Egan WJ, Lauri G: Prediction of intestinal permeability. Adv Drug Deliv Rev. 2002, 54 (3): 273-289. 10.1016/S0169-409X(02)00004-2.
Article
CAS
PubMed
Google Scholar
Zhao YH, Le J, Abraham MH, Hersey A, Eddershaw PJ, Luscombe CN, Butina D, Beck G, Sherborne B, Cooper I: Evaluation of human intestinal absorption data and subsequent derivation of a quantitative structure-activity relationship (QSAR) with the Abraham descriptors. J Pharm Sci. 2001, 90 (6): 749-784. 10.1002/jps.1031.
Article
CAS
PubMed
Google Scholar
Amidon KS, Langguth P, Lennernas H, Yu L, Amidon GL: Bioequivalence of oral products and the biopharmaceutics classification system: science, regulation, and public policy. Clin Pharmacol Ther. 2011, 90 (3): 467-470. 10.1038/clpt.2011.109.
Article
CAS
PubMed
PubMed Central
Google Scholar
Dahan A, Lennernas H, Amidon GL: The fraction dose absorbed, in humans, and high jejunal human permeability relationship. Molecular pharmaceutics. 2012, 9 (6): 1847-1851. 10.1021/mp300140h.
Article
CAS
PubMed
PubMed Central
Google Scholar
Soderholm JD, Olaison G, Kald A, Tagesson C, Sjodahl R: Absorption profiles for polyethylene glycols after regional jejunal perfusion and oral load in healthy humans. Dig Dis Sci. 1997, 42 (4): 853-857. 10.1023/A:1018836803254.
Article
CAS
PubMed
Google Scholar
Levitt DG: The use of a physiologically based pharmacokinetic model to evaluate deconvolution measurements of systemic absorption. BMC Clin Pharmacol. 2003, 3: 1-
Article
PubMed
PubMed Central
Google Scholar
Levitt DG: PKQuest_Java: free, interactive physiologically based pharmacokinetic software package and tutorial. BMC research notes. 2009, 2: 158-10.1186/1756-0500-2-158.
Article
PubMed
PubMed Central
Google Scholar
Sparacino G, Pillonetto G, Capello M, De Nicolao G, Cobelli C: WINSTODEC: a stochastic deconvolution interactive program for physiological and pharmacokinetic systems. Comput Methods Programs Biomed. 2002, 67 (1): 67-77. 10.1016/S0169-2607(00)00151-6.
Article
PubMed
Google Scholar
Verotta D: Estimation and model selection in constrained deconvolution. Ann Biomed Eng. 1993, 21 (6): 605-620. 10.1007/BF02368641.
Article
CAS
PubMed
Google Scholar
Agoram B, Woltosz WS, Bolger MB: Predicting the impact of physiological and biochemical processes on oral drug bioavailability. Adv Drug Deliv Rev. 2001, 50 (Suppl 1): S41-S67.
Article
CAS
PubMed
Google Scholar
Yu LX, Amidon GL: A compartmental absorption and transit model for estimating oral drug absorption. Int J Pharm. 1999, 186 (2): 119-125. 10.1016/S0378-5173(99)00147-7.
Article
CAS
PubMed
Google Scholar
Ni PF HONFH, Fox JL, Leuenberger H, Higuchi HI: Theoretical model studies of intestinal drug absorption V. Non-steady-state fluid flow and absorption. Int J Pharm. 1980, 5: 33-47. 10.1016/0378-5173(80)90048-4.
Article
Google Scholar
Collins PJ, Horowitz M, Cook DJ, Harding PE, Shearman DJ: Gastric emptying in normal subjects–a reproducible technique using a single scintillation camera and computer system. Gut. 1983, 24 (12): 1117-1125. 10.1136/gut.24.12.1117.
Article
CAS
PubMed
PubMed Central
Google Scholar
George JD: New clinical method for measuring the rate of gastric emptying: the double sampling test meal. Gut. 1968, 9 (2): 237-242. 10.1136/gut.9.2.237.
Article
CAS
PubMed
PubMed Central
Google Scholar
Wu CY, Benet LZ, Hebert MF, Gupta SK, Rowland M, Gomez DY, Wacher VJ: Differentiation of absorption and first-pass gut and hepatic metabolism in humans: studies with cyclosporine. Clin Pharmacol Ther. 1995, 58 (5): 492-497. 10.1016/0009-9236(95)90168-X.
Article
CAS
PubMed
Google Scholar
Press WH, Teukolsky SA, Vetterling WT, Flannery BP: Numerical Recipes in C. 1992, Cambridge: Cambridge University Press, 2
Google Scholar
Poulin P, Schoenlein K, Theil FP: Prediction of adipose tissue: plasma partition coefficients for structurally unrelated drugs. J Pharm Sci. 2001, 90 (4): 436-447. 10.1002/1520-6017(200104)90:4<436::AID-JPS1002>3.0.CO;2-P.
Article
CAS
PubMed
Google Scholar
Lennernas H: Intestinal permeability and its relevance for absorption and elimination. Xenobiotica. 2007, 37 (10–11): 1015-1051.
Article
CAS
PubMed
Google Scholar
Miller MS, Galligan JJ, Burks TF: Accurate measurement of intestinal transit in the rat. J Pharmacol Methods. 1981, 6 (3): 211-217. 10.1016/0160-5402(81)90110-8.
Article
CAS
PubMed
Google Scholar
Yu LX, Amidon GL: Characterization of small intestinal transit time distribution in humans. Int J Pharm. 1998, 171 (2): 157-163. 10.1016/S0378-5173(98)00174-4.
Article
CAS
Google Scholar
Caride VJ, Prokop EK, Troncale FJ, Buddoura W, Winchenbach K, McCallum RW: Scintigraphic determination of small intestinal transit time: comparison with the hydrogen breath technique. Gastroenterology. 1984, 86 (4): 714-720.
CAS
PubMed
Google Scholar
Davis SS, Hardy JG, Fara JW: Transit of pharmaceutical dosage forms through the small intestine. Gut. 1986, 27 (8): 886-892. 10.1136/gut.27.8.886.
Article
CAS
PubMed
PubMed Central
Google Scholar
Yang J, Jamei M, Yeo KR, Tucker GT, Rostami-Hodjegan A: Prediction of intestinal first-pass drug metabolism. Curr Drug Metab. 2007, 8 (7): 676-684. 10.2174/138920007782109733.
Article
CAS
PubMed
Google Scholar
Clements JA, Heading RC, Nimmo WS, Prescott LF: Kinetics of acetaminophen absorption and gastric emptying in man. Clin Pharmacol Ther. 1978, 24 (4): 420-431.
Article
CAS
PubMed
Google Scholar
Heading RC, Nimmo J, Prescott LF, Tothill P: The dependence of paracetamol absorption on the rate of gastric emptying. Br J Pharmacol. 1973, 47 (2): 415-421. 10.1111/j.1476-5381.1973.tb08339.x.
Article
CAS
PubMed
PubMed Central
Google Scholar
Ogungbenro K, Vasist L, Maclaren R, Dukes G, Young M, Aarons L: A semi-mechanistic gastric emptying model for the population pharmacokinetic analysis of orally administered acetaminophen in critically ill patients. Pharm Res. 2011, 28 (2): 394-404. 10.1007/s11095-010-0290-8.
Article
CAS
PubMed
Google Scholar
Ameer B, Divoll M, Abernethy DR, Greenblatt DJ, Shargel L: Absolute and relative bioavailability of oral acetaminophen preparations. J Pharm Sci. 1983, 72 (8): 955-958. 10.1002/jps.2600720832.
Article
CAS
PubMed
Google Scholar
Divoll M, Ameer B, Abernethy DR, Greenblatt DJ: Age does not alter acetaminophen absorption. J Am Geriatr Soc. 1982, 30 (4): 240-244.
Article
CAS
PubMed
Google Scholar
Eandi M, Viano I, Ricci Gamalero S: Absolute bioavailability of paracetamol after oral or rectal administration in healthy volunteers. Arzneimittelforschung. 1984, 34 (8): 903-907.
CAS
PubMed
Google Scholar
Mitchell DY, Barr WH, Eusebio RA, Stevens KA, Duke FP, Russell DA, Nesbitt JD, Powell JH, Thompson GA: Risedronate pharmacokinetics and intra- and inter-subject variability upon single-dose intravenous and oral administration. Pharm Res. 2001, 18 (2): 166-170. 10.1023/A:1011024200280.
Article
CAS
PubMed
Google Scholar
Hui YF, Kolars J, Hu Z, Fleisher D: Intestinal clearance of H2-antagonists. Biochem Pharmacol. 1994, 48 (2): 229-231. 10.1016/0006-2952(94)90091-4.
Article
CAS
PubMed
Google Scholar
Walkenstein SS, Dubb JW, Randolph WC, Westlake WJ, Stote RM, Intoccia AP: Bioavailability of cimetidine in man. Gastroenterology. 1978, 74 (2 Pt 2): 360-365.
CAS
PubMed
Google Scholar
Heykants J, Hendriks R, Meuldermans W, Michiels M, Scheygrond H, Reyntjens H: On the pharmacokinetics of domperidone in animals and man. IV. The pharmacokinetics of intravenous domperidone and its bioavailability in man following intramuscular, oral and rectal administration. Eur J Drug Metab Pharmacokinet. 1981, 6 (1): 61-70. 10.1007/BF03189516.
Article
CAS
PubMed
Google Scholar
Gray VA, Dressman JB: Change of pH requirement for simulated intestinal fluid TS. Pharmacopeial Forum. 1996, 22 (1): 1943-1945.
Google Scholar
Ovesen L, Bendtsen F, Tage-Jensen U, Pedersen NT, Gram BR, Rune SJ: Intraluminal pH in the stomach, duodenum, and proximal jejunum in normal subjects and patients with exocrine pancreatic insufficiency. Gastroenterology. 1986, 90 (4): 958-962.
Article
CAS
PubMed
Google Scholar
Evans DF, Pye G, Bramley R, Clark AG, Dyson TJ, Hardcastle JD: Measurement of gastrointestinal pH profiles in normal ambulant human subjects. Gut. 1988, 29 (8): 1035-1041. 10.1136/gut.29.8.1035.
Article
CAS
PubMed
PubMed Central
Google Scholar
Lalezari D: Gastrointestinal pH profile in subjects with irritible syndrome. Ann Gastroenterol. 2012, 25 (4): 1-5.
Google Scholar
Avdeef A: Absorption and drug development. Solubility, permeability and charge state. 2003, Hoboken, New Jersey: John Wiley and Sons,Inc
Google Scholar
Kramer SD: Absorption prediction from physicochemical parameters. Pharm Sci Technology Today. 1999, 2 (9): 373-380. 10.1016/S1461-5347(99)00188-1.
Article
CAS
Google Scholar
Pauli-Magnus C, Murdter T, Godel A, Mettang T, Eichelbaum M, Klotz U, Fromm MF: P-glycoprotein-mediated transport of digitoxin, alpha-methyldigoxin and beta-acetyldigoxin. Naunyn Schmiedebergs Arch Pharmacol. 2001, 363 (3): 337-343. 10.1007/s002100000354.
Article
CAS
PubMed
Google Scholar
Dahan A, Amidon GL: Grapefruit juice and its constituents augment colchicine intestinal absorption: potential hazardous interaction and the role of p-glycoprotein. Pharm Res. 2009, 26 (4): 883-892. 10.1007/s11095-008-9789-7.
Article
CAS
PubMed
Google Scholar
Jung N, Lehmann C, Rubbert A, Knispel M, Hartmann P, van Lunzen J, Stellbrink HJ, Faetkenheuer G, Taubert D: Relevance of the organic cation transporters 1 and 2 for antiretroviral drug therapy in human immunodeficiency virus infection. Drug Metab Dispos. 2008, 36 (8): 1616-1623. 10.1124/dmd.108.020826.
Article
CAS
PubMed
Google Scholar
Levitt DG, Hakim AA, Lifson N: Evaluation of components of transport of sugars by dog jejunum in vivo. Am J Physiol. 1969, 217 (3): 777-783.
CAS
PubMed
Google Scholar
Rolston DD, Mathan VI: Xylose transport in the human jejunum. Dig Dis Sci. 1989, 34 (4): 553-558. 10.1007/BF01536332.
Article
CAS
PubMed
Google Scholar
Csaky TZ, Ho PM, Csaky TZ, Ho PM: Intestinal transport of D-xylose. Proceedings of the Society for Experimental Biology and Medicine Society for Experimental Biology and Medicine (New York, NY). 1965, 120 (2): 403-408.
Article
CAS
Google Scholar
Tsuda M, Terada T, Irie M, Katsura T, Niida A, Tomita K, Fujii N, Inui K: Transport characteristics of a novel peptide transporter 1 substrate, antihypotensive drug midodrine, and its amino acid derivatives. J Pharmacol Exp Ther. 2006, 318 (1): 455-460. 10.1124/jpet.106.102830.
Article
CAS
PubMed
Google Scholar
Rowland M: Influence of route of administration on drug availability. J Pharm Sci. 1972, 61 (1): 70-74. 10.1002/jps.2600610111.
Article
CAS
PubMed
Google Scholar
Bochner F, Williams DB, Morris PM, Siebert DM, Lloyd JV: Pharmacokinetics of low-dose oral modified release, soluble and intravenous aspirin in man, and effects on platelet function. Eur J Clin Pharmacol. 1988, 35 (3): 287-294. 10.1007/BF00558267.
Article
CAS
PubMed
Google Scholar
Hogben CA, Tocco DJ, Brodie BB, Schanker LS: On the mechanism of intestinal absorption of drugs. J Pharmacol Exp Ther. 1959, 125 (4): 275-282.
CAS
PubMed
Google Scholar
Levitt MD, Strocchi A, Levitt DG: Human jejunal unstirred layer: evidence for extremely efficient luminal stirring. Am J Physiol. 1992, 262 (3 Pt 1): G593-G596.
CAS
PubMed
Google Scholar
Rechkemmer G, Wahl M, Kuschinsky W, von Engelhardt W: pH-microclimate at the luminal surface of the intestinal mucosa of guinea pig and rat. Pflugers Arch. 1986, 407 (1): 33-40. 10.1007/BF00580717.
Article
CAS
PubMed
Google Scholar
Takanaga H, Tamai I, Tsuji A: pH-dependent and carrier-mediated transport of salicylic acid across Caco-2 cells. J Pharm Pharmacol. 1994, 46 (7): 567-570. 10.1111/j.2042-7158.1994.tb03858.x.
Article
CAS
PubMed
Google Scholar
Tamai I, Takanaga H, Maeda H, Yabuuchi H, Sai Y, Suzuki Y, Tsuji A: Intestinal brush-border membrane transport of monocarboxylic acids mediated by proton-coupled transport and anion antiport mechanisms. J Pharm Pharmacol. 1997, 49 (1): 108-112. 10.1111/j.2042-7158.1997.tb06762.x.
Article
CAS
PubMed
Google Scholar
Takagi M, Taki Y, Sakane T, Nadai T, Sezaki H, Oku N, Yamashita S: A new interpretation of salicylic acid transport across the lipid bilayer: implications of pH-dependent but not carrier-mediated absorption from the gastrointestinal tract. J Pharmacol Exp Ther. 1998, 285 (3): 1175-1180.
CAS
PubMed
Google Scholar
Fagerholm U, Lennernas H: Experimental estimation of the effective unstirred water layer thickness in the human jejunum, and it importance in oral drug absorption. Eur J Pharm Sci. 1995, 3: 247-253. 10.1016/0928-0987(95)00027-B.
Article
CAS
Google Scholar
Mackenzie NM: Comparison of the metabolic activities of enterocytes isolated from different regions of the small intestine of the neonate. Biol Neonate. 1985, 48 (5): 257-268. 10.1159/000242179.
Article
CAS
PubMed
Google Scholar
Lennernas H: Human intestinal permeability. J Pharm Sci. 1998, 87 (4): 403-410. 10.1021/js970332a.
Article
CAS
PubMed
Google Scholar
Knutson T, Fridblom P, Ahlstrom H, Magnusson A, Tannergren C, Lennernas H: Increased understanding of intestinal drug permeability determined by the LOC-I-GUT approach using multislice computed tomography. Mol Pharm. 2009, 6 (1): 2-10. 10.1021/mp800145r.
Article
CAS
PubMed
Google Scholar
Larregieu CA, Benet LZ: Drug discovery and regulatory considerations for improving in silico and in vitro predictions that use caco-2 as a surrogate for human intestinal permeability measurements. AAPS J. 2013, 15 (2): 483-497. 10.1208/s12248-013-9456-8.
Article
CAS
PubMed
PubMed Central
Google Scholar
Thomas S, Brightman F, Gill H, Lee S, Pufong B: Simulation modelling of human intestinal absorption using Caco-2 permeability and kinetic solubility data for early drug discovery. J Pharm Sci. 2008, 97 (10): 4557-4574. 10.1002/jps.21305.
Article
CAS
PubMed
Google Scholar
Hidalgo IJ, Hillgren KM, Grass GM, Borchardt RT: Characterization of the unstirred water layer in Caco-2 cell monolayers using a novel diffusion apparatus. Pharm Res. 1991, 8 (2): 222-227. 10.1023/A:1015848205447.
Article
CAS
PubMed
Google Scholar