A New System for the Prediction of Drug Absorption Using a pH-Controlled Caco-2 Model: Evaluation of pH-Dependent Soluble Drug Absorption and pH-Related Changes in Absorption

Journal of Pharmaceutical Sciences

Volumn 93, Issue 1, 2004, Pages 71-77

  He, Xin ^a   Kadomura, Shota ^a   Takekuma, Yoh ^a   Sugawara, Mitsuru ^a   Miyazaki, Katsumi ^a  

^a HOKKAIDO UNIVERSITY HOSPITAL   (Japan)

Author keywords

Caco 2 cells; Drug interactions; In vitro models; Oral absorption; Permeability; Prediction; Solubility

Indexed keywords

ANTACID AGENT; DIPYRIDAMOLE; GLIBENCLAMIDE; HISTAMINE H2 RECEPTOR ANTAGONIST; MAGNESIUM HYDROXIDE;

ACCURACY; ARTICLE; CELL STRAIN CACO 2; CONTROLLED STUDY; DRUG ABSORPTION; DRUG SYNTHESIS; GASTROINTESTINAL TRACT; HUMAN; HUMAN CELL; MEDICAL ASSESSMENT; PH; PHYSIOLOGY; PREDICTION; STOMACH PH; TABLET;

EID: 0347755148     PISSN: 00223549     EISSN: None     Source Type: Journal    
DOI: 10.1002/jps.10518     Document Type: Article

References (12)

1. Kobayashi M, Sada N, Sugawara M, Iseki K, Miyazaki K. 2001. Development of a new system for prediction of drug absorption that takes into account drug dissolution and pH change in the gastro-intestinal tract. Int J Pharm 221:87-94.
2. He X, Sugawara M, Kobayashi M, Takekuma Y, Miyazaki K. 2003. An in vitro system for prediction of oral absorption of relatively water-soluble drugs and ester prodrugs. Int J Pharm 263:35-44.
3. Foye WO. 1981. Principles of Medicinal Chemistry. Philadelphia: Lea and Febiger.
4. Kohri N, Miyata N, Takahashi M, Endo H, Iseki K, Miyazaki K, Takechi S, Nomura A. 1992. Evaluation of pH-independent sustained-release granules of dipyridamole by using gastric-acidity-controlled rabbits and human subject. Int J Pharm 81:49-58.
5. Russell TL, Berardi RR, Barnett JL, Dermentzoglou LC, Jarvenpaa KM, Schmaltz SP, Dressman JB. 1993. Upper gastrointestinal pH in seventy-nine healthy, elderly, North American men and women. Pharm Res 10:187-196.
6. Russel TL, Berardi RR, Barnett JL, O'Sullivan TL, Wagner JG, Dressman JB. 1994. pH-related changes in the absorption of dipyridamole in the elderly. Pharm Res 11:136-143.
7. Kaali RN, Rye RM, Wiseman D, York P. 1987. Dissolution of glibenclamide: The role of particle size. J Pharm Pharmacol 39:44.
8. Neuvonen PJ, Kivisto KT. 1991. The effects of magnesium hydroxide on the absorption and efficacy of two glibenclamide preparations. Br J Clin Pharmacol 32:215-220.
9. Kubacka RT, Antal EJ, Juhl RP. 1987. The paradoxical effect of cimetidine and ranitidine on glibenclamide pharmacokinetics and pharmacodynamics. Br J Clin Pharmacol 23:743-751.
10. Tuderman V, Klinge E, Lind H. 1979. In vitro evaluation of antacid suspensions marketed in Finland. Acta Pharm Fenn 88:63-72.
11. Brockmeier D, Grigoleit HG, Leonhardt H. 1985. Absorption of glibenclamide from different sites of the gastro-intestinal tract. Eur J Clin Pharmacol 29:193-197.
12. Palm K, Luthman K, Ros J, Grasjo T, Artursson P. 1999. Effect of molecular charge on intestinal epithelial drug transport: pH-dependent transport of cationic drug. J Pharmacol Exp Ther 291:435-443.