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: S41-67.
Ando H, Hisaka A, and Suzuki H (2015) A new physiologically based pharmacokinetic model for the prediction of gastrointestinal drug absorption: translocation model. Drug Metab Dispos 43: 590-602.
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.
Barbanoj MJ, Urbano G, Antonijoan R, Ballester MR, and Valle M (2007) Different acute tolerance development to EEG, psychomotor performance and subjective assessment effects after two intermittent oral doses of alprazolam in healthy volunteers. Neuropsychobiology 55: 203-212.
Brunton LL, Lazo JS, Parker KL editors (2005) Goodman & Gilman's The Pharmacological Basis of Therapeutics, eleventh edition ed., New York: McGraw-Hill Companies, Inc.
Bergstrand M, Soderlind E, Eriksson UG, Weitschies W, and Karlsson MO (2012) A semi-mechanistic modeling strategy to link in vitro and in vivo drug release for modified release formulations. Pharm Res 29:695-706.
Bergstrand M, Soderlind 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.
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.
Bornemann LD, Min BH, Crews T, Rees MM, Blumenthal HP, Colburn WA, and Patel IH (1985) Dose dependent pharmacokinetics of midazolam. Eur J Clin Pharmacol 29:91-95.
Bruyere A, Decleves X, Bouzom F, Ball K, Marques C, Treton X, Pocard M, Valleur P, Bouhnik Y, Panis Y, Scherrmann JM, and Mouly S (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.
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.
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.
DeSesso JM, and Jacobson CF (2001) Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol 39: 209-228.
DeSesso JM, and Williams AL (2008) Contrasting the Gastrointestinal Tracts of Mammals: Factors that Influence Absorption. Annu Rep Med Chem 43: 353-371.
Drescher S, Glaeser H, Mürdter T, Hitzl M, Eichelbaum M, and Fromm MF (2003) P-glycoprotein-mediated intestinal and biliary digoxin transport in humans. Clin Pharmacol Ther. 73: 223-231.
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.
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.
Fenner KS, Troutman MD, Kempshall S, Cook JA, Ware JA, Smith DA, Lee CA (2009) Drug-drug interactions mediated through P-glycoprotein: clinical relevance and in vitro-in vivo correlation using digoxin as a probe drug. Clin Pharmacol Ther 85: 173-181.
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.
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. European Medicines Agency, Committee for Human Medicinal Products (CHMP), Guideline on the Investigation of Drug Interactions. October 2010. Available at: http://www.ema.europa.eu/docs/en_GB/document_library/Scientific_guideline/2010/05/WC500090112.pdf. Accessed January 27, 2017.
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.
Henin 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.
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.
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.
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.
Ieiri I, Tsunemitsu S, Maeda K, Ando Y, Izumi N, Kimura M, Yamane N, Okuzono T, Morishita M, Kotani N, Kanda E, Deguchi M, Matsuguma K, Matsuki S, Hirota T, Irie S, Kusuhara H, and Sugiyama Y (2013) Mechanisms of pharmacokinetic enhancement between ritonavir and saquinavir; micro/small dosing tests using midazolam (CYP3A4), fexofenadine (p-glycoprotein), and pravastatin (OATP1B1) as probe drugs. J Clin Pharmacol 53: 654-661.
Jamei M, Turner D, Yang J, Neuhoff S, Polak S, Rostami-Hodjegan A, and Tucker G (2009) Population-based mechanistic prediction of oral drug absorption. AAPS J 11:225-237.
Kadono K, Akabane T, Tabata K, Gato K, Terashita S, and Teramura T (2010) Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor. Drug Metab Dispos 38: 1230-1237.
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.
Kamiyama E, Sugiyama D, Nakai D, Miura S, and Okazaki O (2009) Culture period-dependent change of function and expression of ATP-binding cassette transporters in Caco-2 cells. Drug Metab Dispos. 37: 1956-1962.
Kato M, Chiba K, Hisaka A, Ishigami M, Kayama M, Mizuno N, Nagata Y, Takakuwa S, Tsukamoto Y, Ueda K, Kusuhara H, Ito K, and Sugiyama Y (2003) The intestinal first-pass metabolism of substrates of CYP3A4 and P-glycoprotein-quantitative analysis based on information from the literature. Drug Metab Pharmacokinet 18: 365-372.
Kimura T and Higaki K (2002) Gastrointestinal transit and drug absorption. Biol Pharm Bull 25:149-164.
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.
Lavrijsen KL, Van Houdt JM, Van Dyck DM, Hendrickx JJ, Woestenborghs RJ, Lauwers W, Meuldermans WE, and Heykants JJ (1988) Is the metabolism of alfentanil subject to debrisoquine polymorphism? A study using human liver microsomes. Anesthesiology 69: 535-540.
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.
Lin KM, Lau JK, Smith R, Phillips P, Antal E, and Poland RE (1988) Comparison of alprazolam plasma levels in normal Asian and Caucasian male volunteers. Psychopharmacology 96: 365-369.
Maeda K, Takano J, Ikeda Y, Fujita T, Oyama Y, Nozawa K, Kumagai Y, and Sugiyama Y (2011) Nonlinear pharmacokinetics of oral quinidine and verapamil in healthy subjects: a clinical microdosing study. Clin Pharmacol Ther 90:263-270.
Mano Y, Sugiyama Y, and Ito K (2015) Use of a Physiologically Based Pharmacokinetic Model for Quantitative Prediction of Drug-Drug Interactions via CYP3A4 and Estimation of the Intestinal Availability of CYP3A4 Substrates. J Pharm Sci 104:3183-3193
Margolskee A, Darwich AS, Pepin X, Pathak SM, Bolger MB, Aarons L, Rostami-Hodjegan A, Angstenberger J, Graf F, Laplanche L, Müller T, Carlert S, Daga P, Murphy D, Tannergren C, Yasin M, Greschat-Schade S, Mück W, Muenster U, van der Mey D, Frank KJ, Lloyd R, Adriaenssen L, Bevernage J, De Zwart L, Swerts D, Tistaert C, Van Den Bergh A, Van Peer A, Beato S, Nguyen-Trung AT, Bennett J, McAllister M, Wong M, Zane P, Ollier C, Vicat P, Kolhmann M, Marker A, Brun P, Mazuir F, Beilles S, Venczel M, Boulenc X, Loos P, Lennernäs H, and Abrahamsson B (2007) IMI - oral biopharmaceutics tools project - evaluation of bottom-up PBPK prediction success part 1: Characterisation of the OrBiTo database of compounds. Eur J Pharm Sci 96: 598-609.
Margolskee A, Darwich AS, Pepin X, Aarons L, Galetin A, Rostami-Hodjegan A, Carlert S, Hammarberg M, Hilgendorf C, Johansson P, Karlsson E, Murphy D, Tannergren C, Thörn H, Yasin M, Mazuir F, Nicolas O, Ramusovic S, Xu C, Pathak SM, Korjamo T, Laru J, Malkki J, Pappinen S, Tuunainen J, Dressman J, Hansmann S, Kostewicz E, He H, Heimbach T, Wu F, Hoft C, Laplanche L, Pang Y, Bolger MB, Huehn E, Lukacova V, Mullin JM, Szeto KX, Costales C, Lin J, McAllister M, Modi S, Rotter C, Varma M, Wong M, Mitra A, Bevernage J, Biewenga J, Van Peer A, Lloyd R, Shardlow C, Langguth P, Mishenzon I, Nguyen MA, Brown J, Lennernäs H, and Abrahamsson B (2017) IMI - Oral biopharmaceutics tools project - Evaluation of bottom-up PBPK prediction success part 2: An introduction to the simulation exercise and overview of results. Eur J Pharm Sci 96: 610-625.
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.
Mitra P, Audus K, Williams G, Yazdanian M, Galinis D. (2011) A comprehensive study demonstrating that p-glycoprotein function is directly affected by changes in pH: implications for intestinal pH and effects on drug absorption. J Pharm Sci. 100:4258-4268.
MHLW. 2018. Available at: https://www.mhlw.go.jp/hourei/doc/tsuchi/T180724I0150.pdf. Accessed Sptember 12, 2018.
Neuhoff S, Ungell AL, Zamora I, and Artursson P (2003) pH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: implications for drug-drug interactions. Pharm Res. 20:1141-1148.
Neuhoff S, Ungell AL, Zamora I, and Artursson P (2005) pH-Dependent passive and active transport of acidic drugs across Caco-2 cell monolayers. Eur J Pharm Sci 25: 211-220.
Neuhoff S, Yeo KR, Barter Z, Jamei M, Turner DB, and Rostami-Hodjegan A (2013) Application of permeability-limited physiologically-based pharmacokinetic models: part II - prediction of P-glycoprotein mediated drug-drug interactions with digoxin. J Pharm Sci 102: 3161-3173.
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.
Paine MF, Khalighi M, Fisher JM, Shen DD, Kunze KL, Marsh CL, Perkins JD, and Thummel KE (1997) Characterization of interintestinal and intraintestinal variations in human CYP3A-dependent metabolism. J Pharmacol Exp Ther 283:1552-1562.
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.
Petri N, Tannergren C, Holst B, Mellon FA, Bao Y, Plumb GW, Bacon J, O'Leary KA, Kroon PA, Knutson L, Forsell P, Eriksson T, Lennernas H, and Williamson G (2003) Absorption/metabolism of sulforaphane and quercetin, and regulation of phase II enzymes, in human jejunum in vivo. Drug Metab Dispos 31:805-813.
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.
Poulin P, Jones RD, Jones HM, Gibson CR, Rowland M, Chien JY, Ring BJ, Adkison KK, Ku MS, He H, Vuppugalla R, Marathe P, Fischer V, Dutta S, Sinha VK, Bjornsson T, Lave T, and Yates JW (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.
Ring BJ, Chien JY, Adkison KK, Jones HM, Rowland M, Jones RD, Yates JW, Ku MS, Gibson CR, He H, Vuppugalla R, Marathe P, Fischer V, Dutta S, Sinha VK, Björnsson T, Lavé T, Poulin P (2011) PhRMA CPCDC initiative on predictive models of human pharmacokinetics, part 3: comparative assessement of prediction methods of human clearance. J Pharm Sci 100:4090-4110.
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.
Schiller C, Frohlich CP, Giessmann T, Siegmund W, Monnikes H, Hosten N, and Weitschies W (2005) Intestinal fluid volumes and transit of dosage forms as assessed by magnetic resonance imaging. Aliment Pharmacol Ther 22:971-979.
Shimizu M, Uno T, Sugawara K, and Tateishi T (2006) Effects of itraconazole and diltiazem on the pharmacokinetics of fexofenadine, a substrate of P-glycoprotein. Br J Clin Pharmacol 61: 538-544.
Smith RB, Kroboth PD, Vanderlugt JT, Phillips JP, and Juhl RP (1984) Pharmacokinetics and pharmacodynamics of alprazolam after oral and IV administration. Psychopharmacology 84: 452-456.
Stephens RH, O'Neill CA, Warhurst A, Carlson GL, Rowland M, and Warhurst G (2001) Kinetic profiling of P-glycoprotein-mediated drug efflux in rat and human intestinal epithelia. J Pharmacol Exp Ther 296: 584-591.
Sugano K (2009) Introduction to computational oral absorption simulation. Expert Opin Drug Metab Toxicol 5:259-293.
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.
Tachibana T, Kitamura S, Kato M, Mitsui T, Shirasaka Y, Yamashita S, and Sugiyama Y (2010) Model analysis of the concentration-dependent permeability of P-gp substrates. Pharm Res 27:442-446.
Tachibana T, Kato M, Watanabe T, Mitsui T, and Sugiyama Y (2009) Method for predicting the risk of drug-drug interactions involving inhibition of intestinal CYP3A4 and P-glycoprotein. Xenobiotica 39: 430-443.
Takano J, Maeda K, Bolger MB, and Sugiyama Y (2016) The Prediction of the Relative Importance of CYP3A/P-glycoprotein to the Nonlinear Intestinal Absorption of Drugs by Advanced Compartmental Absorption and Transit Model. Drug Metab Dispos 44: 1808-1818.
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.
Troutman MD, and Thakker DR (2003) Efflux ratio cannot assess P-glycoprotein-mediated attenuation of absorptive transport: asymmetric effect of P-glycoprotein on absorptive and secretory transport across Caco-2 cell monolayers. Pharm Res. 20: 1200-1209.
Umeyama Y, Fujioka Y, and Okuda T (2014) Clarification of P-glycoprotein inhibition-related drug-drug interaction risks based on a literature search of the clinical information. Xenobiotica 44: 1135-1144.
U.S. Department of Health and Human Services, Food and Drug Administration, Center for Drug Evaluation and Research (CDER). Guidance for industry, drug interaction studies-study design, data analysis, implications for dosing, and labeling recommendations. February 2012. Available at: http://www.fda.gov/downloads/drugs/guidancecomplianceregulatoryinformation/guida nces/ucm292362.pdf. Accessed January 27, 2017.
Varma MV, and Panchagnula R (2005) pH-dependent functional activity of P-glycoprotein in limiting intestinal absorption of protic drugs: kinetic analysis of quinidine efflux in situ. J Pharm Sci 94: 2632-2643.
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.
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.
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.
Winne D (1978) Blood flow in intestinal absorption models. J Pharmacokinet Biopharm 6: 55-78.
Yang J, Jamei M, Yeo KR, Tucker GT, and Rostami-Hodjegan A (2007) Prediction of intestinal first-pass drug metabolism. Curr Drug Metab 8:676-684.
Yasui N, Otani K, Kaneko S, Ohkubo T, Osanai T, Sugawara K, Chiba K, and Ishizaki T. (1996) A kinetic and dynamic study of oral alprazolam with and without erythromycin in humans: in vivo evidence for the involvement of CYP3A4 in alprazolam metabolism. Clin Pharmacol Ther 59: 514-519.
Yu LX and Amidon GL (1999) A compartmental absorption and transit model for estimating oral drug absorption. Int J Pharm 186:119-125.
Zhang S, and Morris ME (2003) Effect of the flavonoids biochanin A and silymarin on the P-glycoprotein-mediated transport of digoxin and vinblastine in human intestinal Caco-2 cells. Pharm Res. 20: 1184-1191.
論文の公開元へ
