Relative bioavailability of different buprenorphine formulations under chronic dosing conditions

Drug Alcohol Depend. 2004 Apr 9;74(1):37-43. doi: 10.1016/j.drugalcdep.2003.11.008.


Background: Buprenorphine is an approved medication for the treatment of opioid dependence. Three sublingual formulations have been used at various times during its development-a solution containing alcohol, tablets containing buprenorphine alone, and tablets containing buprenorphine plus naloxone. This study compared the relative buprenorphine bioavailability of these different formulations.

Methods: Outpatient volunteers (N = 10) were maintained for 14 days of daily administration on each formulation; the dose of buprenorphine (8 mg) was constant across formulations. Blood samples were collected and tested for buprenorphine and norbuprenorphine concentrations after 7 and 14 days maintenance on each formulation. Serial samples were collected before and for 6 h after a daily dose of each formulation.

Results: Peak buprenorphine concentrations (C(max)) and area under the curve (AUC) for the 6h interval (AUC(0-6)) were highest for the solution and lowest for buprenorphine alone tablets; values for combination tablets were more similar to those for solution. Differences between formulations were less pronounced at day 14 than day 7. There was considerable between-subject variability in concentrations produced.

Conclusions: These results suggest there may be greater bioavailability of buprenorphine/naloxone versus buprenorphine alone tablets, and that the bioavailability of buprenorphine from the former is very similar to that seen with solution after 2 weeks of stabilization on each formulation.

Publication types

  • Comparative Study
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Area Under Curve
  • Biological Availability
  • Buprenorphine / administration & dosage*
  • Buprenorphine / analogs & derivatives*
  • Buprenorphine / blood*
  • Chemistry, Pharmaceutical
  • Female
  • Humans
  • Male
  • Opioid-Related Disorders / blood*
  • Opioid-Related Disorders / drug therapy*


  • Buprenorphine
  • norbuprenorphine