Comprehensive study on regional human intestinal permeability and prediction of fraction absorbed of drugs using the Ussing chamber technique

European Journal of Pharmaceutical Sciences

Volumn 48, Issue 1-2, 2013, Pages 166-180

  Sjöberg, Åsa ^a   Lutz, Mareike ^a   Tannergren, Christer ^a   Wingolf, Caroline ^a   Borde, Anders ^a   Ungell, Anna Lena ^a  

^a ASTRAZENECA R AND D   (Sweden)

Author keywords

Absorption; Human intestine; Intestinal metabolism; Intestinal permeability; Regional permeability; Ussing chamber

Indexed keywords

ATENOLOL; CIMETIDINE; CREATININE; DICLOFENAC; DIGOXIN; DILTIAZEM; FEXOFENADINE; GLUCOSE; HYDROCORTISONE; INDOMETACIN; LEUCINE; MANNITOL; MELAGATRAN; METOPROLOL; MIDAZOLAM; OSELTAMIVIR; OXPRENOLOL; PHENAZONE; PROPRANOLOL; QUINIDINE; RANITIDINE; ROSUVASTATIN; SALAZOSULFAPYRIDINE; SALICYLIC ACID; TESTOSTERONE; VERAPAMIL; VINBLASTINE; XIMELAGATRAN;

ARTICLE; COLON; CONTROLLED STUDY; DIFFUSION CHAMBER; DRUG ABSORPTION; DRUG PENETRATION; DRUG TRANSPORT; DUODENUM; HUMAN; HUMAN TISSUE; ILEUM; INTESTINE MUCOSA PERMEABILITY; JEJUNUM; PRIORITY JOURNAL; SHORT CIRCUIT CURRENT;

DRUG EVALUATION, PRECLINICAL; HUMANS; INTESTINAL ABSORPTION; INTESTINES; PERMEABILITY; PHARMACEUTICAL PREPARATIONS;

EID: 84870163047     PISSN: 09280987     EISSN: 18790720     Source Type: Journal    
DOI: 10.1016/j.ejps.2012.10.007     Document Type: Article

References (56)

1. P. Artursson, A.L. Ungell, and J.E. Löfroth Selective paracellular permeability in two models of intestinal absorption: cultured monolayers of human intestinal epithelial cells and rat intestinal segments Pharm. Res. 10 1993 1123 1129
2. P. Artursson, K. Palm, and K. Luthman Caco-2 monolayers in experimental and theoretical predictions of drug transport Adv. Drug Deliv. 22 1996 67 84
3. L.Z. Benet, T. Izumi, Y. Zhang, J.A. Silverman, and V.J. Wacher Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery J. Control Rel. 62 1999 25 31
4. S. Berggren, P. Lennernäs, M. Ekelund, B. Weström, J. Hoogstraate, and H. Lennernäs Regional transport and metabolism of ropivacaine and its CYP3A4 metabolite PPX in human intestine J. Pharm. Pharmacol. 55 2003 963 972
5. A. Buch, and W.H. Barr Absorption of propranolol in humans following oral, jejunal and ileal administration Pharm. Res. 15 1998 953 957
6. A. Collett, J. Tanianis-Hughes, G.L. Carlson, M.D. Harwood, and G. Warhurst Comparison of P-glycoprotein-mediated drug-digoxin interactions in Caco-2 with human and rodent intestine: relevance to in vivo prediction Eur. J. Pharm. Sci. 26 2005 386 393
7. A. Collett, R.H. Stephens, M.D. Harwood, M. Humphrey, L. Dallman, J. Bennett, J. Davis, G.L. Carlson, and G. Warhurst Investigation of regional mechanisms responsible for poor oral absorption in humans of a modified release preparation of the alpha-adrenoreceptor antagonist, 4-amino-6,7-dimethoxy-2-(5- methanesulfonamido-1,2,3,4-tetrahydroisoquinol-2-yl)-5-(2-pyridyl)- quinazoline (UK-338,003): the rational use of ex vivo intestine to predict in vivo absorption Drug Metab. Dispos. 36 1 2008 87 94
8. B.M. Fihn, A. Sjöqvist, and M. Jodal Involvement of enteric nerves in permeability changes due to deoxycholic acid in rat jejunum in vivo Acta Physiol. Scand. 178 2003 241 250
9. A. Galetin, and J.B. Houston Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: Impact on prediction of first-pass metabolism J. Pharmacol. Exp. Ther. 318 2006 1220 1229
10. I.S. Haslam, D.A. O'Reilly, D.J. Sherlock, A. Kauser, C. Womack, and T. Coleman Pancreatoduodenectomy as a source of human small intestine for Ussing chamber investigations and comparative studies with rat tissue Biopharm. Drug Dispos. 32 2011 210 221
11. R. Hayeshi, C. Hilgendorf, P. Artursson, P. Augustijns, B. Brodin, P. Dehertogh, K. Fisher, L. Fossati, E. Hovenkamp, T. Korjamo, C. Masungi, N. Maubon, R. Mols, A. Müllertz, J. Mönkkönen, C. O'Driscoll, H.M. Oppers-Tiemissen, E.G. Ragnarsson, M. Rooseboom, and A.L. Ungell Comparison of drug transporter gene expression and functionality in Caco-2 cells from 10 different laboratories Eur. J. Pharm. Sci. 35 2008 383 396
12. C. Hilgendorf, G. Ahlin, A. Seithel, P. Artursson, A.L. Ungell, and J. Karlsson Expression of thirty-six drug transporter genes in human intestine, liver, kidney, and organotypic cell lines Drug Metab. Dispos. 35 2007 1333 1340
13. M. Kuentz, S. Nick, N. Parrott, and D. Rothlisberger A strategy for preclinical formulation development using GastroPlus as pharmacokinetic simulation tool and a statistical screening design applied to a dog study Eur. J. Pharm. Sci. 27 2006 91 99
14. O. Kwon, P. Eck, S. Chen, C.P. Corpe, J.H. Lee, M. Kruhlak, and M. Levine Inhibition of the intestinal glucose transporter GLUT2 by flavonoids FASEB J. 21 2007 366 377
15. 2+/glucose co-transporter: re-evaluation of function and distribution of expression J. Biol. Chem. 269 1994 12032 12038
16. H. Lennernäs Human jejunal effective permeability and its correlation with preclinical drug absorption models J. Pharm. Pharmacol. 49 1997 627 638
17. H. Lennernäs Animal data: the contributions of the Ussing Chamber and perfusion systems to predicting human oral drug delivery in vivo Adv. Drug Deliv. Rev. 59 2007 1103 1120
18. J. Linnankoski, J. Makela, J. Palmgren, T. Mauriala, C. Vedin, A.L. Ungell, and M. Yliperttula Paracellular porosity and pore size of the human intestinal epithelium in tissue and cell culture models J. Pharm. Sci. 99 2010 2166 2175
19. M.L. Lucas, F.H. Lei, and J.A. Blair The influence of buffer pH, glucose and sodium ion concentration on the acid microclimate in rat proximal jejunum in vitro Pflugers Arch. 385 1980 137 142
20. V.D. Makhey, A. Guo, D.A. Norris, P. Hu, J. Yan, and P.J. Sinko Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells Pharm. Res. 15 1998 1160 1167
21. J.B. Meddings Lipid permeability of the intestinal microvillus membrane may be modulated by membrane fluidity in the rat Biochim. Biophys. Acta 984 1989 158 166
22. P. Nejdfors, M. Ekelund, B. Jeppsson, and B.R. Weström Mucosal in vitro permeability in the intestinal tract of the pig, the rat, and man: species- and region-related differences Scand. J. Gastroenterol. 35 2000 501 507
23. S. Neuhoff, A.L. Ungell, I. Zamora, and P. Artursson PH-dependent bidirectional transport of weakly basic drugs across Caco-2 monolayers: implications for drug-drug interactions Pharm. Res. 20 2003 1141 1148
24. S. Neuhoff, A.L. Ungell, I. Zamora, and P. Artursson PH-Dependent passive and active transport of acidic drugs across Caco-2 cell monolayers Eur. J. Pharm. Sci. 25 2005 211 220
25. T. Olbers, H. Lönroth, M. Fagevik-Olsen, and L. Lundell Laparoscopic gastric bypass: development of technique, respiratory function, and long-term outcome Obes. Surg. 13 2003 364 370
26. M.F. Paine, D.D. Shen, K.L. Kunze, J.D. Perkins, C.L. Marsh, J.P. McVicar, and K.E. Thummel First-pass metabolism of midazolam by the human intestine Clin. Pharmacol. Ther. 60 1996 14 24
27. K. Palm, K. Luthman, A.L. Ungell, G. Strandlund, and P. Artursson Correlation of drug absorption with molecular surface properties J. Pharm. Sci. 85 1996 32 39
28. N. Parrott, and T. Lave Applications of physiologically based absorption models in drug discovery and development Mol. Pharm. 5 2008 760 775
29. S.A. Peters, A.L. Ungell, and H. Dolgos Physiologically based pharmacokinetic (PBPK) modeling and simulation: applications in lead optimization Curr. Opin. Drug Discov. Devel. 12 2009 509 518
30. B.I. Polentarutti, A.L. Peterson, Å.K. Sjöberg, E.K. Anderberg, L.M. Utter, and A.L. Ungell Evaluation of viability of excised rat intestinal segments in the Ussing chamber: investigation of morphology, electrical parameters, and permeability characteristics Pharm. Res. 16 1999 446 454
31. C.G. Regardh, B. Edgar, R. Olsson, M. Kendall, P. Collste, and C. Shansky Pharmacokinetics of felodipine in patients with liver disease Eur. J. Clin. Pharmacol. 36 1989 473 479
32. V. Rozehnal, D. Nakai, U. Hoepner, T. Fischer, E. Kamiyama, M. Takahashi, and J. Mueller Human small intestinal and colonic tissue mounted in the Ussing chamber as a tool for characterizing the intestinal absorption of drugs Eur. J. Pharm. Sci. 46 2012 367 373
33. R.H. Stephens, C.A. O'Neill, A. Warhurst, G.L. Carlson, M. Rowland, and G. Warhurst Kinetic profiling of P-glycoprotein-mediated drug efflux in rat and human intestinal epithelia J. Pharmacol. Exp. Ther. 296 2001 584 591
34. S.M. Strasberg, J.A. Drebin, and N.J. Soper Evolution and current status of the Whipple procedure: an update for gastroenterologists Gastroenterology 113 1997 983 994
35. K.S. Sundell, and H. Sundh Intestinal fluid absorption in anadromous salmonids: importance of tight junctions and aquaporins Front. Physio. 3 2012 388
36. J.D. Söderholm, L. Hedman, P. Artursson, L. Franzen, J. Larsson, N. Pantzar, and G. Olaison Integrity and metabolism of human ileal mucosa in vitro in the Ussing chamber Acta Physiol. Scand. 162 1998 47 56
37. C. Tannergren, A. Bergendal, H. Lennernäs, and B. Abrahamsson Toward an increased understanding of the barriers to colonic drug absorption in humans: Implications for early controlled release candidate assessment Mol. Pharm. 6 2009 60 73
38. K. Thelen, K. Coboeken, S. Willmann, R. Burghaus, J. Dressman, and J. Lippert Evolution of a detailed physiological model to simulate the gastrointestinal transit and absorption process in humans, Part 1: Oral solutions J. Pharm. Sci. 100 2011 5324 5345
39. K.E. Thummel Gut instincts: CYP3A4 and intestinal drug metabolism J. Clin. Invest. 117 2007 3173 3176
40. K.E. Thummel, and D.D. Shen Design and optimization of dosage regimens: pharmacokinetic data Appendix II. In: Goodman & Gilman 10th Edition 2001 J.D. Hardman, L.E. Limbird, G.A. Gilman, The Pharmacological basis of Therapeutics 10th ed. 2001 The McGraw Hill Company Inc. 1917 2025
41. E.H. Ugelstad, C. Bundgaard, and H.M. Nielsen Evaluation of different toxicity assays applied to proliferating cells and to stratified epithelium in relation to permeability enhancement with glycocholate Toxicology 18 2004 649 657
42. A.L. Ungell, A. Andreasson, K. Lundin, and L. Utter Effects of enzymatic inhibition and increased paracellular shunting on transport of vasopressin analogues in the rat J. Pharm. Sci. 81 1992 640 645
43. A.L. Ungell In vitro absorption studies and their relevance to absorption from the GI tract Drug Develop Ind. Pharm. 23 1997 879 892
44. A.L. Ungell, S. Nylander, S. Bergstrand, Å. Sjöberg, and H. Lennernäs Membrane transport of drugs in different regions of the intestinal tract of the rat J. Pharm. Sci. 87 1998 360 366
45. A.L. Ungell, and B. Abrahamsson Biopharmaceutical support in candidate drug selection M. Gibson, Pharmaceutical Performulation and Formulation: A Practical Guide from Candidate Drug Selection to Commercial Dosage Form 2001 HIS Health Group Engelwood 97 143
46. A.L. Ungell Transport studies using intestinal tissue ex-vivo C.M. Lehr, Cell culture models of biological barriers; in vitro test systems for drug absorption and delivery 2002 Taylor&Francis NY 164 188
47. A.L. Ungell, and J. Karlsson Cell cultures in drug discovery: an industrial perspective H. van de Waterbeemd, H. Lennernäs, P. Artursson, Drug Bioavailability: Estimation of Solubility, Permeability, Absorption and Bioavailability 2003 Wiley-VCH Weinheim 90 131
48. A.L. Ungell Prediction of human drug absorption using in silico and in vitro techniques C. Pouton, Drug Candidate Optimization, Formulation and Early Development vol. 98 2005 Bulletin Technique-Gattefossé 19 31
49. A.L. Ungell, and P. Artursson An Overview of Caco-2 and Alternatives for Prediction of Intestinal Drug Transport and Absorption Drug Bioavailability 2009 Wiley-VCH Verlag GmbH & Co.; KGaA pp. 133-159
50. A.L. Ungell Preclinical evaluation of drug transport B.B. Steffansen, C.U. Nielsen, Molecular Biopharmaceutics; Aspects of Drug Characterization, Drug Delivery and Dosage Form Evaluation 2010 Pharmaceutical Press UK 225 247
51. H.H. Ussing, and K. Zerahn Active transport of sodium as the source of electric current in the short-circuited isolated frog skin Acta Physiol. Scand. 23 1951 110 127
52. E.G. van de Kerkhof, A.L. Ungell, Å.K. Sjöberg, M.H. de Jager, C. Hilgendorf, I.A. de Graaf, and G.M. Groothuis Innovative methods to study human intestinal drug metabolism in vitro: precision-cut slices compared with Ussing chamber preparations Drug Metab. Dispos. 34 2006 1893 1902
53. E.G. van de Kerkhof, I.A. de Graaf, and G.M. Groothuis In vitro methods to study intestinal drug metabolism Curr. Drug Metab. 8 2007 658 675
54. F. Verrey, E.I. Closs, C.A. Wagner, M. Palacin, H. Endou, and Y. Kanai CATs and HATs: the SLC7 family of amino acid transporters Plügers Arch. Eur J Physiol 447 2004 532 542
55. S. Wu-Pong, V. Livesay, B. Dvorchik, and W.H. Barr Oligonucleotide transport in rat and human intestine Ussing chamber models Biopharm. Drug Dispos. 20 1999 411 416
56. C. Zimmermann, H. Gutmann, P. Hruz, J.-P. Gutzwiller, C. Beglinger, and J. Drewe Mapping of multidrug resistance gene 1 and multidrug resistance-associated protein isoform 1 to 5 mRNA expression along the human intestinal tract Drug Metab. Dispos. 33 2005 219 224