Development of an in vitro rat intestine segmental perfusion model to investigate permeability and predict oral fraction absorbed

Pharmaceutical Research

Volumn 23, Issue 7, 2006, Pages 1543-1553

  Castella, Marc Etienne ^a   Reist, Marianne ^a   Mayer, Joachim M ^a   Turban, Jean Jacques ^a   Testa, Bernard ^b   Boursier Neyret, Claire ^c   Walther, Bernard ^c   Delbos, Jean Marie ^c   Carrupt, Pierre Alain ^a  

^a UNIVERSITY OF GENEVA   (Switzerland)

^b LAUSANNE UNIVERSITY HOSPITAL   (Switzerland)

^c INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

Absorption model; In vitro intestinal metabolism; In vitro intestinal permeability; In vitro in vivo correlation; Rat jejunal perfusion

Indexed keywords

ATENOLOL; DRUG METABOLITE; LUCIFER YELLOW; MACROGOL 4000; MANNITOL; NADOLOL; NAPROXEN; NORVERAPAMIL; PHENAZONE; TESTOSTERONE; VERAPAMIL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONTROLLED STUDY; CORRELATION COEFFICIENT; DEMETHYLATION; DRUG ABSORPTION; DRUG METABOLISM; DRUG PENETRATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; INTESTINE MUCOSA PERMEABILITY; INTESTINE PERFUSION; MALE; MODEL; NONHUMAN; PREDICTION; PRIORITY JOURNAL; RAT; STANDARD;

ANIMALS; ANTIPYRINE; DEALKYLATION; INTESTINAL ABSORPTION; JEJUNUM; MALE; MODELS, ANIMAL; NAPROXEN; PERFUSION; PERMEABILITY; PHARMACEUTICAL PREPARATIONS; RATS; RATS, SPRAGUE-DAWLEY; TESTOSTERONE; VERAPAMIL;

EID: 33745603186     PISSN: 07248741     EISSN: 1573904X     Source Type: Journal    
DOI: 10.1007/s11095-006-0249-y     Document Type: Article

References (48)

1. J. J. Tukker 1996 In vitro methods for the assessment of permeability J. B. Dressman H. Lennernäs Oral Drug Absorption-Prediction and Assessment Vol. 106 Marcel Dekker Inc. New York 51 72
2. K. Koga M. Murakami S. Kawashima 1998 Effects of fatty acid sucrose esters on ceftibuten transport by rat intestinal brush-border membrane vesicles Biol. Pharm. Bull. 21 747 751
3. I. J. Hidalgo T. J. Raub R. T. Borchardt 1989 Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability Gastroenterology 96 736 749
4. P. Artursson R. T. Borchardt 1997 Intestinal drug absorption and metabolism in cell cultures: Caco-2 and beyond Pharm. Res. 14 1655 1658
5. J. D. Irvine L. Takahashi K. Lockhart J. Cheong J. W. Tolan H. E. Selick J. R. Grove 1999 MDCK (Madin-Darby canine kidney) cells: a tool for membrane permeability screening J. Pharm. Sci. 88 28 33
6. A. Braun S. Hämmerle K. Suda B. Rothen-Rutishauser M. Günthert S. D. Kramer H. Wunderli-Allenspach 2000 Cell culture as tools in biopharmacy Eur. J. Pharm. Sci. 11 S51 S60
7. L. Barthe J. F. Woodley S. Kenworthy G. Houin 1998 An improved everted gut sac as a simple and accurate technique to measure paracellular transport across the small intestine Eur. J. Drug Metab. Pharmacokinet. 23 313 323
8. Z. T. Chowhan A. A. Amaro 1977 Everted rat intestinal sacs as an in vitro model for assessing absorptivity of new drugs J. Pharm. Sci. 66 1249 1253
9. A. L. Ungell S. Nylander S. Bergstrand A. Sjoberg H. Lennernäs 1998 Membrane transport of drugs in different regions of the intestinal tract of the rat J. Pharm. Sci. 87 360 366
10. P. L. Smith 1996 Methods for evaluating intestinal permeability and metabolism in vitro R. T. Borchardt P. L. Smith G. Wilson Models for Assessing Drug Absorption and Metabolism Vol. 8 Plenum New York 13 34
11. H. Lennernäs S. Nylander A. L. Ungell 1997 Jejunal permeability: a comparison between the Ussing chamber technique and the single-pass perfusion in humans Pharm. Res. 14 667 671
12. L. Salphati K. Childers L. Pan K. Tsutsui L. Takahashi 2001 Evaluation of a single-pass intestinal-perfusion method in rat for the prediction of absorption in man J. Pharm. Pharmacol. 53 1007 1013
13. K. Palm P. Artursson K. Luthman 1997 Experimental and theoretical predictions of intestinal drug absorption H. van de Waterbeemd B. Testa G. Folkers Computer-Assisted Lead Finding and Optimization Wiley-VCH Weinheim 277 289
14. Y. H. Zhao M. H. Abraham J. Le A. Hersey C. N. Luscombe G. Beck B. Sherborne I. Cooper 2003 Evaluation of rat intestinal absorption data and correlation with human intestinal absorption Eur. J. Med. Chem. 38 233 243
15. G. L. Amidon P. J. Sinko D. Fleisher 1988 Estimating human oral fraction dose absorbed: a correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds Pharm. Res. 5 651 654
16. B. M. Johnson W. N. Charman C. J. Porter 2003 Application of compartmental modelling to an examination of in vitro intestinal permeability data: assessing the impact of tissue uptake, p-glycoprotein, and CYP3A Drug Metab. Dispos. 31 1151 1160
17. B. M. Johnson W. N. Charman C. J. Porter 2001 The impact of p-glycoprotein efflux on enterocyte residence time and enterocyte-based metabolism of verapamil J. Pharm. Pharmacol. 53 1611 1619
18. B. M. Johnson W. N. Charman C. J. Porter 2002 An in vitro examination of the impact of polyethylene glycol 400, pluronic P85 and vitamin E d-a-tocopheryl polyethylene glycol 1000 succinate on p-glycoprotein efflux and enterocyte-based metabolism in excised rat intestine AAPS Pharm. Sci. 4 E40
19. R. Sandstrom H. Lennernäs 1999 Repeated oral rifampicin decreases the jejunal permeability of R/S-verapamil in rats Drug Metab. Dispos. 27 951 955
20. B. M. Johnson W. Chen R. T. Borchardt W. N. Charman C. J. Porter 2002 A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum J. Pharmacol. Exp. Ther. 305 151 158
21. U. Fagerholm M. Johansson H. Lennernäs 1996 Comparison between permeability coefficients in rat and human jejunum Pharm. Res. 13 1336 1342
22. M. E. Dowty C. R. Dietsch 1997 Improved prediction of in vivo peroral absorption from in vitro intestinal permeability using an internal standard to control for intra- and inter-rat variability Pharm. Res. 14 1792 1797
23. Y. Konishi K. Hagiwara M. Shimizu 2002 Transepithelial transport of fluorescein in Caco-2 cell monolayers and use of such transport in in vitro evaluation of phenolic acid availability Biosci. Biotechnol. Biochem. 66 2449 2457
24. G. L. Amidon H. Lennernäs V. P. Shah J. R. Crison 1995 A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability Pharm. Res. 12 413 420
25. S. Winiwarter N. M. Bonham F. Ax A. Hallberg H. Lennernäs A. Karlen 1998 Correlation of human jejunal permeability (in vivo) of drugs with experimentally and theoretically derived parameters. A multivariate data analysis approach J. Med. Chem. 41 4939 4949
26. C. A. Bergström M. Strafford L. Lazorova A. Avdeef K. Luthman P. Artursson 2003 Absorption classification of oral drugs based on molecular surface properties J. Med. Chem. 46 558 570
27. G. W. Caldwell S. M. Easlick J. Gunnet J. A. Masucci K. Demarest 1998 In vitro permeability of eight beta-blockers through Caco-2 monolayers utilizing liquid chromatography/electrospray ionization mass spectrometry J. Mass Spectrom. 33 607 614
28. S. Yamashita Y. Tanaka Y. Endoh Y. Taki T. Sakane T. Nadai H. Sezaki 1997 Analysis of drug permeation across Caco-2 monolayer: implication for predicting in vivo drug absorption Pharm. Res. 14 486 491
29. J. R. Pappenheimer C. C. Michel 2003 Role of villus microcirculation in the intestinal absorption of glucose: coupling of epithelial with endothelial transport J. Physiol. 553 561 574
30. B. I. Polentarutti A. L. Peterson A. K. Sjoberg E. K. Anderberg L. M. Utter A. L. Ungell 1999 Evaluation of viability of excised rat intestinal segments in the Ussing chamber: investigation of morphology, electrical parameters, and permeability characteristics Pharm. Res. 16 446 454
31. J. Kalitsky-Szirtes A. Shayeganpour D. R. Brocks M. Piquette-Miller 2004 Suppression of drug-metabolizing enzymes and efflux transporters in the intestine of endotoxin-treated rats Drug Metab. Dispos. 32 20 27
32. Y. H. Wang D. R. Jones S. D. Hall 2004 Prediction of cytochrome P450 3A inhibition by verapamil enantiomers and their metabolites Drug Metab. Dispos. 32 259 266
33. J. C. Kolars P. Schmiedlin-Ren W. O. Dobbins J. Schuetz S. A. Wrighton P. B. Watkins 1992 Heterogeneity of cytochrome P450 3A expression in rat gut epithelia Gastroenterology 102 1186 1198
34. M. J. Ginski J. E. Polli 1999 Prediction of dissolution-absorption relationships from a dissolution/Caco-2 system Int. J. Pharm. 177 117 125
35. M. Kobayashi N. Sada M. Sugawara K. Iseki K. Miyazaki 2001 Development of a new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract Int. J. Pharm. 221 87 94
36. X. He M. Sugawara M. Kobayashi Y. Takekuma K. Miyazaki 2003 An in vitro system for prediction of oral absorption of relatively water-soluble drugs and ester prodrugs Int. J. Pharm. 263 35 44
37. M. Kataoka Y. Masaoka Y. Yamasaki T. Sakane H. Sezaki S. Yamashita 2003 In vitro system to evaluate oral absorption of poorly water-soluble drugs: simultaneous analysis on dissolution and permeation of drugs Pharm. Res. 20 1674 1680
38. F. Meriani N. Coceani C. Sirotti D. Voinovich M. Grassi 2003 In vitro nimesulide absorption from different formulations J. Pharm. Sci. 93 540 552
39. C. Zhu L. Jiang T. M. Chen K. K. Hwang 2002 A comparative study of artificial membrane permeability assay for high-throughput profiling of drug absorption potential Eur. J. Med. Chem. 37 399 407
40. P. Artursson J. Karlsson 1991 Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells Biochem. Biophys. Res. Commun. 175 880 885
41. K. Tsutsumi S. K. Li A. H. Ghanem N. F. Ho W. I. Higuchi 2003 A systematic examination of the in vitro Ussing chamber and the in situ single-pass perfusion model systems in rat ileum permeation of model solutes J. Pharm. Sci. 92 344 359
42. M. Eichelbaum H. R. Ochs G. Roberts A. Somogyi 1982 Pharmacokinetics and metabolism of antipyrine (phenazone) after intravenous and oral administration Arzneim.-Forsch. 32 575 578
43. G. Bouchard P. A. Carrupt B. Testa V. Gobry H. H. Girault 2002 Lipophilicity and solvation of anionic drugs Chem. Eur. J. 8 3478 3484
44. G. Caron G. Steyaert A. Pagliara F. Reymond P. Crivori P. Gaillard P. A. Carrupt A. Avdeef J. Comer K. J. Box H. H. Girault B. Testa 1999 Structure-lipophilicity relationships of neutral and protonated β-blockers. Part I. Intra- and intermolecular effects in isotropic systems Helv. Chim. Acta 82 1211 1222
45. W. L. Chiou A. Barve 1998 Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rats Pharm. Res. 15 1792 1795
46. S. M. Nasrallah F. L. Iber 1969 Mannitol absorption and metabolism in man Am. J. Med. Sci. 258 80 88
47. F. Ingels B. Beck M. Oth P. Augustijns 2004 Effect of simulated intestinal fluid on drug permeability estimation across Caco-2 monolayers Int. J. Pharm. 274 221 232
48. J. Dreyfuss J. M. Shaw J. J. Ross 1978 Absorption of the beta-adrenergic-blocking agent, nadolol, by mice, rats, hamsters, rabbits, dogs, monkeys, and man: an unusual species difference Xenobiotica 8 503 508