Relative bioavailability of different buprenorphine formulations under chronic dosing conditions

Eric C. Strain, David E. Moody, Kenneth B. Stoller, Sharon L. Walsh, George E. Bigelow

Research output: Contribution to journalArticlepeer-review

69 Scopus citations


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 (8mg) 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 6h after a daily dose of each formulation. Results: Peak buprenorphine concentrations (Cmax) and area under the curve (AUC) for the 6h interval (AUC0-6) 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.

Original languageEnglish
Pages (from-to)37-43
Number of pages7
JournalDrug and Alcohol Dependence
Issue number1
StatePublished - Apr 9 2004

Bibliographical note

Funding Information:
Some of these data were presented at the annual meeting of the College on Problems of Drug Dependence, held in Quebec City, Canada (June of 2002). The authors thank the staff at the Behavioral Pharmacology Research Unit for their help on this project, and the National Institute on Drug Abuse for its assistance and the supplies of buprenorphine used in this study. This study was supported by US Public Health Service Scientist Development Award K02 DA00332 (E.C.S.), Research Scientist Award K05 DA00050 (G.E.B.), T32 DA07209, R01 DA08045, R01 DA10100, and N01 DA-7-8074 from the National Institute on Drug Abuse.


  • Buprenorphine
  • Formulation
  • Pharmacokinetics
  • Pharmacotherapy
  • Treatment

ASJC Scopus subject areas

  • Toxicology
  • Pharmacology
  • Psychiatry and Mental health
  • Pharmacology (medical)


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