Determining intestinal metabolism and permeability for several compounds in rats. Implications on regional bioavailability in humans

Pharmaceutical Research

Volumn 13, Issue 1, 1996, Pages 108-113

  Sinko, Patrick J ^a   Hu, Peidi ^b  

^a RUTGERS UNIVERSITY   (United States)

^b NONE

Author keywords

Bioavailability; Captopril; Didanosine; Intestinal permeability; Mannitol; Metabolism; Ofloxacin; Regional oral absorption; Site specific; Zidovudine

Indexed keywords

CAPTOPRIL; DIDANOSINE; MANNITOL; OFLOXACIN; ZIDOVUDINE;

ANIMAL TISSUE; ARTICLE; BIOAVAILABILITY; CONTROLLED STUDY; DRUG METABOLISM; FEMALE; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; INTESTINE PERFUSION; NONHUMAN; PRIORITY JOURNAL; RAT; TISSUE HOMOGENATE; ANIMAL; HUMAN; MALE; METABOLISM; PERMEABILITY; SMALL INTESTINE; SPRAGUE DAWLEY RAT;

ANIMALS; BIOLOGICAL AVAILABILITY; CAPTOPRIL; DIDANOSINE; HUMANS; INTESTINE, SMALL; MALE; MANNITOL; OFLOXACIN; PERMEABILITY; RATS; RATS, SPRAGUE-DAWLEY; ZIDOVUDINE;

EID: 0029664578     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1016041620024     Document Type: Article

References (26)

1. D. W. Powell. Intestinal water and electrolyte transport. In L. R. Johnson (ed.). Physiology of the Gastrointestinal Tract, Raven Press, New York, 1987, pp. 1267-1306.
2. G.-B. Park and A. K. Mitra. Mechanism and Site Dependency of Intestinal Mucosal Transport and Metabolism of Thymidine Analogues. Pharm. Res. 9:326-331 (1992).
3. S. L. Bramer, J. L.-S. Au and M. G. Wientjes. Gastrointestinal and hepatic first pass elimination of 2′,3′-dideoxyinosine. J. Pharmacol. Exp. Ther. 265:731-738 (1993).
4. P. J. Sinko, P. Hu and N. R. Patel. Site-Specific Oral Absorption of Didanosine: In Situ Characterization and Correlation with Extent of Absorption In Vivo. Int. J. Pharm. 109:125-133, (1994).
5. M. L. Stolz, M. El-hawari and L. Litle. Pharmacokinetics and Bioavailability of 2′,3′-Dideoxynucleoside Anti-AIDS Agents in Beagle Dogs. Proc. Am. Assoc. Cancer Res. 30:535 (1989).
6. Y. Seta, F. Higuchi, Y. Kawahara, K. Nishimura and R. Okada. Design and preparation of captopril sustained-release dosage forms and their biopharmaceutical properties. Int. J. Pharm. 41:245-254 (1988).
7. J. Brennan, D. O'Donnell, M. Zinny, N. Jain, E. Ivashkiv and M. Arnold. The Comparative Bioavailability of Captopril after Colonie Infusion and Oral Administration in Healthy Subjects. Clin. Pharmacol. and Ther. 49:131 (1991).
8. N. R. Hartman, R. Yarchoan, J. M. Pluda, et al. Pharmacokinetics of 2′,3′-Dideoxyinosine in Patients with Severe Human Immunodeficiency Infection. II. The Effects of Different Oral Formulations and the Presence of Other Medications. Clin. Pharmacol. Ther. 50:278-285 (1991).
9. I. R. Wilding, S. S. Davis, M. Bakhshee, H. N. E. Stevens, R. A. Sparrow and J. Brennan. Gastrointestinal transit and systemic absorption of captopril from a pulsed release dosage form. Pharm. Res. 9:654-657 (1992).
10. D. A. Johnson and G. L. Amidon. Determination of intrinsic membrane transport parameters from perfused intestine experiments: A boundary layer approach to estimating the aqueous and unbiased membrane permeabilities. J. Theor. Biol. 131:93-106 (1988).
11. H. Yuasa, D. Fleisher and G. L. Amidon. Noncompetitive inhibition of cephradine uptake by enalapril in rabbit intestinal brush-border membrane vesicles: An enalapril specific inhibitory binding site on the peptide carrier. J. Pharmacol. Exp. Ther. 269:1107-1111 (1994).
12. Worthington Enzymes Manual. L. A. Decker (ed.), Worthington Biochemical Corporation, Freehold, NJ, pp. 19-22 (1977).
13. S. P. Colowick, N. O. Kaplan and B. Mackler. In: Methods in Enzymology: Oxidation and Phosphorylation, R. W. Estabrook and M. E. Pullman (eds), Academic Press, NY, NY page 551 (1967).
14. H. D. Tisdale. In: Methods in Enzymology: Oxidation and Phosphorylation, R. W. Estabrook and M. E. Pullman (eds.), Academic Press, NY, NY page 213 (1967).
15. H.-H. Lu, P. J. Sinko, and D. Fleisher. Fed-state zidovudine-absorption. AIDS, 5:907-908 (1991).
16. J. Diamond and W. Bossert. Standing-gadient osmotic flow. A mechanism for coupling of water and solute transport in epithelia. J. Gen. Physiol. 50:2061-2083 (1967).
17. M. Hu and G. L. Amidon. Passive and carrier-mediated intestinal absorption components of captopril. J. Pharm. Sci. 77:1007-1011 (1988).
18. J. A. Romankiewicz, R. N. Brogden, R. C. Heel, T. M. Speight and G. S. Avery. Captopril: An update review of its pharmacological properties and therapeutic efficacy in congestive heart failure. Drugs 25:6-40 (1983).
19. S. H. Kubo and R. J. Cody. Clinical pharmacokinetics of the angiotensin converting enzyme inhibitors: A review. Clin. Pharmacokinet. 10:377-391 (1985).
20. G. L. Amidon, P. J. Sinko and D. Fleisher. Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier mediated compounds. Pharm. Res. 5:651-654 (1988).
21. W. Hindle and C. F. Code. Some differences between duodenal and ileal sorption. Am. J. Physiol. 203:215-220 (1962).
22. G. R. Davis, C. A. Santa Ana, S. G. Morawski and J. S. Fordtran. Permeability characteristics of human jejunum, ileum, proximal colon and distal colon: Results of potential difference measurements and unidirectional fluxes. Gastro. 83:844-850 (1982).
23. J. S. Fordtran, F. C. Rector, M. F. Ewton, N. Sotor and J. Kinney. Permeability characteristics of the human small intestine. J. Clin. Invest. 44:1935-1944 (1965).
24. K. D. Peck, A. H. Ghanem and W. I. Higuchi. Hindered diffusion of polar molecules through and effective pore radii estimates of intact and ethanol treated human epidermal membrane. Pharm. Res. 11:1306-14 (1994).
25. 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. 10:1123-1129 (1993).
26. N. Jezyk, W. Rubas and G. M. Grass. Permeability characteristics of various intestinal regions of rabbit, dog and monkey. Pharm. Res. 9:1580-1586 (1992).