In vivo non-linear intestinal permeability of celiprolol and propranolol in conscious dogs: Evidence for intestinal secretion

European Journal of Pharmaceutical Sciences

Volumn 6, Issue 1, 1998, Pages 75-81

  Lipka, E ^a,b   Spahn Langguth, H ^c   Mutschler, E ^c   Amidon, G L ^a  

^a UNIVERSITY OF MICHIGAN   (United States)

^b TSRL INC   (United States)

^c GOETHE UNIVERSITY   (Germany)

Author keywords

Celiprolol; Intestinal secretion; Non linear drug uptake; Oral absorption; Permeability; Propranolol

Indexed keywords

CELIPROLOL; PROPRANOLOL;

ANIMAL EXPERIMENT; ARTICLE; DOG; DRUG ABSORPTION; DRUG UPTAKE; INTESTINE ABSORPTION; INTESTINE MUCOSA PERMEABILITY; INTESTINE SECRETION; NONHUMAN; PRIORITY JOURNAL; REGIONAL PERFUSION; STEREOCHEMISTRY;

ANIMALS; CELIPROLOL; CONSCIOUSNESS; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; INTESTINAL ABSORPTION; INTESTINAL SECRETIONS; JEJUNUM; MALE; METABOLIC CLEARANCE RATE; PERMEABILITY; PROPRANOLOL; TIME FACTORS; VASODILATOR AGENTS;

EID: 0031963285     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(97)00070-5     Document Type: Article

References (30)

1. Al-Angary A.A., El-Sayed Y.M., Al-Meshal M.A., Al-Dardiri M.M., Mahrous G.M. A sensitive high-performance liquid chromatographic analysis of propranolol in serum. J. Clin. Pharm. Ther. 16:1991;93-101.
2. Amidon G.L., Lennernas H., Shah V.P., Crison J.R. A theoretical basis for a biopharmaceutic drug classification: the correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm. Res. 12:(3):1995;413-420.
3. Bergstrom R.F., Kay D.R., Wagner J.G. The pharmacokinetics of penicillamine in a female mongrel dog. J. Pharmacokin. Biopharm. 9:(5):1981;603-621.
4. Caruso F.S., Doshan H.D., Hernandez P.H., Costello R., Applin W., Neiss E.S. Celiprolol: pharmacokinetic and duration of pharmacodynamic activity. Br. J. Clin. Pract. 40:1985;12-16.
5. Cornwell M.M. Molecular biology of P-glycoprotein. Ozols R. Molecular and Clinical Advances in Anticancer Drugs. 1991;37-56 Kluwer Academic Publishers, Boston.
6. George C.F., Gruchy B.S. Elimination of drugs by active intestinal transport. J. Pharm. Pharmacol. 31:1979;643-644.
7. Hartmann C. Enantiomerenanalytik und -kinetik des β-Adrenozeptorenblockers Celiprolol. Thesis. 1989;Department of Pharmacology, University of Frankfurt, Germany.
8. Hartmann C., Krauss D., Spahn H., Mutschler E. Simultaneous determination of (R)- and (S)-celiprolol in human plasma and urine: high performance liquid chromatographic assay on a chiral stationary phase with fluorimetric detection. J. Chromatogr. 496:1989;387-396.
9. Hitzenberger G., Takacs F., Pittner H. Pharmakokinetik des β-Rezeptorenblockers Celiprolol nach einmaliger intravenöser und oraler Gabe. Arzneim.-Forsch./Drug. Res. 33:(1):1983;50-52.
10. Hsyu P.-H., Giacomini K.M. Stereoselective renal clearance of pindolol in humans. J. Clin. Invest. 76:1985;1720-1726.
11. Hunter J., Hirst B.H., Simmons N.L. Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cells. Pharm. Res. 10:(5):1993;743-749.
12. Karlson J., Kuo S.M., Ziemniak J., Artursson P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: mediation of secretion by multiple transporters including P-glycoprotein. Br. J. Pharmacol. 110:(3):1993;1009-1016.
13. Knudson L., Odind B., Haellgren R. A new technique for segmental jejunal perfusion in man. Am. J. Gastroenterol. 84:1989;1278-1284.
14. Kuo S.M., Whitby B.R., Artursson P., Ziemniak J.A. The contribution of intestinal secretion to the dose-dependent absorption of celiprolol. Pharm. Res. 11:(5):1994;648-653.
15. Lauterbach F. Intestinal absorption and secretion of cardioactive glycosides. Verh. Dtsch. Ges. Inn. Med. 83:1977;33-45.
16. Lennernas H., Regardh C.G. Pharmacokinetics of pafenolol in the rat: a suitable model for studying absorption mechanisms of a drug exhibiting unusual absorption properties in man. Biopharm. Drug Dispos. 11:1990;619-631.
17. Lennernas H., Regardh C.G. Dose-dependent intestinal absorption and significant intestinal excretion (exsorption) of the beta-blocker pafenolol in the rat. Pharm. Res. 10:(5):1993;727-731.
18. Lennernas H., Regardh C.G. Evidence for an interaction between the β-blocker pafenolol and bile salts in the intestinal lumen of the rat leading to dose-dependent oral absorption and double peaks in the plasma concentration-time profile. Pharm. Res. 10:(6):1993;879-883.
19. Lipka E., Langguth P., Spahn-Langguth H., Mutschler E., Amidon G.L. Celiprolol double-peak occurrence and gastric motility: non-linear mixed effects modeling of bioavailability data obtained in dogs. J. Pharmacokin. Biopharm. 23:(3):1995;267-286.
20. Meier J. Pharmacokinetic comparison of pindolol with other beta-adrenoceptor-blocking agents. Am. Heart J. 104:(2):1982;364-373.
21. Milne R.J., Buckley M.T. Celiprolol: an updated review of its pharmacokinetic properties and therapeutic efficacy in cardiovascular diseases. Drugs. 41:(6):1991;941-969.
22. Ott R., Giacomini K.M. Stereoselective interaction of organic cations with the organic cation transporter in OK cells. Pharm. Res. 10:(8):1993;1169-1173.
23. Pittner H., Takacs F., Fellier H. Pharmakokinetische und toxikokinetische Untersuchungen mit dem kardioselektiven β-Rezeptorenblocker Celiprolol an Ratten, Hunden und Kaninchen. Arzneim. Forsch./Drug Res. 33:(1):1983;33-41.
24. Regardh C.G., Heggelund A., Kylberg-Hanssen K., Lundborg P. Pharmacokinetics of pafenolol after iv and oral administration of three separate doses of different strength to man. Biopharm. Drug Dispos. 11:1990;607-617.
25. Rindell J.G., Shanks R.G., Brogden R.N. Celiprolol: a preliminary review of its pharmacodynamic and pharmacokinetic properties and its therapeutic use in hypertension and angina pectoris. Drugs. 34:1987;438-458.
26. Sinko P.J., Leesman G.L., Amidon G.L. Predicting fraction dose absorbed in humans using a macroscopic mass balance approach. Pharm Res. 8:(8):1991;979-988.
27. Turnheim K., Lauterbach F. Interaction between intestinal absorption and secretion of monoquaternary ammonium compounds in guinea pigs - a concept for the absorption kinetics of organic cations. J. Pharmacol. Exp. Ther. 212:(3):1980;418-424.
28. Wetterich U., Mutschler E., Spahn-Langguth H., Langguth P. Evidence for intestinal secretion of the β-adrenoceptor antagonist talinolol: data from humans and studies with Caco-2 cells. Naunyn Schmiedebergs Arch. Pharmacol. 351:1995;R1. (Suppl.).
29. Yamagushi T., Ikeda C., Sekine Y. Intestinal absorption of a β-adrenergic blocking agent nadolol I. Comparison of absorption behavior of nadolol with those of other β-blocking agents in rats. Chem. Pharm. Bull. 34:(8):1986;3362-3369.
30. Yamagushi T., Ikeda C., Sekine Y. Intestinal absorption of a β-adrenergic blocking agent nadolol II. Mechanism of the inhibitory effect on the intestinal absorption of nadolol by sodium cholate in rats. Chem. Pharm. Bull. 34:(9):1986;3836-3843.