Buprenorphine tablet versus liquid: A clinical trial comparing plasma levels, efficacy, and symptoms

• Published in: Journal of substance abuse treatment Vol. 29; no. 4; pp. 307 - 312
• Main Authors: Chawarski, Marek C., Moody, David E., Pakes, Juliana, O'Connor, Patrick G., Schottenfeld, Richard S.
• Format: Journal Article
• Language: English
• Published: New York, NY Elsevier Inc 01.12.2005; Elsevier Science; Elsevier Limited
• Subjects: Addictive behaviors; Administration, Sublingual; Adult; Adult and adolescent clinical studies; Biological and medical sciences; Buprenorphine; Buprenorphine - administration & dosage; Buprenorphine - adverse effects; Buprenorphine - pharmacokinetics; Clinical trials; Desintoxication. Drug withdrawal; Drug addiction; Drug therapy; Female; Humans; Male; Medical sciences; Metabolic Clearance Rate; Middle Aged; Miscellaneous; Narcotic Antagonists - administration & dosage; Narcotic Antagonists - adverse effects; Narcotic Antagonists - pharmacokinetics; Opioid maintenance; Opioid-Related Disorders - blood; Opioid-Related Disorders - rehabilitation; Pharmaceutical Solutions; Plasma; Plasma concentration; Psychology. Psychoanalysis. Psychiatry; Psychopathology. Psychiatry; Public health. Hygiene; Public health. Hygiene-occupational medicine; Substance abuse; Substance Withdrawal Syndrome - blood; Substance Withdrawal Syndrome - diagnosis; Tablets; Treatment Outcome; Treatments; Substance abuse; Opioid maintenance; Buprenorphine; Plasma concentration; Human; Drug addiction; Replacement therapy; Poison withdrawal; Treatment efficiency; Opiates; Concentration; Narcotic analgesic; Symptomatology; Dependence; Dosage form; Clinical trial; Drug of abuse; Pharmacokinetics; Comparative study; Heroin; Public health
• ISSN: 0740-5472; 1873-6483
• DOI: 10.1016/j.jsat.2005.08.011

We evaluated peak plasma concentrations, trough concentrations, and the 24-hour area under the concentration curve (AUC 0–24 h) during maintenance with sublingual (SL) liquid or tablet formulations in 57 opiate-dependent volunteers. Study participants were assigned randomly to one of three SL daily buprenorphine dose pairs and maintained for 2 weeks with the liquid formulation followed by 2 weeks with the corresponding tablet dose. Plasma samples were obtained after at least 10 days of maintenance with the liquid formulation and after at least 10 days of that with the tablet formulation. The bioequivalence of the tablet compared with the liquid doses ranged from 57% to 75% based on peak concentrations, from 102% to 108% based on trough concentrations, and from 66% to 86% based on 24-hour AUC, but there was a large intersubject and intrasubject variability in plasma concentrations, with greater variability following tablets than liquid. Measures of withdrawal symptoms or illicit opioid use were not associated with buprenorphine dose, formulation, or plasma buprenorphine levels.