pH and energy dependent transport of ketoprofen across rat jejunum in vitro

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 56, Issue 1, 2003, Pages 87-94

  Legen, Igor ^a   Kristl, Albin ^a  

^a UNIVERSITY OF LJUBLJANA   (Slovenia)

Author keywords

Drug absorption; Microclimate pH; Monocarboxylate transporter; Non steroidal anti inflammatory drugs; pH partition theory

Indexed keywords

ACETIC ACID; ALPHA CYANO 4 HYDROXYCINNAMIC ACID; BENZOIC ACID; KETOPROFEN; LACTIC ACID; MONOCARBOXYLATE TRANSPORTER;

ARTICLE; CONTROLLED STUDY; DRUG PENETRATION; DRUG TRANSPORT; IN VITRO STUDY; INCUBATION TIME; JEJUNUM; MUCOSA; NONHUMAN; PH; PROBABILITY; RAT; SEROSA; SURFACE PROPERTY;

EID: 0038692045     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0939-6411(03)00039-0     Document Type: Article

References (32)

1. Jamali F., Brocks D.R. Clinical pharmacokinetics of ketoprofen and its enantiomers. Clin. Pharmacokinet. 19:1990;197-217.
2. Fagerholm U., Johansson M., Lennernäs H. Comparison between permeability coefficients in rat and human jejunum. Pharmacol. Res. 13:1996;1336-1341.
3. Hilgendorf C., Spahn-Langguth H., Regårdh C.G., Lipka E., Amidon G.L., Langguth P. Caco-2 versus Caco-2/HT29-MTX co-cultured cell lines: permeabilities via diffusion, inside- and outside-directed carrier-mediated transport. J. Pharm. Sci. 89:2000;63-74.
4. Brodie B.B., Hogben C.A.M. Some physico-chemical factors in drug action. J. Pharm. Pharmacol. 9:1957;345-380.
5. Högerle M.L., Winne D. Drug absorption by the rat jejunum perfused in situ. Naunyn-Schmiedeberg's Arch. Pharmacol. 322:1983;249-255.
6. Rechkemmer G., Wahl M., Kuschinsky W., von Engelhardt W. pH-Microclimate at the luminal surface of the intestinal mucosa of guinea pig and rat. Pflügers Arch. 407:1986;33-40.
7. Said H.M., Smith R., Redha R. Studies on the intestinal surface acid microclimate: developmental aspects. Pediatr. Res. 22:1987;497-499.
8. Jackson M.J., Tai C.Y., Steane J.E. Weak electrolyte permeation in alimentary epithelia. Am. J. Physiol. 240:1981;G191-G198.
9. Tamai I., Takanaga H., Maeda H., Ogihara T., Yoneda M., Tsuji A. Proton-cotransport of pravastatin across intestinal brush-border membrane. Pharmacol. Res. 12:1995;1727-1732.
10. Ogihara T., Tamai I., Takanaga H., Sai Y., Tsuji A. Stereoselective and carrier-mediated transport of monocarboxylic acids across Caco-2 cells. Pharmacol. Res. 13:1996;1828-1832.
11. Li Y.H., Ito K., Tsuda Y., Kohda R., Yamada H., Itoh T. Mechanism of intestinal absorption of an orally active β-lactam prodrug: uptake and transport of carindacillin in Caco-2 cells. J. Pharmacol. Exp. Ther. 290:1999;958-964.
12. Wu X., Whitfield L.R., Stewart B.H. Atorvastatin transport in the Caco-2 cell model: contributions of P-Glycoprotein and the proton-monocarboxylic acid co-transporter. Pharmacol. Res. 17:2000;209-215.
13. Takagi M., Taki Y., Sakane T., Nadai T., Sezaki H., Oku N., Yamashita S. A new interpretation of salicylic acid transport across the lipid bilayer: implications of pH-dependent but not carrier-mediated absorption from the gastrointestinal tract. J. Pharmacol. Exp. Ther. 285:1998;1175-1180.
14. Kristl A., Tukker J.J. Negative correlation of n-octanol water partition coefficient and transport of some guanine derivatives through rat jejunum in vitro. Pharmacol. Res. 15:1998;499-501.
15. Elbert J., Daniel H., Rehner G. Intestinal uptake of nicotinic acid as a function of microclimate-pH. Int. J. Vitam. Nutr. Res. 56:1986;85-93.
16. Lucas M. Determination of acidic surface pH in vivo in rat proximal jejunum. Gut. 24:1983;734-739.
17. Genz A.K., von Engelhardt W., Busche R. Maintenance and regulation of the pH microclimate at the luminal surface of the distal colon of guinea-pig. J. Physiol. 517:1999;507-519.
18. Alberts B., Bray D., Lewis J., Raff M., Roberts K., Watson J.D. Molecular Biology of the Cell. 1994M;Garland Publishing, Inc, New York/London.
19. Kang J., Heart E., Sung C.K. Effects of cellular ATP depletion on glucose transport and insulin signalling in 3T3-L1 adipocytes. Am. J. Physiol. Endocrinol. Metab. 280:2001;E428-E435.
20. Ikuma M., Hanai H., Kaneko E., Hayashi H., Hoshi T. Effects of aging on the microclimate pH of the rat jejunum. Biochim. Biophys. Acta. 1280:1996;19-26.
21. 3 exchanger in the rat jejunal enterocyte. Biochim. Biophys. Acta. 1372:1998;323-330.
22. + exchangers. Physiol. Rev. 77:1997;51-73.
23. + antiport in cultured human cells. J. Biol. Chem. 261:1986;5460-5466.
24. Mandel L.J., Bacallao R., Zampighi G. Uncoupling of the molecular fence and paracellular gate functions in epithelial tight junctions. Nature. 361:1993;552-555.
25. Tamai I., Sai Y., Ono A., Kido Y., Yabuuchi H., Takanaga H., Satoh E., Ogihara T., Amano O., Izeki S., Tsuji A. Immunohistochemical and functional characterization of pH-dependent intestinal absorption of weak organic acids by the monocarboxylic acid transporter MCT1. J. Pharm. Pharmacol. 51:1999;1113-1121.
26. Davies N.M., Wright M.R., Russell A.S., Jamali F. Effect of the enantiomers of flurbiprofen, ibuprofen, and ketoprofen on intestinal permeability. J. Pharm. Sci. 85:1996;1170-1173.
27. Den Hond E., Peeters M., Hiele M., Bulteel V., Ghoos Y., Rutgeerts P. Effect of glutamine on the intestinal permeability changes induced by indomethacin in humans. Aliment. Pharmacol. Ther. 13:1999;679-685.
28. Legen I., Kristl A. Ketoprofen induced intestinal permeability changes studied in side-by-side diffusion cells. J. Pharm. Pharmacol. 54:2002;1419-1422.
29. Bröer S., Schneider H.P., Bröer A., Rahman B., Hamprecht B., Deitmer J.W. Characterization of the monocarboxylate transporter 1 expressed in Xenopus laevis oocytes by changes in cytosolic pH. Biochem. J. 333:1998;167-174.
30. Stein J., Zores M., Schröder O. Short-chain fatty acid (SCFA) uptake into Caco-2 cells by a pH-dependent and carrier mediated transport mechanism. Eur. J. Nutr. 39:2000;121-125.
31. Price N.T., Jackson V.N., Halestrap A.P. Cloning and sequencing of four new mammalian monocarboxylate transporter (MCT) homologues confirms the existence of a transporter family with an ancient past. Biochem. J. 329:1998;321-328.
32. Halestrap A.P., Price N.T. The proton-linked monocarboxylate transporter (MCT) family: structure, function and regulation. Biochem. J. 343:1999;281-299.