Kinetic modelling of the intestinal transport of sarafloxacin. Studies in situ in rat and in vitro in Caco-2 cells

Journal of Drug Targeting

Volumn 13, Issue 3, 2005, Pages 199-212

  Fernandez Teruel, C ^a,b   Gonzalez Alvarez, I ^a   Casabo V G ^a   Ruiz Garcia, A ^a,c   Bermejo, M ^a,d  

^a UNIVERSITY OF VALENCIA   (Spain)

^b Intervelance Biokinetics SL   (Spain)

^c Sonus Pharmaceuticals   (United States)

^d NONE   (Spain)

Author keywords

Active transport; Fluoroquinolones; In situ model; Intestinal absorption; Kinetic modelling

Indexed keywords

ADENOSINE TRIPHOSPHATE; CIPROFLOXACIN; NORDIFLOXACIN; NORFLOXACIN; QUINOLINE DERIVED ANTIINFECTIVE AGENT; SODIUM AZIDE;

ANIMAL EXPERIMENT; ARTICLE; CELL STRAIN CACO 2; CONCENTRATION RESPONSE; CONTROLLED STUDY; CORRELATION ANALYSIS; DRUG ABSORPTION; DRUG DELIVERY SYSTEM; DRUG TRANSPORT; HUMAN; HUMAN CELL; IN VITRO STUDY; INTESTINE ABSORPTION; LIPOPHILICITY; MALE; MATHEMATICAL MODEL; NONHUMAN; PHARMACODYNAMICS; PRIORITY JOURNAL; RAT; SMALL INTESTINE;

ADENOSINE TRIPHOSPHATE; ALGORITHMS; ANIMALS; ANTI-INFECTIVE AGENTS; ANTIMETABOLITES; BIOLOGICAL TRANSPORT; CACO-2 CELLS; CHEMISTRY, PHYSICAL; CIPROFLOXACIN; DIFFUSION; ENERGY METABOLISM; FLUOROQUINOLONES; HUMANS; INTESTINAL ABSORPTION; INTESTINES; LIPIDS; MALE; MODELS, STATISTICAL; OXIDATIVE PHOSPHORYLATION; RATS; RATS, WISTAR; SODIUM AZIDE;

EID: 18744366654     PISSN: 1061186X     EISSN: None     Source Type: Journal    
DOI: 10.1080/10611860500087835     Document Type: Article

References (54)

1. Aarons L, Balant LP, Mentre F, Morselli PL, Rowland M, Steimer JL, Vozeh S. 1994. Population approaches in drug development. Report on an expert meeting to discuss population pharmacokinetic/pharmacodynamic software. Eur J Clin Pharmacol 46:389-391.
2. Balant LP, Garret ER. 1985. Computer use in pharmacokinetics. In: Garret ER, Hirtz JL, editors. Drug fate and metabolism. New York: Dekker p 1-78.
3. Bermejo M, Merino V, Garrigues TM, Pla Delfina JM, Mulet A, Vizet P, Trouiller G, Mercier C. 1999. Validation of a biophysical drug absorption model by the PATQSAR system. J Pharm Sci 88:398-405.
4. Bermejo M, Avdeef A, Ruiz A, Nalda R, Ruell JA, Tsinman O, Gonzalez I, Fernandez C, Sanchez G, Garrigues TM, Merino V. 2004. PAMPA - a drug absorption in vitro model 7. Comparing rat in situ, Caco-2, and PAMPA permeability of fluoroquinolones. Eur J Pharm Sci 21:429-441.
5. Blondeau JM. 1999. Expanded activity and utility of the new fluoroquinolones: A review. Clin Ther 21:3-40.
6. Camenisch G, Folkers G, Van de Waterbeemd H. 1998. Shapes of membrane permeability-lipophilicity curves: Extension of theoretical models with an aqueous pore pathway. Eur J Pharm Sci 6:325-333.
7. Cormet E, Huneau JF, Bouras M, Carbon C, Rubinstein E, Tome D. 1997. Evidence for a passive diffusion mechanism for sparfloxacin uptake at the brush-border membrane of the human intestinal cell-line Caco-2. J Pharm Sci 86:33-36.
8. Curry SH, Whelpton R. 1983. Physicochemical properties of drugs and dosage forms. Manual of laboratory pharmacokinetics. New York: John Willey and Sons Eds. p 39-54.
9. Doluisio JT, Billups NF, Dittert LW, Sugita ET, Swintosky JV. 1969. Drug absorption. I. An in situ rat gut technique yielding realistic absorption rates. J Pharm Sci 58:1196-1200.
10. Durr D, Stieger B, Kullak-Ublick GA, Rentsch KM, Steinert HC, Meier PJ, Fattinger K. 2000. St John's Wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic CYP3A4. Clin Pharmacol Ther 68:598-604.
11. Escribano E, Calpena AC, Garrigues TM, Freixas J, Domenech J, Moreno J. 1997. Structure-absorption relationships of a series of 6-fluoroquinolones. Antimicrob Agents Chemother 41:1996-2000.
12. Estrada E, Hernández M. 1976. Transporte activo. In: Blume HM, editor. Cinética del Transporte a Través de Membranas. Madrid. p 37-71.
13. Etxeberria J, Joaristi L, Lizasoain L, Programación y análisis estadisticos básicos con SPSS- PC(+).
14. Ferrando R, Garrigues TM, Bermejo MV, Martin-Algarra R, Merino V, Polache A. 1999. Effects of ethanol on intestinal absorption of drugs: In situ studies with ciprofloxacin analogs in acute and chronic alcohol-fed rats. Alcohol Clin Exp Res 23:1403-1408.
15. Gabus Sannie C, Buri P. 1987. Étude comparative des méthodes de détermitaion du volume d'eau absorbé lors de perfusion de l'intestine grêle du rat. S.T.P. Pharma 3:856-860.
16. Griffiths NM, Hirst BH, Simmons NL. 1993. Active secretion of the fluoroquinolone ciprofloxacin by human intestinal epithelial Caco-2 cell layers. Br J Pharmacol 108:575-576.
17. Griffiths NM, Hirst BH, Simmons NL. 1994. Active intestinal secretion of the fluoroquinolone antibacterials ciprofloxacin, norfloxacin and pefloxacin; a common secretory pathway? J Pharmacol Exp Ther 269:496-502.
18. Hidalgo IJ, Raub TJ, Borchardt RT. 1989. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 96:736-749.
19. Hirohashi T, Suzuki H, Chu XY, Tamai I, Tsuji A, Sugiyama Y. 2000. Function and expression of multidrug resistance associated protein family in human colon adenocarcinoma cells (Caco-2). J Pharmacol Exp Ther 292:265-270.
20. Hu M, Chen J, Tran D, Zhu Y, Leonardo G. 1994a. The Caco-2 cell monolayers as an intestinal metabolism model: Metabolism of dipeptide Phe-Pro. J Drug Target 2:79-89.
21. Hu M, Chen J, Zhu Y, Dantzig AH, Stratford Jr, RE, Kuhfeld MT. 1994b. Mechanism and kinetics of transcellular transport of a new beta-lactam antibiotic loracarbef across an intestinal epithelial membrane model system (Caco-2). Pharm Res 11:1405-1413.
22. Idkaidek NM, Amidon GL, Smith DE, Najib NM, Hassan MM. 1998. Determination of the population pharmacokinetic parameters of sustained-release and enteric-coated oral formulations, and the suppository formulation of diclofenac sodium by simultaneous data fitting using NONMEM. Biopharm Drug Dispos 19:169-174.
23. Ito A, Hirai K, Inoue M, Koga H, Suzue S, Irikura T, Mitsuhashi S. 1980. In vitro antibacterial activity of AM-715, a new nalidixic acid analog. Antimicrob Agents Chemother 17:103-108.
24. Ladu BN, Mandel HG, Way EL. 1972. Inhibition of enzyme systems Fundamentals of Drug Metabolism and Drug Disposition. Baltimore: The Williams and Wilkins Company. p 406-407.
25. Leo AJ, Hansch C, Elkins D. 1971. Partition coefficients and their uses. Chem Rev 71:525-553.
26. Litman T, Skovsgaard T, Stein WD. 2003. Pumping of drugs by P-glycoprotein: A two-step process? J Pharmacol Exp Ther 307:846-853.
27. Lowes S, Simmons NL. 2002. Multiple pathways for fluoroquinolone secretion by human intestinal epithelial (Caco-2) cells. Br J Pharmacol 135:1263-1275.
28. Mager DE, Wyska E, Jusko WJ. 2003. Diversity of mechanism-based pharmacodynamic models. Drug Metab Dispos 31:510-518.
29. Mandema JW, Verotta D, Sheiner LB. 1992. Building population pharmacokinetic-pharmacodynamic models. I. Models for covariate effects. J Pharmacokinet Biopharm. 20:511-528.
30. Martin-Algarra RV, Pascual-Costa RM, Merino M, Casabo VG. 1997. Intestinal absorption kinetics of amiodarone in rat small intestine. Biopharm Drug Dispos 18:523-532.
31. Martin-Villodre A, Pla-Delfina JM, Moreno J, Perez-Buendia D, Miralles J, Collado EF, Sanchez-Moyano E, Del Pozo A. 1986. Studies on the reliability of a bihyperbolic functional absorption model. I. Ring-substituted anilines. J Pharmacokinet Biopharm 14:615-633.
32. Merino V, Freixas J, Bermejo M, Garrigues TM, Moreno J, Pla-Delfina JM. 1995. Biophysical models as an approach to study passive absorption in drug development: 6-fluoroquinolones. J Pharm Sci 84:777-782.
33. Montalar M, Nalda-Molina R, Rodriguez-Ibanez M, Garcia-Valcarcel I, Garrigues TM, Merino V, Bermejo M. 2003. Kinetic modeling of triamterene intestinal absorption and its inhibition by folic acid and methotrexate. J Drug Target 11:215-223.
34. Naruhashi K, Tamai I, Inoue N, Muraoka H, Sai Y, Suzuki N, Tsuji A. 2001. Active intestinal secretion of new quinolone antimicrobials and the partial contribution of P-glycoprotein. J Pharm Pharmacol 53:699-709.
35. Powell DW, Johnson LR. 1987. Physiology of the gastrointestinal tract. 2nd ed. New York: Raven Press. p 1267-1305.
36. Prieto JG, Barrio JP, Alvarez AI, Gomez G. 1988. Kinetic mechanism for the intestinal absorption of ofloxacin. J Pharm Pharmacol 40:211-212.
37. Rabbaa L, Dautrey S, Colas-Linhart N, Carbon C, Farinotti R. 1995. Stereoselectivity of ofloxacin intestinal transport in the rat. Drugs 49(Suppl 2):333-334.
38. Rabbaa L, Dautrey S, Colas-Linhart N, Carbon C, Farinotti R. 1997. Absorption of ofloxacin isomers in the rat small intestine. Antimicrob Agents Chemother 41:2274-2277.
39. Ramon J, Dautrey S, Farinoti R, Carbon C, Rubinstein E. 1994. Intestinal elimination of ciprofloxacin in rabbits. Antimicrob Agents Chemother 38:757-760.
40. Rodriguez-Ibanez M, Nalda-Molina R, Montalar-Montero M, Bermejo MV, Merino V, Garrigues TM. 2003. Transintestinal secretion of ciprofloxacin, grepafloxacin and sparfloxacin: In vitro and in situ inhibition studies. Eur J Pharm Biopharm 55:241-246.
41. Rubinstein E, St Julien L, Ramon J, Dautrey S, Farinotti R, Huneau JF, Carbon C. 1994. The intestinal elimination of ciprofloxacin in the rat. J Infect Dis 169:218-221.
42. Ruiz-Garcia A, Lin H, Pla-Delfina JM, Hu M. 2002. Kinetic characterization of secretory transport of a new ciprofloxacin derivative (CNV97100) across Caco-2 cell monolayers. J Pharm Sci 91:2511-2519.
43. Sanchez-Castano G, Ruiz-Garcia A, Banon N, Bermejo M, Merino V, Freixas J, Garrigues TM, Pla-Delfina JM. 2000. Intrinsic absolute bioavailability prediction in rats based on in situ absorption rate constants and/or in vitro partition coefficients: 6- fluoroquinolones. J Pharm Sci 89:1395-1403.
44. Saunders BD, Trapp RG. 1994. Basic and clinical biostatistics. Connecticut: Prentice Hall Inc.
45. Schwarz UI, Gramatte T, Krappweis J, Oertel R, Kirch W. 2000. P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans. Int J Clin Pharmacol Ther 38:161-167.
46. Seelig A, Landwojtowicz E. 2000. Structure-activity relationship of P-glycoprotein substrates and modifiers. Eur J Pharm Sci 12:31-40.
47. Shah VP, Midha KK, Dighe S, Mcgilveray IJ, Skelly JP, Yacobi A, Layloff T, Viswanathan CT, Cook CE, Mcdowall RD. 1991. Analytical methods validation: Bioavailability, bioequivalence and pharmacokinetic studies. Conference report. Eur J Drug Metab Pharmacokinet 16:249-255.
48. Sheiner LB, Beal SL. 1980. Evaluation of methods for estimating population pharmacokinetics parameters. I. Michaelis-Menten model: Routine clinical pharmacokinetic data. J Pharmacokinet Biopharm 8:553-571.
49. Staib AH, Harder S, Mieke S, Beer C, Stille W, Shah PM, Frech K. 1986. Gyrase inhibitors can delay caffeine elimination. Dtsch Med Wochenschr 111:1500.
50. Tamai I, Saheki A, Saitoh R, Sai Y, Yamada I, Tsuji A. 1997. Nonlinear intestinal absorption of 5-hydroxytryptamine receptor antagonist caused by absorptive and secretory transporters. J Pharmacol Exp Ther 283:108-115.
51. Valenzuela B, Nacher A, Casabo VG, Martin-Villodre A. 2001. The influence of active secretion processes on intestinal absorption of salbutamol in the rat. Eur J Pharm Biopharm 52:31-37.
52. Vasilyeva E, Forgac M. 1998. Interaction of the clathrin-coated vesicle V-ATPase with ADP and sodium azide. J Biol Chem 273:23823-23829.
53. Yamaguchi H, Yano I, Saito H, Inui K. 2001. Transport characteristics of grepafloxacin and levofloxacin in the human intestinal cell line Caco-2. Eur J Pharmacol 431:297-303.
54. Yoshida F, Topliss JG. 2000. QSAR model for drug human oral bioavailability. J Med Chem 43:2575-2585.