Does the well-stirred model the intestinal first-pass effect well?

Journal of Pharmacy and Pharmacology

Volumn 56, Issue 12, 2004, Pages 1597-1599

  Mizuma, Takashi ^a   Tsuji, Akira ^b   Hayashi, Masahiro ^a  

^a TOKYO UNIVERSITY OF PHARMACY AND LIFE SCIENCES   (Japan)

^b KANAZAWA UNIVERSITY   (Japan)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 2D6; METOPROLOL; DRUG;

ARTICLE; CALCULATION; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG METABOLISM; FIRST PASS EFFECT; INTESTINE; LIVER; MEMBRANE TRANSPORT; MICROSOME; MODEL; BIOLOGICAL MODEL; COMPARATIVE STUDY; DRUG EFFECT; INTESTINE ABSORPTION; METABOLIC CLEARANCE RATE; METABOLISM; PHYSIOLOGY;

INTESTINAL ABSORPTION; METABOLIC CLEARANCE RATE; MODELS, BIOLOGICAL; PHARMACEUTICAL PREPARATIONS;

EID: 16644403480     PISSN: 00223573     EISSN: None     Source Type: Journal    
DOI: 10.1211/0022357044850     Document Type: Article

References (14)

1. Benet, L. Z., Oie, S., Schwartz, J. B. (1996) Design and optimization of dosage regimens: pharmacokinetic data. In: Hardman, J. G., Limbard, L. E., Molinoff, P. B., Rudden, R. W., Gilman, A. G. (eds). The Pharmacological basis of therapeutics, 9th edn. McGraw-Hill, New York, pp 1707-1792
2. Chiba, M., Hensleigh, M., Lin, J. H. (1997) Hepatic and intestinal metabolism of indinavir, an HIV protease inhibitor, in rat and human microsomes. Biochem. Pharmacol. 53: 1187-1195
3. Gibaldi, M., Perrier, D. (1982) Pharmacokinetics. Marcel Dekker, New York, pp 319-353
4. Hulten, L., Lindhagen, J., Lundgren, O. (1977) Sympathetic nervous control of intramural blood flow in the feline and human intestines. Gastroenterology 72: 41-48
5. Klippert, P., Borm, P., Noordhoek, J. (1982) Prediction of intestinal first-pass effect of phenacetin in the rat from enzyme kinetic data - correlation with in vivo data using mucosal blood flow. Biochem. Pharmacol. 31: 2545-2548
6. 2-sympathomimetics in isolated rat intestinal epithelial cells. Drug Metab. Dispos. 13: 232-238
7. Lennernas, H., Lee, I.-D., Fagerholm, U., Amidon, G. L. (1997) A residence-time distribution analysis of the hydrodynamics within the intestine in man during a regional single-pass perfusion with Loc-I-Gut: in vivo permeability estimation. J. Pharm. Pharmacol. 49: 682-686
8. Madani, S., Paine, M. F., Lewis, L., Thummel, K. E., Shen, D. D. (1999) Comparison of CYP2D6 content and metoprolol oxidation between microsomes isolated from human livers and small intestines. Pharm. Res. 16: 1199-1205
9. Mistry, M., Houston, B. (1987) Glucuronidation in vitro and in vivo. Comparison of intestinal and hepatic conjugation of morphine, naloxone and buprenorphine. Drug Metab. Dispos. 15: 710-717
10. Mizuma, T. (2002) Kinetic impact of presystemic intestinal metabolism on drug absorption: experiment and data analysis for the prediction of in vivo absorption from in vitro data. Drug Metab. Pharmacokinet. 17: 496-506
11. Mizuma, T., Ohta, K., Koyanaagi, A., Awazu, S. (1996) Improvement of intestinal absorption of leucine enkephalin by sugar coupling and peptide inhibitors. J. Pharm. Sci. 85: 854-857
12. Rowland, M., Tozer, T. N. (1995) Clinical pharmacokinetics. Williams & Willkins, Philadelphia, pp 119-136
13. Thummel, K. E., Kunze, K. L., Shen, D. D. (1997) Enzyme-catalyzed processes of first-pass hepatic and intestinal drug extraction. Adv. Drug Deliv. Rev. 27: 99-127
14. Wacher, V. J., Silverman, J. A., Zhang, Y., Benet, L. Z. (1998) Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J. Pharm. Sci. 87: 1322-1330