메뉴 건너뛰기




Volumn 43, Issue 4, 2015, Pages 590-602

A new physiologically based pharmacokinetic model for the prediction of gastrointestinal drug absorption: Translocation model

Author keywords

[No Author keywords available]

Indexed keywords

GASTROINTESTINAL AGENT; MIDAZOLAM; DRUG;

EID: 84940045984     PISSN: 00909556     EISSN: 1521009X     Source Type: Journal    
DOI: 10.1124/dmd.114.060038     Document Type: Article
Times cited : (16)

References (51)
  • 1
    • 0035478779 scopus 로고    scopus 로고
    • Predicting the impact of physiological and biochemical processes on oral drug bioavailability
    • Agoram B, Woltosz WS, and Bolger MB (2001) Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Adv Drug Deliv Rev 50(Suppl 1):S41-S67.
    • (2001) Adv Drug Deliv Rev , vol.50 , pp. S41-S67
    • Agoram, B.1    Woltosz, W.S.2    Bolger, M.B.3
  • 2
    • 67049114269 scopus 로고    scopus 로고
    • Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption
    • Badhan R, Penny J, Galetin A, and Houston JB (2009) Methodology for development of a physiological model incorporating CYP3A and P-glycoprotein for the prediction of intestinal drug absorption. J Pharm Sci 98:2180-2197.
    • (2009) J Pharm Sci , vol.98 , pp. 2180-2197
    • Badhan, R.1    Penny, J.2    Galetin, A.3    Houston, J.B.4
  • 3
    • 84862316790 scopus 로고    scopus 로고
    • A semimechanistic modeling strategy to link in vitro and in vivo drug release for modified release formulations
    • Bergstrand M, Söderlind E, Eriksson UG, Weitschies W, and Karlsson MO (2012) A semimechanistic modeling strategy to link in vitro and in vivo drug release for modified release formulations. Pharm Res 29:695-706.
    • (2012) Pharm Res , vol.29 , pp. 695-706
    • Bergstrand, M.1    Söderlind, E.2    Eriksson, U.G.3    Weitschies, W.4    Karlsson, M.O.5
  • 4
    • 67650581753 scopus 로고    scopus 로고
    • Mechanistic modeling of a magnetic marker monitoring study linking gastrointestinal tablet transit, in vivo drug release, and pharmacokinetics
    • Bergstrand M, Söderlind E, Weitschies W, and Karlsson MO (2009) Mechanistic modeling of a magnetic marker monitoring study linking gastrointestinal tablet transit, in vivo drug release, and pharmacokinetics. Clin Pharmacol Ther 86:77-83.
    • (2009) Clin Pharmacol Ther , vol.86 , pp. 77-83
    • Bergstrand, M.1    Söderlind, E.2    Weitschies, W.3    Karlsson, M.O.4
  • 5
    • 68249144520 scopus 로고    scopus 로고
    • Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine
    • Bolger MB, Lukacova V, and Woltosz WS (2009) Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine. AAPS J 11:353-363.
    • (2009) AAPS J , vol.11 , pp. 353-363
    • Bolger, M.B.1    Lukacova, V.2    Woltosz, W.S.3
  • 7
    • 77957735036 scopus 로고    scopus 로고
    • Effect of variations in the amounts of P-glycoprotein (ABCB1), BCRP (ABCG2) and CYP3A4 along the human small intestine on PBPK models for predicting intestinal first pass
    • Bruyère A, Declèves X, Bouzom F, Ball K, Marques C, Treton X, Pocard M, Valleur P, Bouhnik Y, and Panis Y, et al. (2010) Effect of variations in the amounts of P-glycoprotein (ABCB1), BCRP (ABCG2) and CYP3A4 along the human small intestine on PBPK models for predicting intestinal first pass. Mol Pharm 7:1596-1607.
    • (2010) Mol Pharm , vol.7 , pp. 1596-1607
    • Bruyère, A.1    Declèves, X.2    Bouzom, F.3    Ball, K.4    Marques, C.5    Treton, X.6    Pocard, M.7    Valleur, P.8    Bouhnik, Y.9    Panis, Y.10
  • 8
    • 8244231924 scopus 로고    scopus 로고
    • Effect of flow on first-pass metabolism of drugs: Single pass studies on 4-methylumbelliferone conjugation in the serially perfused rat intestine and liver preparations
    • Chen J and Pang KS (1997) Effect of flow on first-pass metabolism of drugs: single pass studies on 4-methylumbelliferone conjugation in the serially perfused rat intestine and liver preparations. J Pharmacol Exp Ther 280:24-31.
    • (1997) J Pharmacol Exp Ther , vol.280 , pp. 24-31
    • Chen, J.1    Pang, K.S.2
  • 9
    • 0033984905 scopus 로고    scopus 로고
    • A new physiologically based, segregated-flow model to explain route-dependent intestinal metabolism
    • Cong D, Doherty M, and Pang KS (2000) A new physiologically based, segregated-flow model to explain route-dependent intestinal metabolism. Drug Metab Dispos 28:224-235.
    • (2000) Drug Metab Dispos , vol.28 , pp. 224-235
    • Cong, D.1    Doherty, M.2    Pang, K.S.3
  • 10
    • 0035201323 scopus 로고    scopus 로고
    • Absorption of benzoic acid in segmental regions of the vascularly perfused rat small intestine preparation
    • Cong D, Fong AK, Lee R, and Pang KS (2001) Absorption of benzoic acid in segmental regions of the vascularly perfused rat small intestine preparation. Drug Metab Dispos 29:1539-1547.
    • (2001) Drug Metab Dispos , vol.29 , pp. 1539-1547
    • Cong, D.1    Fong, A.K.2    Lee, R.3    Pang, K.S.4
  • 11
    • 0035078138 scopus 로고    scopus 로고
    • Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats
    • De Sesso JM and Jacobson CF (2001) Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol 39:209-228.
    • (2001) Food Chem Toxicol , vol.39 , pp. 209-228
    • De Sesso, J.M.1    Jacobson, C.F.2
  • 12
    • 0032822383 scopus 로고    scopus 로고
    • Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates
    • Ekins S, Bravi G, Wikel JH, and Wrighton SA (1999) Three-dimensional-quantitative structure activity relationship analysis of cytochrome P-450 3A4 substrates. J Pharmacol Exp Ther 291:424-433.
    • (1999) J Pharmacol Exp Ther , vol.291 , pp. 424-433
    • Ekins, S.1    Bravi, G.2    Wikel, J.H.3    Wrighton, S.A.4
  • 13
    • 33750181267 scopus 로고    scopus 로고
    • Regional levels of drug transporters along the human intestinal tract: Co-expression of ABC and SLC transporters and comparison with Caco-2 cells
    • Englund G, Rorsman F, Rönnblom A, Karlbom U, Lazorova L, Gråsjö J, Kindmark A, and Artursson P (2006) Regional levels of drug transporters along the human intestinal tract: co-expression of ABC and SLC transporters and comparison with Caco-2 cells. Eur J Pharm Sci 29:269-277.
    • (2006) Eur J Pharm Sci , vol.29 , pp. 269-277
    • Englund, G.1    Rorsman, F.2    Rönnblom, A.3    Karlbom, U.4    Lazorova, L.5    Gråsjö, J.6    Kindmark, A.7    Artursson, P.8
  • 14
    • 77953737073 scopus 로고    scopus 로고
    • Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data
    • Gertz M, Harrison A, Houston JB, and Galetin A (2010) Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data. Drug Metab Dispos 38:1147-1158.
    • (2010) Drug Metab Dispos , vol.38 , pp. 1147-1158
    • Gertz, M.1    Harrison, A.2    Houston, J.B.3    Galetin, A.4
  • 15
    • 80052002510 scopus 로고    scopus 로고
    • Physiologically based pharmacokinetic modeling of intestinal first-pass metabolism of CYP3A substrates with high intestinal extraction
    • Gertz M, Houston JB, and Galetin A (2011) Physiologically based pharmacokinetic modeling of intestinal first-pass metabolism of CYP3A substrates with high intestinal extraction. Drug Metab Dispos 39:1633-1642.
    • (2011) Drug Metab Dispos , vol.39 , pp. 1633-1642
    • Gertz, M.1    Houston, J.B.2    Galetin, A.3
  • 16
    • 84864414534 scopus 로고    scopus 로고
    • Application of PBPK modeling to predict human intestinal metabolism of CYP3A substrates - An evaluation and case study using GastroPlus
    • Heikkinen AT, Baneyx G, Caruso A, and Parrott N (2012) Application of PBPK modeling to predict human intestinal metabolism of CYP3A substrates - an evaluation and case study using GastroPlus. Eur J Pharm Sci 47:375-386.
    • (2012) Eur J Pharm Sci , vol.47 , pp. 375-386
    • Heikkinen, A.T.1    Baneyx, G.2    Caruso, A.3    Parrott, N.4
  • 17
    • 84860733061 scopus 로고    scopus 로고
    • A mechanism-based approach for absorption modeling: The Gastro-Intestinal Transit Time (GITT) model
    • Hénin E, Bergstrand M, Standing JF, and Karlsson MO (2012) A mechanism-based approach for absorption modeling: the Gastro-Intestinal Transit Time (GITT) model. AAPS J 14:155-163.
    • (2012) AAPS J , vol.14 , pp. 155-163
    • Hénin, E.1    Bergstrand, M.2    Standing, J.F.3    Karlsson, M.O.4
  • 18
    • 84907451665 scopus 로고    scopus 로고
    • Assessment of intestinal availability (FG) of substrate drugs of cytochrome p450s by analyzing changes in pharmacokinetic properties caused by drug-drug interactions
    • Hisaka A, Nakamura M, Tsukihashi A, Koh S, and Suzuki H (2014) Assessment of intestinal availability (FG) of substrate drugs of cytochrome p450s by analyzing changes in pharmacokinetic properties caused by drug-drug interactions. Drug Metab Dispos 42:1640-1645.
    • (2014) Drug Metab Dispos , vol.42 , pp. 1640-1645
    • Hisaka, A.1    Nakamura, M.2    Tsukihashi, A.3    Koh, S.4    Suzuki, H.5
  • 19
    • 77949300138 scopus 로고    scopus 로고
    • Theoretical considerations on quantitative prediction of drug-drug interactions
    • Hisaka A, Ohno Y, Yamamoto T, and Suzuki H (2010) Theoretical considerations on quantitative prediction of drug-drug interactions. Drug Metab Pharmacokinet 25:48-61.
    • (2010) Drug Metab Pharmacokinet , vol.25 , pp. 48-61
    • Hisaka, A.1    Ohno, Y.2    Yamamoto, T.3    Suzuki, H.4
  • 20
    • 0032423390 scopus 로고    scopus 로고
    • Analysis of nonlinear and nonsteady state hepatic extraction with the dispersion model using the finite difference method
    • Hisaka A and Sugiyama Y (1998) Analysis of nonlinear and nonsteady state hepatic extraction with the dispersion model using the finite difference method. J Pharmacokinet Biopharm 26:495-519.
    • (1998) J Pharmacokinet Biopharm , vol.26 , pp. 495-519
    • Hisaka, A.1    Sugiyama, Y.2
  • 22
    • 25844448609 scopus 로고    scopus 로고
    • Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: Effect of fibrates and rifampicin
    • Kajosaari LI, Laitila J, Neuvonen PJ, and Backman JT (2005) Metabolism of repaglinide by CYP2C8 and CYP3A4 in vitro: effect of fibrates and rifampicin. Basic Clin Pharmacol Toxicol 97:249-256.
    • (2005) Basic Clin Pharmacol Toxicol , vol.97 , pp. 249-256
    • Kajosaari, L.I.1    Laitila, J.2    Neuvonen, P.J.3    Backman, J.T.4
  • 23
    • 0032939195 scopus 로고    scopus 로고
    • Heterogeneous tube model for the study of small intestinal transit flow
    • Kalampokis A, Argyrakis P, and Macheras P (1999) Heterogeneous tube model for the study of small intestinal transit flow. Pharm Res 16:87-91.
    • (1999) Pharm Res , vol.16 , pp. 87-91
    • Kalampokis, A.1    Argyrakis, P.2    Macheras, P.3
  • 24
    • 0036481691 scopus 로고    scopus 로고
    • Gastrointestinal transit and drug absorption
    • Kimura T and Higaki K (2002) Gastrointestinal transit and drug absorption. Biol Pharm Bull 25:149-164.
    • (2002) Biol Pharm Bull , vol.25 , pp. 149-164
    • Kimura, T.1    Higaki, K.2
  • 25
    • 44149107346 scopus 로고    scopus 로고
    • The contributions of cytochromes P450 3A4 and 3A5 to the metabolism of the phosphodiesterase type 5 inhibitors sildenafil, udenafil, and vardenafil
    • Ku HY, Ahn HJ, Seo KA, Kim H, Oh M, Bae SK, Shin JG, Shon JH, and Liu KH (2008) The contributions of cytochromes P450 3A4 and 3A5 to the metabolism of the phosphodiesterase type 5 inhibitors sildenafil, udenafil, and vardenafil. Drug Metab Dispos 36:986-990.
    • (2008) Drug Metab Dispos , vol.36 , pp. 986-990
    • Ku, H.Y.1    Ahn, H.J.2    Seo, K.A.3    Kim, H.4    Oh, M.5    Bae, S.K.6    Shin, J.G.7    Shon, J.H.8    Liu, K.H.9
  • 27
    • 0033009998 scopus 로고    scopus 로고
    • Is the role of the small intestine in first-pass metabolism overemphasized?
    • Lin JH, Chiba M, and Baillie TA (1999) Is the role of the small intestine in first-pass metabolism overemphasized? Pharmacol Rev 51:135-158.
    • (1999) Pharmacol Rev , vol.51 , pp. 135-158
    • Lin, J.H.1    Chiba, M.2    Baillie, T.A.3
  • 29
    • 77649092851 scopus 로고    scopus 로고
    • Pharmacokinetics and pharmacodynamics of low doses of midazolam administered intravenously and orally to healthy volunteers
    • Misaka S, Uchida S, Imai H, Inui N, Nishio S, Ohashi K, Watanabe H, and Yamada S (2010) Pharmacokinetics and pharmacodynamics of low doses of midazolam administered intravenously and orally to healthy volunteers. Clin Exp Pharmacol Physiol 37:290-295.
    • (2010) Clin Exp Pharmacol Physiol , vol.37 , pp. 290-295
    • Misaka, S.1    Uchida, S.2    Imai, H.3    Inui, N.4    Nishio, S.5    Ohashi, K.6    Watanabe, H.7    Yamada, S.8
  • 30
    • 79960143955 scopus 로고    scopus 로고
    • Evaluation of transport mechanism of prodrugs and parent drugs formed by intracellular metabolism in Caco-2 cells with modified carboxylesterase activity: Temocapril as a model case
    • Ohura K, Nozawa T, Murakami K, and Imai T (2011) Evaluation of transport mechanism of prodrugs and parent drugs formed by intracellular metabolism in Caco-2 cells with modified carboxylesterase activity: temocapril as a model case. J Pharm Sci 100:3985-3994.
    • (2011) J Pharm Sci , vol.100 , pp. 3985-3994
    • Ohura, K.1    Nozawa, T.2    Murakami, K.3    Imai, T.4
  • 32
    • 84866461807 scopus 로고    scopus 로고
    • Commentary: Theoretical predictions of flow effects on intestinal and systemic availability in physiologically based pharmacokinetic intestine models: The traditional model, segregated flow model, and QGut model
    • Pang KS and Chow EC (2012) Commentary: theoretical predictions of flow effects on intestinal and systemic availability in physiologically based pharmacokinetic intestine models: the traditional model, segregated flow model, and QGut model. Drug Metab Dispos 40:1869-1877.
    • (2012) Drug Metab Dispos , vol.40 , pp. 1869-1877
    • Pang, K.S.1    Chow, E.C.2
  • 35
    • 77951916870 scopus 로고    scopus 로고
    • In vitro-in vivo extrapolation of zolpidem as a perpetrator of metabolic interactions involving CYP3A
    • Polasek TM, Sadagopal JS, Elliot DJ, and Miners JO (2010) In vitro-in vivo extrapolation of zolpidem as a perpetrator of metabolic interactions involving CYP3A. Eur J Clin Pharmacol 66:275-283.
    • (2010) Eur J Clin Pharmacol , vol.66 , pp. 275-283
    • Polasek, T.M.1    Sadagopal, J.S.2    Elliot, D.J.3    Miners, J.O.4
  • 36
    • 80052262709 scopus 로고    scopus 로고
    • PHRMA CPCDC initiative on predictive models of human pharmacokinetics, part 5: Prediction of plasma concentration-time profiles in human by using the physiologically-based pharmacokinetic modeling approach
    • Poulin P, Jones RD, Jones HM, Gibson CR, Rowland M, Chien JY, Ring BJ, Adkison KK, Ku MS, and He H, et al. (2011) PHRMA CPCDC initiative on predictive models of human pharmacokinetics, part 5: prediction of plasma concentration-time profiles in human by using the physiologically-based pharmacokinetic modeling approach. J Pharm Sci 100:4127-4157.
    • (2011) J Pharm Sci , vol.100 , pp. 4127-4157
    • Poulin, P.1    Jones, R.D.2    Jones, H.M.3    Gibson, C.R.4    Rowland, M.5    Chien, J.Y.6    Ring, B.J.7    Adkison, K.K.8    Ku, M.S.9    He, H.10
  • 37
    • 0031795570 scopus 로고    scopus 로고
    • Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources
    • Rotzinger S, Fang J, and Baker GB (1998) Trazodone is metabolized to m-chlorophenylpiperazine by CYP3A4 from human sources. Drug Metab Dispos 26:572-575.
    • (1998) Drug Metab Dispos , vol.26 , pp. 572-575
    • Rotzinger, S.1    Fang, J.2    Baker, G.B.3
  • 39
    • 0023143943 scopus 로고
    • Relationship between antipyrine absorption and blood flow rate in rat jejunum, ileum, and colon
    • Schulz R and Winne D (1987) Relationship between antipyrine absorption and blood flow rate in rat jejunum, ileum, and colon. Naunyn Schmiedebergs Arch Pharmacol 335:97-102.
    • (1987) Naunyn Schmiedebergs Arch Pharmacol , vol.335 , pp. 97-102
    • Schulz, R.1    Winne, D.2
  • 41
    • 65549089670 scopus 로고    scopus 로고
    • Introduction to computational oral absorption simulation
    • Sugano K (2009) Introduction to computational oral absorption simulation. Expert Opin Drug Metab Toxicol 5:259-293.
    • (2009) Expert Opin Drug Metab Toxicol , vol.5 , pp. 259-293
    • Sugano, K.1
  • 42
    • 0036805724 scopus 로고    scopus 로고
    • Comparison of human duodenum and Caco-2 gene expression profiles for 12, 000 gene sequences tags and correlation with permeability of 26 drugs
    • Sun D, Lennernas H, Welage LS, Barnett JL, Landowski CP, Foster D, Fleisher D, Lee KD, and Amidon GL (2002) Comparison of human duodenum and Caco-2 gene expression profiles for 12, 000 gene sequences tags and correlation with permeability of 26 drugs. Pharm Res 19:1400-1416.
    • (2002) Pharm Res , vol.19 , pp. 1400-1416
    • Sun, D.1    Lennernas, H.2    Welage, L.S.3    Barnett, J.L.4    Landowski, C.P.5    Foster, D.6    Fleisher, D.7    Lee, K.D.8    Amidon, G.L.9
  • 44
    • 0037378726 scopus 로고    scopus 로고
    • Segmental intestinal transporters and metabolic enzymes on intestinal drug absorption
    • Tam D, Tirona RG, and Pang KS (2003) Segmental intestinal transporters and metabolic enzymes on intestinal drug absorption. Drug Metab Dispos 31:373-383.
    • (2003) Drug Metab Dispos , vol.31 , pp. 373-383
    • Tam, D.1    Tirona, R.G.2    Pang, K.S.3
  • 45
    • 48049089223 scopus 로고    scopus 로고
    • Simulation modelling of human intestinal absorption using Caco-2 permeability and kinetic solubility data for early drug discovery
    • Thomas S, Brightman F, Gill H, Lee S, and Pufong B (2008) Simulation modelling of human intestinal absorption using Caco-2 permeability and kinetic solubility data for early drug discovery. J Pharm Sci 97:4557-4574.
    • (2008) J Pharm Sci , vol.97 , pp. 4557-4574
    • Thomas, S.1    Brightman, F.2    Gill, H.3    Lee, S.4    Pufong, B.5
  • 46
    • 77249122159 scopus 로고    scopus 로고
    • Physicochemical space for optimum oral bioavailability: Contribution of human intestinal absorption and first-pass elimination
    • Varma MV, Obach RS, Rotter C, Miller HR, Chang G, Steyn SJ, El-Kattan A, and Troutman MD (2010) Physicochemical space for optimum oral bioavailability: contribution of human intestinal absorption and first-pass elimination. J Med Chem 53:1098-1108.
    • (2010) J Med Chem , vol.53 , pp. 1098-1108
    • Varma, M.V.1    Obach, R.S.2    Rotter, C.3    Miller, H.R.4    Chang, G.5    Steyn, S.J.6    El-Kattan, A.7    Troutman, M.D.8
  • 47
    • 0344084044 scopus 로고    scopus 로고
    • A physiologic model for simulating gastrointestinal flow and drug absorption in rats
    • Willmann S, Schmitt W, Keldenich J, and Dressman JB (2003) A physiologic model for simulating gastrointestinal flow and drug absorption in rats. Pharm Res 20:1766-1771.
    • (2003) Pharm Res , vol.20 , pp. 1766-1771
    • Willmann, S.1    Schmitt, W.2    Keldenich, J.3    Dressman, J.B.4
  • 48
    • 3242778534 scopus 로고    scopus 로고
    • A physiological model for the estimation of the fraction dose absorbed in humans
    • Willmann S, Schmitt W, Keldenich J, Lippert J, and Dressman JB (2004) A physiological model for the estimation of the fraction dose absorbed in humans. J Med Chem 47:4022-4031.
    • (2004) J Med Chem , vol.47 , pp. 4022-4031
    • Willmann, S.1    Schmitt, W.2    Keldenich, J.3    Lippert, J.4    Dressman, J.B.5
  • 49
    • 0017838459 scopus 로고
    • Blood flow in intestinal absorption models
    • Winne D (1978) Blood flow in intestinal absorption models. J Pharmacokinet Biopharm 6:55-78.
    • (1978) J Pharmacokinet Biopharm , vol.6 , pp. 55-78
    • Winne, D.1
  • 51
    • 0032888376 scopus 로고    scopus 로고
    • A compartmental absorption and transit model for estimating oral drug absorption
    • Yu LX and Amidon GL (1999) A compartmental absorption and transit model for estimating oral drug absorption. Int J Pharm 186:119-125.
    • (1999) Int J Pharm , vol.186 , pp. 119-125
    • Yu, L.X.1    Amidon, G.L.2


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.