Intestinal permeability of metformin using single-pass intestinal perfusion in rats

World Journal of Gastroenterology

Volumn 12, Issue 25, 2006, Pages 4064-4070

  Song, Nai Ning ^a,b   Li, Quan Sheng ^b   Liu, Chang Xiao ^b  

^a TIANJIN UNIVERSITY   (China)

^b The State Key Laboratories of Pharmacodynamics and Pharmacokinetics   (China)

Author keywords

Intestinal permeability; Metformin; P glycoprotein; RP HPLC; Single pass intestinal perfusion

Indexed keywords

GLYCOPROTEIN P; METFORMIN; VERAPAMIL;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG ABSORPTION; DRUG PENETRATION; DRUG POTENTIATION; DUODENUM; ILEUM; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; INTESTINE PERFUSION; JEJUNUM; MALE; NONHUMAN; PREDICTION; RAT; RAT STRAIN; TISSUE HOMOGENATE;

EID: 33746217592     PISSN: 10079327     EISSN: None     Source Type: Journal    
DOI: 10.3748/wjg.v12.i25.4064     Document Type: Article

References (36)

1. Dunn CJ, Peters DH. Metformin. A review of its pharmacological properties and therapeutic use in non-insulin-dependent diabetes mellitus. Drugs 1995; 49: 721-749
2. Tucker GT, Casey C, Phillips PJ, Connor H, Ward JD, Woods HF. Metformin kinetics in healthy subjects and in patients with diabetes mellitus. Br J Clin Pharmacol 1981; 12: 235-246
3. Vidon N, Chaussade S, Noel M, Franchisseur C, Huchet B, Bernier JJ. Metformin in the digestive tract. Diabetes Res Clin Pract 1988; 4: 223-229
4. Fojo AT, Ueda K, Slamon DJ, Poplack DG, Gottesman MM, Pastan I. Expression of a multidrug-resistance gene in human tumors and tissues. Proc Natl Acad Sci USA 1987; 84: 265-269
5. Thiebaut F, Tsuruo T, Hamada H, Gottesman MM, Pastan I, Willingham MC. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc Natl Acad Sci USA 1987; 84: 7735-7738
6. Terao T, Hisanaga E, Sai Y, Tamai I, Tsuji A. Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier. J Pharm Pharmacol 1996; 48: 1083-1089
7. Greiner B, Eichelbaum M, Fritz P, Kreichgauer HP, von Richter O, Zundler J, Kroemer HK. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J Clin Invest 1999; 104: 147-153
8. Ambudkar SV, Dey S, Hrycyna CA, Ramachandra M, Pastan I, Gottesman MM. Biochemical, cellular, and pharmacological aspects of the multidrug transporter. Annu Rev Pharmacol Toxicol 1999; 39: 361-398
9. Williams GC, Sinko PJ. Oral absorption of the HIV protease inhibitors: a current update. Adv Drug Deliv Rev 1999; 39: 211-238
10. Saitoh H, Aungst BJ. Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine. Pharm Res 1995; 12: 1304-1310
11. Cutler DJ. Theory of the mean absorption time, an adjunct to conventional bioavailability studies. J Pharm Pharmacol 1978; 30: 476-478
12. Sinko PJ, Hu P, Waclawski AP, Patel NR. Oral absorption of anti-AIDS nucleoside analogues. 1. Intestinal transport of didanosine in rat and rabbit preparations. J Pharm Sci 1995; 84: 959-965
13. Svensson US, Sandstrom R, Carlborg O, Lennernas H, Ashton M. High in situ rat intestinal permeability of artemisinin unaffected by multiple dosing and with no evidence of P-glycoprotein involvement. Drug Metab Dispos 1999; 27: 227-232
14. Amidon GL, Kou J, Elliott RL, Lightfoot EN. Analysis of models for determining intestinal wall permeabilities. J Pharm Sci 1980; 69: 1369-1373
15. Komiya I, Park JY, Kamaani A, Ho NFH, Higuchi WI. Quantitative mechanistic studies in simultaneous fluid flow and intestinal absorption using steroids as model solutes. Int. J. Pharmaceutics 1980; 4: 249-262
16. Fagerholm U, Johansson M, Lennernas H. Comparison between permeability coefficients in rat and human jejunum. Pharm Re 1996; 13: 1336-1342
17. Kararli TT. Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos 1995; 16: 351-380
18. Lipinski CA, Lombardo F, Dominy BW, Feeney PJ. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev 2001; 46: 3-26
19. Knipp GT, Ho NF, Barsuhn CL, Borchardt RT. Paracellular diffusion in Caco-2 cell monolayers: effect of perturbation on the transport of hydrophilic compounds that vary in charge and size. J Pharm Sci 1997; 86: 1105-1110
20. Amidon GL, Lennernas H, Shah VP, Crison JR. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res 1995; 12: 413-420
21. Lennernas H, Nylander S, Ungell A-L. Jejunal permeability: a comparison between the ussing chamber technique and the single-pass perfusion in humans. Pharm Res 1997; 14: 667-671
22. Lennernas H. Human jejunal effective permeability and its correlation with preclinical drug absorption models. J Pharm Pharmacol 1997; 49: 627-638
23. Kimura T, Higaki K. Gastrointestinal transit and drug absorption. Biol Pharm Bull 2002; 25: 149-164
24. Yamashita S, Furubayashi T, Kataoka M, Sakane T, Sezaki H, Tokuda H. Optimized conditions for prediction of intestinal drug permeability using Caco-2 cells. Eur J Pharm Sci 2000; 10: 195-204
25. Hogerle ML, Winne D. Drug absorption by the rat jejunum perfused in situ. Dissociation from the pH-partition theory and role of microclimate-pH and unstirred layer. Naunyn Schmiedebergs Arch Pharmacol 1983; 322: 249-255
26. Shiau YF, Fernandez P, Jackson MJ, McMonagle S. Mechanisms maintaining a low-pH microclimate in the intestine. Am J Physiol 1985; 248: G608-617
27. Ungell AL, Nylander S, Bergstrand S, Sjoberg A, Lennernas H. Membrane transport of drugs in different regions of the intestinal tract of the rat. J Pharm Sci 1998; 87: 360-366
28. Hakkak R, Ronis MJ, Badger TM. Effects of enteral nutrition and ethanol on cytochrome P450 distribution in small intestine of male rats. Gastroenterology 1993; 104: 1611-1618
29. Zhang QY, Wikoff J, Dunbar D, Kaminsky L. Characterization of rat small intestinal cytochrome P450 composition and inducibility. Drug Metab Dispos 1996; 24: 322-328
30. Makhey VD, Guo A, Norris DA, Hu P, Yan J, Sinko PJ. Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells. Pharm Res 1998; 15: 1160-1167
31. Chiou WL, Barve A. Linear correlation of the fraction of oral dose absorbed of 64 drugs between humans and rats. Pharm Res 1998; 15: 1792-1795
32. Lennernas H. Human intestinal permeability. J Pharm Sci 1998; 87: 403-410
33. Amidon GL, Sinko PJ, Fleisher D. Estimating human oral fraction dose absorbed: a correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds. Pharm Res 1988; 5: 651-654
34. Amnon H, David S, Eran L, Sara E, Eytan K, Michael F. Pharmacokinetic and Pharmaco- dynamic aspects of gastroretentive dosage forms. Int J Pharm 2004; 277: 141-153
35. Pentikainen PJ, Neuvonen PJ, Penttila. A. Pharmacokinetics of metformin after intravenous and oral administration to man. Eur J Clin Pharmacol 1979; 16: 195-202
36. Gusler G, Gorsline J, Levy G, Zhang SZ, Weston IE, Naret D, Berner B. Pharmacokinetics of metformin gastric-retentive tablets in healthy volunteers. J Clin Pharmacol 2001; 41: 655-661