The AAPS Journal

, Volume 10, Issue 2, pp 360–362 | Cite as

Effect of Ethanol on Opioid Drug Permeability Through Caco-2 Cell Monolayers

  • Donna A. Volpe
  • Ebenezer B. Asafu-Adjaye
  • Christopher D. Ellison
  • Suresh Doddapaneni
  • Ramana S. Uppoor
  • Mansoor A. Khan
Brief/Technical Note

Key words

Caco-2 ethanol hydromorphone oxycodone oxymorphone permeability 


  1. 1.
    A. G. Fraser. Pharmacokinetic interactions between alcohol and other drugs. Clin. Pharmacokinet. 33:79–90 (1997).PubMedCrossRefGoogle Scholar
  2. 2.
    E. M. Sellers, and M. R. Holloway. Drug kinetics and alcohol ingestion. Clin. Pharmacokinet. 3:440–452 (1978).PubMedCrossRefGoogle Scholar
  3. 3.
    A. Pfeiffer, B. Hogl, and H. Kaess. Effect of ethanol and commonly ingested alcoholic beverages on gastric emptying and gastrointestinal transit. Clin. Investig. 70:487–491 (1992).PubMedCrossRefGoogle Scholar
  4. 4.
    M. Linnoila, M. J. Mattila, and B. S. Kitchell. Drug interactions with alcohol. Drugs. 18:299–311 (1979).PubMedCrossRefGoogle Scholar
  5. 5.
    J. Persson. Alcohol and the small intestine. Scand. J. Gastroenterol. 26:3–15 (1999).CrossRefGoogle Scholar
  6. 6.
    L. R. Draper, L. A. Gyure, J. G. Hall, and D. Robertson. Effect of alcohol on the integrity of the intestinal epithelium. Gut. 24:399–404 (1983).PubMedCrossRefGoogle Scholar
  7. 7.
    A. Tarnawski, D. Hollander, and H. Gergely. Ethanol-induced gastric mucosal injury: sequential analysis of morphologic and functional changes. Gastroenterol. Clin. Biol. 9:88–92 (1995).Google Scholar
  8. 8.
    T. Y. Ma, D. Nguyen, V. Bui, H. Nguyen, and N. Hoa. Ethanol modulation of intestinal epithelial tight junction barrier. Am. J. Physiol. 276:G965–G974 (1999).PubMedGoogle Scholar
  9. 9.
    G. Sathyan, K. Sivakumar, and J. Thipphawong. Pharmacokinetic profile of a 24-hour controlled-release OROS formulation of hydromorphone in the presence of alcohol. Curr. Med. Res. Opin. 24:297–305 (2008).PubMedCrossRefGoogle Scholar
  10. 10.
    H. R. Wallage, and J. P. F. P. Palmentier. Hydromorphone-related fatalities in Ontario. J. Anal. Toxicol. 30:202–209 (2006).PubMedGoogle Scholar
  11. 11.
    Product Information: Opana® ER Oxymorphone Hydrochloride Extended-Release Tablets. Endo Pharmaceuticals Inc. Chadds Ford, Pennsylvania 19317. July 2006. PDR® Electronic Library™, accessed 12/06/07.Google Scholar
  12. 12.
    W. D. Fiske, G. Photivihok, and I. H. Benedek. The effects of graded concentrations of oral ethanol on the in vivo bioavailability of oxymorphone HCl extended release (ER) tablets. Clin. Pharmacol. Ther. 81(suppl 1):S112 (2007), (abstract PIII-83).Google Scholar
  13. 13.
    M. Abdelhameed, M. Guirguis, J. Van Berkum, R. Chaouki, J. Jenkins, P. Perrino, S. Harris, D. Cilla, and A. Kristensen. Effect of varying concentrations of ethanol administration on the pharmacokinetics (PK) of oxycodone melt extrusion multiparticulate (OCM) 10-mg capsule + naltrexone melt extrusion multiparticulate (NXM) 8-mg capsule in the fasted state in normal healthy subjects [abstract]. AAPS J. 81(suppl 2):W4385 (2006).Google Scholar
  14. 14.
    Product Information: Oxycontin® Oxycodone HCl Controlled-Release Tablets Purdue Pharma L.P., Stamford, CT. May 31, 2005. PDR® Electronic Library™, accessed 12/06/07.Google Scholar
  15. 15.
    J. J. Vallner, J. T. Stewart, J. A. Kotzan, E. B. Kirsten, and I. L. Honigberg. Pharmacokinetics and bioavailability of hydromorphone following intravenous and oral administration to human subjects. J. Clin. Pharmacol. 21:152–156 (1981).PubMedGoogle Scholar
  16. 16.
    D. A. Volpe, A. B. Ciavarella, E. B. Asafu-Adjaye, C. D. Ellison, P. J. Faustino, L. X. Yu, and A. S. Hussain. Classification of drug permeability with a Caco-2 cell monolayer assay. Clin. Res. Regul. Affairs. 24:39–47 (2007).CrossRefGoogle Scholar
  17. 17.
    S. Yamashita, T. Furubayashi, M. Kataoka, T. Sakane, H. Sezaki, and H. Tokuda. Optimized conditions for intestinal drug permeability using Caco-2 cells. Eur. J. Pharm. Sci. 10:194–204 (2000).CrossRefGoogle Scholar
  18. 18.
    G. M. Pauletti, K. L. Audus, and I. J. Hidalgo. Effect of co-solvents on the physical barrier properties of Caco-2 cell monolayers [abstract]. Pharm. Sci. 1(1):182 (1998).Google Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2008

Authors and Affiliations

  • Donna A. Volpe
    • 1
  • Ebenezer B. Asafu-Adjaye
    • 1
  • Christopher D. Ellison
    • 1
  • Suresh Doddapaneni
    • 2
  • Ramana S. Uppoor
    • 2
  • Mansoor A. Khan
    • 1
  1. 1.Division of Product Quality ResearchFood and Drug AdministrationSilver SpringUSA
  2. 2.Division of Clinical Pharmacology, Center for Drug Evaluation and ResearchFood and Drug AdministrationSilver SpringUSA

Personalised recommendations