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J Addict Med. 2007 Jun;1(2):88-95. doi: 10.1097/ADM.0b013e31806dcc3e.

Pharmacokinetics of buprenorphine: a comparison of sublingual tablet versus liquid after chronic dosing.

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From the UCLA School of Nursing (PC), Los Angeles, CA; UCLA Integrated Substance Abuse Programs (WL, DL, CC), Los Angeles, CA; Division of Pharmacotherapies and Medical Consequences of Drug Abuse (CNC), National Institute on Drug Abuse, Bethesda, MD; Center for Human Toxicology (DEM), University of Utah, Salt Lake City, UT; and University of Washington (AH), Drug and Alcohol Institute, Seattle, WA.


Although buprenorphine is approved for use in the outpatient treatment of opioid addiction in 2 tablet formulations, a monoproduct containing buprenorphine only (Subutex) and a buprenorphine/naloxone combination product (Suboxone), much of the clinical data that support the approval by the U.S. Food and Drug Administration were generated by using a sublingual liquid. To interpret the literature in prescribing parameters for tablet buprenorphine, this study was designed to determine steady state buprenorphine plasma levels for the 2 formulations and to assess the relative bioavailability of each. A randomized, double-blind, crossover study with dose increases was conducted during a 12-week period at an outpatient treatment clinic. Of the 184 subjects initially randomized to treatment, 133 (72.3%) were evaluated for the steady-state trough plasma concentration, 16 (8.7%) for relative bioavailability, and 31 (16.8%) for dose proportionality. At steady state, differences in the trough plasma concentrations of buprenorphine between the 2 formulations were found across all the dose levels. Average plasma concentration (Cavg) of the tablet at twice the milligram dose of the liquid was twice that of the liquid; intersubject variability was greater for the tablet. At double the dose of tablet, there is no difference in steady state plasma concentrations. The bioavailability seems equivalent for the 2 formulations across all the dose levels.

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