Influence of food on the oral bioavailability of deramciclane from film-coated tablet in healthy male volunteers

European Journal of Pharmaceutics and Biopharmaceutics

Volumn 58, Issue 3, 2004, Pages 689-695

  Drabant, Sándor ^a   Balogh Nemes, Katalin ^a   Horváth, Viola ^c   Tolokán, Antal ^c   Grézal, Gyula ^a   Anttila, Markku ^d   Gachályi, Béla ^b   Kanerva, Harri ^d   Al Behaisi, Samar ^a   Horvai, George ^c   Klebovich, Imre ^a  

^a EGIS PHARMACEUTICALS LTD   (Hungary)

^b SEMMELWEIS UNIVERSITY   (Hungary)

^c BUDAPEST UNIVERSITY OF TECHNOLOGY AND ECONOMICS   (Hungary)

^d ORION CORPORATION   (Finland)

Author keywords

Acid labile; Clinical study; Deramciclane; Food interaction; Pharmacokinetics

Indexed keywords

DERAMCICLANE FUMARATE;

ADULT; AREA UNDER THE CURVE; ARTICLE; BLOOD LEVEL; CLINICAL TRIAL; CONFIDENCE INTERVAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BIOAVAILABILITY; DRUG SCREENING; FILM COATING; FOOD; GEOMETRY; HUMAN; LIPID DIET; MALE; MASS SPECTROMETRY; NORMAL HUMAN; PARAMETER; RANDOMIZED CONTROLLED TRIAL; TECHNIQUE; VOLUNTEER;

ADMINISTRATION, ORAL; ADULT; BIOLOGICAL AVAILABILITY; BORNANES; CROSS-OVER STUDIES; DIETARY FATS; FASTING; FOOD-DRUG INTERACTIONS; HUMANS; MALE; TABLETS, ENTERIC-COATED;

EID: 4644293132     PISSN: 09396411     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejpb.2004.03.036     Document Type: Article

References (29)

1. 2 receptors. Pharm. Pharmacol. Lett. 6:1996;82-85
2. Gacsályi I., Schmidt É., Gyertyán I., Vasar E., Lang A., Haapalinna Á., Fekete M., Hietala J., Syvälahti E., Tuomainen P., Männistö P.T. Receptor binding profile and anxiolytic-type activity of deramciclane (EGIS-3886) in animal models. Drug Dev. Res. 40:1997;333-348
3. 2c-receptor down-regulation when administered chronically. Psychopharmacology. 136:1998;99-104
4. 2A receptor occupancy of deramciclane in man after single oral administration - a positron emission tomography study. Psychopharmacology. 145:1999;76-81
5. Gacsályi I., Gyertyány I., Petöcz L., Budai Z. Psychopharmacology of a new anxiolytic agent EGYT-3886. Pharm. Res. Commun. 20:(Suppl 1):1988;115-117
6. -1. Pharm. Pharmacol. Commun. 4:1998;129-136
7. Magyar K., Lengyel J., Klebovich I., Ürmös I., Grézal G. Distribution of deramciclane (EGIS-3886) in rat brain regions. Eur. J. Drug Metab. Pharmacokinet. 23:1998;125-131
8. Lengyel J., Bolehovszky A., Klebovich I., Abermann M., Magyar K. Absorption of the new anxiolytic compound deramciclane in rats, dogs and rabbit. Arzneim.-Forsch./Drug Res. 48:1998;455-460
9. Hazai I., Pátfalusi M., Klebovich I., Ürmös I. Whole-body autoradiography and quantitative organ level distribution study of deramciclane in rats. J. Pharm. Pharmacol. 51:1999;165-174
10. Balogh Nemes K., Abermann M., Bojti E., Grézal G., Al-Behaisi S., Klebovich I. Oral, intraperitoneal and intravenous pharmacokinetics of deramciclane and its desmethyl metabolite in the rat. J. Pharm. Pharmacol. 52:2000;47-51
11. Kanerva H., Kilkku O., Heinonen E., Helminen A., Rouru J., Tarpila S., Scheinin M., Huupponen R., Klebovich I., Drabant S., Urtti A. The single dose pharmacokinetics and safety of deramciclane in healthy male volunteers. Biopharm. Drug Dispos. 20:1999;327-334
12. Kanerva H., Kilkku O., Helminen A., Rouru J., Scheinin M., Huupponen R., Klebovich I., Drabant S., Urtti A. Pharmacokinetics and safety of deramciclane during multiple oral dosing. Int. J. Clin. Pharm. Ther. 37:1999;589-597
13. Kanerva H., Klebovich I., Drabant S., Urtti A., Nevalainen T. Different absorption profiles of deramciclane in man and in dog. J. Pharm. Pharmacol. 50:1998;1087-1093
14. Drabant S., Klebovich I., Gachályi B., Renczes G., Farsang C. Role of food interaction pharmacokinetic studies in drug development. Food interaction studies of theophylline and nifedipine retard, and buspirone tablets. Acta Pharm. Hung. 68:1998;294-306
15. Welling P.G., Tse F.L. The influence of food on the absorption of antimicrobial agents. J. Antimicrob. Chemother. 9:1982;7-27
16. Sande A.M., Mandel G.L. Antimicrobal agents, tetracyclines, chloramphenicol, erythromycine, and miscellaneous agents. Gilman A.G., Rall T.W., Nies A.S., Taylor P. Goodman and Gilman's The Pharmacological Basis of Therapeutics. eighth ed:1990;1117-1145 Pergamon Press, New York, NY
17. Guidance for Industry. Food-Effect Bioavailability and Bioequivalence Studies. 1997;FDA-CDER
18. Tolokán A., Horváth V., Horvai G., Egresi A., Balogh Nemes K., Klebovich I. Determination of deramciclane and N-desmethyderamciclane in human plasma by liquid chomatography-tandem mass spectrometry using off-line robotic sample pretreatment. J. Chromatogr. A. 896:2000;279-290
19. Neuvonen P.J., Kivistö K.T. The clinical significance of food-drug interactions: a review. Med. J. Aust. 150:1989;36-40
20. Williams L., Davis J.A., Lowenthal D.T. The influence of food on the absorption and metabolism of drugs. Clin. Nutr. 77:1993;815-829
21. Toothaker R.D., Welling P.G. The effect of food on drug bioavailability. Ann. Rev. Pharmacol. Toxicol. 20:1980;173-199
22. Neuvonen P.J. Interactions with the absorption of tetracyclines. Drugs. 11:1976;45-54
23. Depperman K.M., Lode H. Fluorokinolones: interaction profile during enteral absorption. Drugs. 45:(Suppl. 3):1993;65-72
24. Rolan P.E., Mercer A.J., Weatherley B.C., Holdich T., Meire H., Peck R.W., Ridout G., Posner J. Examination of some factors responsible for a food induced increase in absorption of atovaquon. Br. J. Clin. Pharmacol. 37:1994;13-20
25. Liedholm H., Wählin-Boll E., Melander A. Mechanism and variations in the food effect on propranolol bioavailability. Eur. J. Clin. Pharmacol. 38:1990;469-475
26. Reynolds J.E.F. Martindale The Extra Pharmacopoeia. 30th ed:1993;The Pharmaceutical Press, London. pp. 162-164
27. Lui C.Y., Amidon G.L., Berardi R.R., Fleisher D., Youngberg C., Dressman J.B. Comparison of gastrointestinal pH in dogs and humans: implications on the use of beagle dog as a model for oral absorption in humans. J. Pharm. Sci. 75:1986;271-274
28. Dressman J.B., Berardi R., Dermentzoglou L., Russel T.L., Schmaltz S.P., Barnet J.L., Jarvenpaa K.M. Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm. Res. 7:1990;756-761
29. Ritschel W.A. Handbook of Basic Pharmacokinetics. third ed:1986;Drug Intelligence Publications Inc. pp. 94-111