Factors influencing regional differences in intestinal absorption of UK-343,664 in Rat: Possible role in dose-dependent pharmacokinetics

Journal of Pharmaceutical Sciences

Volumn 95, Issue 2, 2006, Pages 435-445

  Kaddoumi, Amal ^a   Fleisher, David ^b   Heimbach, Tycho ^c   Li, Lilian Y ^d   Cole, Susan ^e  

^a UNIVERSITY OF WASHINGTON   (United States)

^b UNIVERSITY OF MICHIGAN   (United States)

^c PFIZER INC   (United States)

^d PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United States)

^e PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Cytochrome P4503A; Intestinal absorption; Intestinal metabolism; Mucosal export; Nonlinear pharmacokinetics; P glycoprotein

Indexed keywords

CYTOCHROME P450 3A4; DRUG METABOLITE; ELACRIDAR; GLYCOPROTEIN P; KETOCONAZOLE; PHOSPHODIESTERASE V INHIBITOR; UK 340943; UK 343664; UK 347334; UNCLASSIFIED DRUG; VERAPAMIL;

ANIMAL TISSUE; ARTICLE; CONCENTRATION RESPONSE; CONTROLLED STUDY; DOSE RESPONSE; DRUG ABSORPTION; DRUG METABOLISM; DRUG PENETRATION; ILEUM; INTESTINE ABSORPTION; INTESTINE PERFUSION; JEJUNUM; MALE; MAMMAL; MESENTERY; NONHUMAN; RAT; REGULATORY MECHANISM; SMALL INTESTINE;

EID: 32644434548     PISSN: 00223549     EISSN: 15206017     Source Type: Journal    
DOI: 10.1002/jps.20527     Document Type: Article

References (38)

1. Wallis RM, Corein JD, Francis SH, Ellis P. 1999. Tissue distribution of phosphodiesterase families and the effects of sidenafil on tissuecyclic nucleotides, platelet function and the contractile responses of trabeculae carneae and aortic rings in vitro. Am J Cardiol 83:3C-12C.
2. Walker DK, Beaumont KC, Compy P, Evans KM, Gedge JI, Halliday RC, Roffey SJ, Wright PA. 2001. Pharmacokinetics and metabolism of a selective PDE5 inhibitor (UK-343,664) in rat and dog. Xenobiotica 31:651-664.
3. Abel S, Beaumont KC, Crespi CL, Eve MD, Fox L, Hyland R, Jones BC, Muirhead GJ, Smith DA, Venn RF, Walker DK. 2001. Potential role fro P-glycoprotein in the non-proportional pharmacokinetics of UK-343,664 in man. Xenobiotica 31: 665-676.
4. Amidon GL, Sinko P, Fleisher D. 1988. Estimating human oral fraction dose absorbed: A correlation using rat intestinal membrane permeability for passive and carrier-mediated compounds. Pharm Res 5:651-654.
5. Fagerholm U, Johansson M, Lennernas H. 1996. Comparison between permeability coefficients in rat and human jejunum. Pharm Res 13:1336-1342.
6. Li LY, Amidon GL, Kim JS, Heimbach T, Kesisoglou F, Topliss JT, Fleisher D. 2002. Intestinal metabolism promotes regional differences in apical uptake of indinavir: Coupled effect of P-glycoprotein and cytochrome P450 on indinavir membrane permeability in rat. J Pharmacol Exp Ther 301: 586-593.
7. Tamura S, Ohike A, Ibuki R, Amidon GL, Yamashita S. 2002. Tacrolimus is a class II low-solubility high-permeability drug: The effect of P-glycoprotein efflux on regional permeability of tacrolimus in rats. J Pharm Sci 91:719-729.
8. Tamura S, Tokunaga Y, Ibuki R, Amidon GL, Sezaki H, Yamashita S. 2003. The site-specific transport and metabolism of tacrolimus in rat small intestine. J Pharmacol Exp Ther 306:310-316.
9. Singhal D, Ho NF, Anderson GD. 1998. Absorption and intestinal metabolism of purine dideoxynucleosides and an adenosine deaminase-activated prodrug of 2′,3′-dideoxyinosine in the mesenteric vein canulated rat ileum. J Pharm Sci 87:569-577.
10. Lucas M. 1983. Determination of acid surface pH in vivo in rat proximal jejunum. Gut 24:734-739.
11. Genz A, Engelhardt WV, Busche R. 1999. Maintenance and regulation of the pH microclimate at the luminal surface of the distal colon of guinea-pig. J Physiol 517:507-519.
12. Tsuruo T, Iida H, Tsukagoshi S, Sakuri Y. 1981. Overcoming of vincristine resistance in P388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res 41:4403-4412.
13. Witherspoon SM, Emerson DL, Kerr BM, Lloyd TL, Dalton WS, Wissel PS. 1996. Flow cytometric assay of modulation of P-glycoprotein function in whole blood by the multi-drug resistance inhibitor GF120918. Clin Cancer Res 2:7-12.
14. Traunecker HC, Stevens MC, Kerr DJ, Ferry DR. 1999. The acridonecarboxamide GF120918 potently reverses P-glycoprotein-mediated resistance in human sarcoma MES-Dx5 cells. Br J Cancer 81: 942-951.
15. Van Rensburg CEJ, Joone G, Anderson R. 1998. a-Tocopherol antagonizes the multidrug-resistance-reversal activity of cyclosporine A, verapamil, GF120918, clofazimine and B669. Cancer Lett 127:107-112.
16. Cummins CL, Salphati L, Reid MJ, Bene LZ. 2003. In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: Studies using the rat intestinal single-pass intestinal perfusion model. J Pharm Exp Ther 305:306-314.
17. Floren LC, Bekersky I, Benet LZ, Mekki Q, Dressier D, Lee JW, Robert JP, Hebert MF. 1997. Tacrolimus oral bioavailability doubles with coadministration of ketoconazole. Clin Pharmacol Ther 62:41-49.
18. Boolell M, Gepi-Attee S, Gingell JC, Allen MJ. 1996. Sildenafil, a novel effective treatment for male erectile dysfunction. Br J Urol 78:257-261.
19. Muirhead GJ, Allen MJ, James GC, Pearson J, Rance DJ, Houston AC, Dewland PM. 1996. Pharmacokinetics of sildenafil (Viagra), a selective cGMP PDE5 inhibitor, after single oral doses in fasted and fed healthy volunteers. Br J Clin Pharm 42:268P.
20. Walker DK, Ackland MJ, James GC, Muirhead GJ, Rance DJ, Wastall P, Wright PA. 1999. Pharmacokinetics and metabolism of sildenafil in mouse, rat, rabbit, dog and man. Xenobiotica 29:297-310.
21. Benet LZ, Wu CY, Hebert MF, Watcher VJ. 1996. Intestinal drug metabolism and antitransport processes: A potential paradigm shift to oral drug delivery. J Control Release 39:139-143.
22. Benet LZ, Izumi T, Zhang Y, Silverman JA, Wacher V. 1999. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery. J Control Release 62:25-31.
23. Watcher VJ, Salphati L, Benet LZ. 2001. Active secretion and enterocytic drug metabolism barriers to drug absorption. Adv Drug Deliv Rev 46:89-102.
24. Waziers D, Cugnenc PH, Yang CS, Leroux JP, Beaune PH. 1990. Cytochrome P450 isoenzymes, epoxide hydrolase and glutathione transferases in rat and human hepatic and extrahepatic tissues. J Pharmco Exp Ther 253:387-394.
25. Lown KS, Kolars JC, Thummel KE, Barnett JL, Kunze KL, Wrighton SA, Watkins PB. 1994. Interpatient heterogeneity in expression of CYP3A4 and CYP3A5 in small bowel. Lack of prediction by erythromycin breath test. Drug Metab Dispos 22: 947-955.
26. Lown KS, Ghosh M, Watkins PB. 1998. Sequences of intestinal and hepatic and cytochrome P450 3A4 cDNA are identical. Drug Metab Dispos 26:185-187.
27. Makhey VD, Guo A, Norris DA, Hu P, Yan J, Sinko PJ. 1998. Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells. Pharm Res 15:1160-1167.
28. Shimomura M, Masuda S, Saito H, Sakamoto S, Uemoto S, Tanaka K, Inui K. 2002. Roles of the jejunum and ileum in the first-pass effect as absorptive barriers for orally administered tacrolimus. J Surg Res 103:215-222.
29. Yeh KC, Deutsch PJ, Haddix H, Hesney M, Hoagland V, Ju WD, Justice SJ, Osborne B, Sterrett AT, Stone JA, Woolf E, Waldman S. 1998. Single-dose pharmacokinetics of indinavir and the effect of food. Antimicrob Agents Chemother 42: 332-338.
30. Goh LB, Spears KJ, Yao D, Ayrton A, Morgan P, Ronald WC, Friedberg T. 2002. Endogenous drug transporters in in vitro and in vivo models for the prediction of drug disposition in man. Biochem Pharmacol 64:1569-1578.
31. Williams GC, Liu A, Knipp G, Sinko PG. 2002. Direct evidence that saquinavir is transported by multidrug resistance-associated protein (MRP1) and canalicular multispecific organic anion transporter (MRP2). Antimicrob Agents Chemother 4611:3456-3462.
32. Johnson BM, Chen W, Borchardt RT, Charman WN, Porter CJH. 2003. A kinetic evaluation of the absorption, efflux, and metabolism of verapamil in the autoperfused rat jejunum. J Pharm Exp Ther 305:151-158.
33. Sinicrope FA, Dudeja PK, Bissonnette BM, Safa AR, Brasitus TA. 1992. Modulation of P-glycoprotein-mediated drug transport by alterations in lipid fluidity of rat liver canalicular membrane vesicles. J Biol Chem 267:24995-25002.
34. Drori S, Eytan GD, Assaraf YG. 1995. Potentiation of anticancer-drug cytotoxicity by multidrug-resistence chemosensitizers involves alterations in membrane fluidity leading to increased membrane permeability. Eur J Biochem 228:1020-1029.
35. Regev R, Assaraf YG, Eytan GD. 1999. Membrane fluidization by ether, other anesthetics, and certain agents abolishes P-glycoprotein ATPase activity and modulates efflux from multidrug-resistant cells. Eur J Biochem 259:18-24.
36. Yu Z, Quinn PJ. 1998. The modulation of membrane structure and stability by dimethyl sulphoxide. Mol Membrane Biol 15:59-68.
37. Hashimoto M, Hossain S, Yamasaki H, Yazawa K, Masumura S. 1999. Effects of eicosapentaenoic acid and docosahexaenoic acid on plasma membrane fluidity of aortic endothelial cells. Lipids 34:1207-1304.
38. Mallipattu SK, Haidekker MA, Von Dassow P, Latz MI, Frangos JA. 2002. Evidence for shear-induced increase in membrane fluidity in the finoflagellate Lingulodinium polyedrum. J Comp Physiol A 188: 409-416.