Comparison between active and passive drug transport in human intestinal epithelial (Caco-2) cells in vitro and human jejunum in vivo

International Journal of Pharmaceutics

Volumn 127, Issue 1, 1996, Pages 103-107

  Lennernas H ^a   Palm, K ^a   Fagerholm, U ^a   Artursson, P ^a  

^a UPPSALA UNIVERSITY   (Sweden)

Author keywords

Caco 2 cell; Drug absorption; Drug transport; Human intestinal permeability; In vitro in vivo correlation; Membrane transport; Permeability coefficient

Indexed keywords

NAPROXEN;

ARTICLE; DRUG TRANSPORT; PRIORITY JOURNAL;

EID: 0030023536     PISSN: 03785173     EISSN: None     Source Type: Journal    
DOI: 10.1016/0378-5173(95)04204-0     Document Type: Article

References (20)

1. Amidon., G.L., Lennernäs, H., Shah, V. and Crison, J., Theoretical considerations in the correlation of in vitro drug product dissolution and in vivo bioavailability: A basis for a biopharmaceutics drug classification. Pharm. Res., 12 (1995) 413-420.
2. Artursson, P., Epithelial transport of drugs in cell culture I: A model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells. J. Pharm. Sci., 79 (1990) 476-482.
3. Artursson, P. and Karlsson, J., Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem. Biophys. Res. Comm., 3 (1991) 880-885.
4. Artursson, P., Ungell, A.-L. and Löfroth J.-E., 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.
5. Borgström, L., Nyberg, L., Jönsson, S., Lindberg, C. and Paulson, J., Pharmacokinetic evaluation in man of terbutaline given as separate enantiomers and as the racemate. Br. J. Clin. Pharmacol., 27 (1989) 49-56.
6. Chang, E.B. and Rao, M.C., Intestinal water and electrolyte transport: mechanisms of physiological and adaptive responses. In Johnson L.R. (Ed.), Physiology of the Gastrointestinal Tract, Raven Press, New York, 1994, pp. 2027-2081.
7. Clarke's Isolation and Identifying of Drugs, 2nd edition. Ed. A.C. Moffat. The Pharmaceutical Press, London (1986).
8. Eichelbaum, M., Ochs, H.R., Roberts, G. and Somogyi, A., Pharmacokinetics and metabolism of antipyrine (phenazone) after intravenous and oral administration. Arzneim.-Forsch., 32 (1982) 575-8.
9. Fagerholm, U., Borgström, L., Ahrenstedt, Ö., Lennernäs, H., The influence of net water absorption on the small intestinal permeability of terbutaline, studied in vivo in man. J. Drug Targeting., 3 (1995) 191-200.
10. Hu, M. and Borchardt, R.T., Mechanism of L-α-methyldopa transport through a monolayer of polarized human intestinal epithelial cells (Caco-2). Pharm. Res., 7 (1990) 1313-1319.
11. Karlsson, J. and Artursson, P., A method for the determination of cellular permeability coefficients and aqueous boundary layer thickness in monolayers of intestinal epithelial (Caco-2) cells grown in permeable filter chambers. Int. J. Pharm., 71 (1991) 55-64.
12. Lennernäs, H., Ahrenstedt, Ö., Hällgren, R., Knutson, L., Ryde, M. and Paalzow, L.K., Regional jejunal perfusion, a new in vivo approach to study oral drug absorption in man. Pharm. Res., 9 (1992) 1243-1251.
13. Lennernäs, H., Nilsson, D., Aquilonius, S.-M., Ahrenstedt, Ö., Knutson, L. and Paalzow, L.K., The effect of L-leucine on the absorption of levodopa, studied by regional jejunal perfusion in man. Br. J. Clin. Pharmacol., 35 (1993) 243-250.
14. Lennernäs, H., Ahrenstedt, Ö. and Ungell, A.-L., Intestinal drug absorption during induced net water absorption in man; A mechanistic study using antipyrine, atenolol and enalaprilat. Br. J. Clin. Pharmacol., 37 (1994) 589-596.
15. Lennernäs, H., Gastrointestinal absorption mechanisms: A comparison between animal and human models. Eur J. Pharm. Sci., 2 (1994) 39-43.
16. Martindale, 27th edition. Ed. A. Wade, The Pharmaceutical Press, London (1977).
17. Nyberg, L. Pharmacokinetic parameters of terbutaline in healthy man. An overview. Eur. J. Resp. Dis., 65 (1984) 149-60.
18. Sandberg, A. Extended-release metoprolol. Doctorial thesis, Uppsala (1994).
19. Therapeutic Drugs. Ed. Sir C. Dollery. Churchill Livingstone, New York (1991).
20. Yeh, K.C.H., August, T.F., Bush, D.F., Lasseter, K.C., Musson, D.G., Schwartz, S., Smith, M.E., and Titus, D.C., Pharmacokinetics and bioavailability of Sinemet CR: A summary of human studies. Neurol., 39 (1989) 25-35.