP, Shin HC, Lennernäs H, Zhong Y, Amidon GL, Yu LX, Sun D. (2006). Why is it challenging to predict intestinal drug absorption and oral bioavailability in human using rat model. Pharmaceut Res 23:1675–86.
   PubMed Web of Science ®Google Scholar
• Charpentier KP, Von Moltke LL, Poku JW, Harmatz JS, Shader RI, Greenblatt DJ. (1997). Alprazolam hydroxylation by mouse liver microsomes in vitro: The effect of age and phenobarbital induction. Pharmaceut Drug Disposit 18:139–49.
   PubMedGoogle Scholar
• Cummins CL, Wu C-Y, Benet LZ. (2002). Sex-related differences in the clearance of cytochrome P450 3A4 substrates may be caused by P-glycoprotein. Clin Pharmacol Ther 72:474–89.
   PubMed Web of Science ®Google Scholar
• Dahan A, Amidon GL. (2009). Segmental dependent transport of low permeability compounds along the small intestine due to P-glycoprotein: the role of efflux transport in the oral absorption of BCS class III drugs. Mol Pharmaceut 6:19–28.
   PubMed Web of Science ®Google Scholar
• Davies B, Morris T. (1993). Physiological parameters in laboratory animals and humans. Pharmaceut Res 10:1093–5.
   PubMed Web of Science ®Google Scholar
• Ekins S, Waller CL, Swaan PW, Cruciani G, Wrighton SA, Wikel JH. (2000). Progress in predicting human ADME parameters in silico. J Pharmacol Toxicol Meth 44:251–72.
   PubMed Web of Science ®Google Scholar
• Frank R, Hargreaves R. (2003). Clinical biomarkers in drug discovery and development. Nature 2:566–80.
   Web of Science ®Google Scholar
• Fujieda Y, Yamaoka K, Ito T, Nakagawa T. (1996). Local absorption kinetics of levofloxacin from intestinal tract into portal vein in conscious rat using portal–venous concentration difference. Pharmaceut Res 13:1201–4.
   PubMed Web of Science ®Google Scholar
• Galetin A, Houston JB. (2006). Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: impact on prediction of first-pass metabolism. J Pharmacol Exp Ther 318:1220–9.
   PubMed Web of Science ®Google Scholar
• Goho C. (2001). Oral midazolam–grapefruit juice drug interaction. Pediatr Dent 23:365–6.
   PubMedGoogle Scholar
• Hoffman DJ, Seifert T, Borre A, Nellans HN. (1995). Method to estimate the rate and extent of intestinal absorption in conscious rats using an absorption probe and portal blood sampling. Pharmaceut Res 12:889–94.
   PubMed Web of Science ®Google Scholar
• Ito K, Kusuhara H, Suguyama Y. (1999). Effects of intestinal CYP3A4 and P-glycoprotein on oral drug absorption − theoretical approach. Pharmaceut Res 16:225–31.
   PubMed Web of Science ®Google Scholar
• Jones HM, Houston JB. (2004). Substrate depletion approach for determining in vitro metabolic clearance: time dependencies in hepatocyte and microsomal incubations. Drug Metab Disposit 352:973–82.
   Google Scholar
• Kanazu T, Okamura N, Yamaguchi Y, Baba T, Koike M. (2005). Assessment of the hepatic and intestinal first-pass metabolism of midazolam in a CYP3A drug–drug interaction model rats. Xenobiotica 35:305–17.
   PubMed Web of Science ®Google Scholar
• Kato M. (2008). Intestinal first-pass metabolism of CYP3A4 substrates. Drug Metab Pharmacokinet 23:87–94.
   PubMed Web of Science ®Google Scholar
• Klippert P, Borm P. Noordhoek J. (1982). Prediction of intestinal first-pass effect of phenacetin in the rat from enzyme kinetic data-correlation with in vivo data using mucosal blood flow. Biochem Pharmacol 31:2545–8.
   PubMed Web of Science ®Google Scholar
• Kupferschmidt HH, Ha HR, Ziegler WH, Meier PJ, Krähenbühl S. (1995). Interaction between grapefruit juice and midazolam in humans. Clin Pharmacol Ther 58:20–8.
   PubMed Web of Science ®Google Scholar
• Lennernäs H, Ahrenstedt O, Hallgren R, Knutson L, Ryde M, Paalzow LK. (1992). Regional jejunal perfusion, a new in vivo approach to study oral drug absorption in man. Pharmaceut Res 9:1243–51.
   PubMed Web of Science ®Google Scholar
• Moriwaki T, Yasui H, Yamamoto A. (2003). A recirculatory model with enterohapatic circulation by measuring portal and systemic blood concentration difference. J Pharmacokinet Pharmacodyn 30:119–44.
   PubMedGoogle Scholar
• Murakami T, Nakanishi M, Yoshimori T, Okanura N, Norikura R, Mizojiri K. (2003). Separate assessment of intestinal and hepatic first-pass effects using a rat model with double cannulation of the portal and jugular veins. Drug Metab Pharmacokinet 18:252–60.
   PubMedGoogle Scholar
• Nakao K, Fujiwara M, Shimizu R, Akamatsu M. (2009). QSAR application for the prediction of compound permeability with in silico descriptors in practical use. J Comput-Aid Mol Des 23:309–19.
   PubMed Web of Science ®Google Scholar
• Odou P, Ferrari N, Barthelemy C, Brique S, Lheemitte M, Vincent A, Libersa C, Robert H. (2005). Grapefruit juice–nifedipine interaction: possible involvement of several mechanisms. J Clin Pharm Ther 30:153–8.
   PubMed Web of Science ®Google Scholar
• Oosterdorp RL, Beijnen JH, Shellens JHM. (2009). The biological and clinical role of drug transporters at the intestinal barrier. Cancer Treatment Reviews 35:137–147.
   PubMedGoogle Scholar
• Paine MF, Criss AB, Watkins PB. (2005). Two major grapefruit juice components differ in time to onset of intestinal CYP3A4 inhibition. J Pharmacol Exp Ther 312:1151–60.
   PubMed Web of Science ®Google Scholar
• Pal D, Mitra AK. (2006). MDR- and CYP3A4-mediated drug–drug interactions. J Neuroimm Pharmacol 1:323–39.
   PubMed Web of Science ®Google Scholar
• Pelkonen O, Turpeinen M, Hakkola J, Honkakoski P, Hukkanen J, Raunio H. (2008). Inhibition and induction of human cytochrome P450 enzymes. Current status. Arch Toxicol 82:667–715.
   PubMed Web of Science ®Google Scholar
• Perloff MD, Von Moltke LL, Court MH, Kotegawa T, Shader RI, Greenblatt DJ. (2000). Midazolam and triazolam biotransformation in mouse and human liver microsomes: relative contribution of CYP3A and CYP2C isoforms. J Pharmacol Exp Ther 292:618–28.
   PubMed Web of Science ®Google Scholar
• Richardson PD, Withrington PG. (1981). Liver blood flow I. Intrinsic and nervous control of liver blood flow. Gastroenterology 81:159–73.
   PubMed Web of Science ®Google Scholar
• Ruiz-Garcia A, Bermejo M, Moss A, Casabo VG. (2008). Pharmacokinetics in drug discovery. J Pharmaceut Sci 97:654–90.
   PubMed Web of Science ®Google Scholar
• Schmiedlin-Ren P, Edwards DJ, Fitzsimmons ME, He K, Lown KS, Woster PM, Rahman A, Thummel KE, Fisher JM, Hollenberg PF, Watkins PB. (1997). Mechanisms of enhanced oral availability of CYP3A4 substrates by grapefruit constituents. Decreased enterocyte CYP3A4 concentration and mechanism-based inactivation by furanocoumarins. Drug Metab Disposit 25:1228–33.
   PubMed Web of Science ®Google Scholar
• Shirasaka Y, Sakane T, Yamashita S. (2008). Effect of P-glycoprotein expression levels on the concentration-dependent permeability of drugs to the cell membrane. J Pharmaceut Sci 97:553–65.
   PubMed Web of Science ®Google Scholar
• Suzuki H, Sugiyama Y. (2000). Role of metabolic enzymes and efflux transporters in the absorption of drugs from the small intestine. Eur J Pharmaceut Sci 12:3–12.
   PubMed Web of Science ®Google Scholar
• Tabata K, Yamaoka K, Fukuyama T, Nakagawa T. (1995). Evaluation of intestinal absorption into the portal system in enterohepatic circulation by measuring the difference in portal–venous blood concentrations of diclofenac. Pharmaceut Res 12:880–3.
   PubMed Web of Science ®Google Scholar
• Troutman MD, Thakker DR. (2003). Novel experimental parameters to quantify the modulation of absorptive and secretory transport of compounds by P-glycoprotein in cell culture models of intestinal epithelium. Pharmaceut Res 20:1210–24.
   PubMed Web of Science ®Google Scholar
• Van Herwaaden AE, van Watershoot RA, Schinkel AH. (2009). How important is intestinal cytochrome P450 3A metabolism? Trend Pharmacol Sci 30:223–7.
   PubMedGoogle Scholar
• Wacher VJ, Salphati L, Benet LZ. (2001). Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv Drug Del Rev 1:89–102.
   Google Scholar
• Walsky RL, Boldt SE. (2008). In vitro cytochrome P450 inhibition and induction. Curr Drug Metab 9:928–39.
   PubMed Web of Science ®Google Scholar
• Willmann S, Schmitt W, Keldenich J, Dressman JB. (2003). A physiologic model for simulating gastrointestinal flow and drug absorption in rats. Pharmaceut Res 20:1766–71.
   PubMed Web of Science ®Google Scholar
• Yamashita F, Hashida M. (2004). In silico approaches for predicting ADME properties of drugs. Drug Metab Pharmacokinet 19:327–38.
   PubMedGoogle Scholar
• Yee S. (1997). In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in man–fact or myth. Pharmaceut Res 14:763–6.
   PubMed Web of Science ®Google Scholar
• Zhang Q, Dunbar D, Ostrowska A, Zeisloft S, Yang J, Kaminsky LS. (2007). Characterization of human small intestinal cytochromes P-450. Drug Metab Disposit 27:804–9.
   Google Scholar
• Zhou SF. (2008). Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica 38:802–32.
   PubMed Web of Science ®Google Scholar