A study of intestinal absorption of bicyclol in rats: Active efflux transport and metabolism as causes of its poor bioavailability

Journal of Pharmacy and Pharmaceutical Sciences

Volumn 11, Issue 3, 2008, Pages 97-105

  Tan, Wei ^a   Chen, Hui ^a   Zhao, Jing ^a   Hu, Jinping ^a   Li, Yan ^a  

^a INSTITUTE OF MATERIA MEDICA   (China)

Author keywords

[No Author keywords available]

Indexed keywords

BICYCLOL; BIPHENYL DERIVATIVE; CYTOCHROME P450 3A; GLYCOPROTEIN P; UNCLASSIFIED DRUG;

ACTIVE TRANSPORT; ANIMAL; ARTICLE; BIOAVAILABILITY; CELL STRAIN CACO 2; DOSE RESPONSE; DRUG ANTAGONISM; HUMAN; INTESTINE ABSORPTION; MALE; METABOLISM; PERFUSION; PERMEABILITY; RAT; SPRAGUE DAWLEY RAT;

ANIMALS; BIOLOGICAL AVAILABILITY; BIOLOGICAL TRANSPORT, ACTIVE; BIPHENYL COMPOUNDS; CACO-2 CELLS; CYTOCHROME P-450 CYP3A; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; INTESTINAL ABSORPTION; MALE; P-GLYCOPROTEIN; PERFUSION; PERMEABILITY; RATS; RATS, SPRAGUE-DAWLEY;

EID: 58149105671     PISSN: None     EISSN: 14821826     Source Type: Journal    
DOI: 10.18433/j3b88v     Document Type: Article

References (25)

1. Yao, G.B., Xu, D. Zh., Lan, P., Xu, Ch.B., Wang, Ch., Luo, J., Shen, Y.M., Li, Q., Efficacy and safety of bicyclol in treatment of 2,200 chronic viral hepatitis. Chin J New Drugs Clin Rem, 24:421-426, 2005.
2. Liu, G.T., The anti-virus and hepatoprotective effect of bicyclol and its mechanism of action. Clin J New Drug, 10:325-327, 2001.
3. Li, Y., Li, Y., Liu, G.T., Protective effects of bicyclol on liver fibrosis induced by carbon tetrachloride. Chin Med J, 84:2096-2101, 2004.
4. Wang, H.P., and Li, Y., Protective effect of bicyclol on acute hepatic failure induced by lipopolysaccharide and D-galactosamine in mice. Eur J Pharmacol, 534:194-201, 2006.
5. Hu, Q.W., and Liu, G.T., Effects of bicyclol on dimethylnitrosamine-induced liver fibrosis in mice and its mechanism of action. Life Sci, 79:606-612, 2006.
6. Ju, M.H., Li, Y., Metabolism of bicyclol in rat and human liver microsomes in vitro. Acta Pharmaceutica Sinica 2005;2:111-116.
7. Thummel, K.E., Kunze, K.L., Shen, D.D., Enzyme-catalyzed processes of firstpass hepatic and intestinal drug extraction. Adv Drug Deliv Rev, 27:99-127, 1997.
8. Watkins, P.B., The barrier function of CYP3A4 and P-glycoprotein in the small bowel. Adv Drug Deliv Rev, 27:161-170, 1997.
9. Benet, L.Z., Cummins, C.L., The drug efflux-metabolism alliance: biochemical aspects. Adv Drug Deliv Rev, 50:S3-S11, 2001.
10. Johnson, B.M., Charman, W.N., Porter, C.J.H., The impact of P-glycoprotein efflux on enterocyte residence time and enterocyte-based metabolism of verapamil. J Pharm Pharmacol, 53:1611-1619, 2001.
11. Cummins, C.L., Jacobsen, W., Benet, L.Z., Unmasking the Dynamic Interplay between Intestinal P-Glycoprotein and CYP3A4. J Pharmacol Exp Ther, 300:1036-1045, 2002.
12. De, Waziers., Cugnenc, P.H., Yang, C.S., Leroux, J.P., Beaune, P.H., Cytochrome P450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extrahepatic tissues. J Pharmacol Exp Ther, 253:387-394, 1990.
13. Kolars, J.C., Lown, K.S., Schmiedlin, R.P., Ghosh, M., Fang, C., Wrighton, S.A., Merion, R.M., Watkins, P.B., CYP3A gene expression in human gut epithelium. Pharmacogenetics, 4:247-259, 1994.
14. Wacher, V.J., Silverman, J.A., Zhang, Y., Benet, L.Z., Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics. J Pharm Sci, 87:1322-1330, 1998.
15. Liu, Z, Q., Jiang, Z.H., Liu, L., Hu, M., Mechanisms responsible for poor oral bioavailability of paeoniflorin: role of intestinal disposition and interactions with sinomenine. Pharm Res, 12:2768-2780, 2006.
16. Hu, M., Chen, J., Tran, D., Zhu, Y., Leonardo, G., The Caco-2 cell monolayers as an intestinal metabolism model: metabolism of dipeptide Phe-Pro. J. Drug. Target, 2:79-89, 1994.
17. Hu, M., Chen, J., Zhu, Y., Dantzig, AH., Stratford, J.R., Kuhfeld, M.T. Mechanism and kinetics of transcellular transport of a new β-lactam antibiotic loracarbef across an human intestinal epithelial model system (Caco-2). Pharm Res (NY), 11:1405-1413, 1994.
18. Johnson, B.M., Chen, W.Q., Borchardt, R.T., Charman, W.N., Porter, C.J.H., A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum. J Pharmacol Exp Ther 305:151-158, 2003.
19. Singhal, D., Ho, NF., Anderson, B.D., Absorption and intestinal metabolism of purine dideoxynucleosides and an adenosine deaminase-activated prodrug of 2',3'-dideoxyinosine in the mesenteric vein cannulated rat ileum. J Pharm Sci, 87:569-577, 1998.
20. 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 Commun, 175:880-885, 1991.
21. Yee, S., In vitro permeability across Caco-2 cells (colonic) can predict in vivo (small intestinal) absorption in manVfact or myth. Pharm Res, 14:763-766, 1997.
22. Cummins, C.L., Salphati, L., Reid, M.J., Benet, L.Z., In Vivo Modulation of Intestinal CYP3A Metabolism by P-Glycoprotein: Studies Using the Rat Single-Pass Intestinal Perfusion Model. J Pharmacol Exp Ther, 305:306-314, 2003.
23. Zhang, L., Lin, G., Chang, Q., Zuo, Z., Role of intestinal first-pass metabolism of baicalein in its absorption process. Pharm Res, 7:1050-1058, 2005.
24. Jeong, E.J., Liu, Y., Lin, H., Hu, M., In situ single-pass perfused rat intestinal model for absorption and metabolism. In Z. Yan and G. W. Caldwell (eds.), In Methods in Pharmacology and Toxicology: Optimization in Drug Discovery-In Vitro Methods, Human, Totowa, NJ, pp. 65-76, 2004.
25. Wang, Y., Aun, R., Tse, F.L., 1 Absorption of D-glucose in the rat studied using in situ intestinal perfusion: a permeability-index approach. Pharm Res, 14:1563-1567, 1997.