• DOI:10.1177/009127009703700106
• Corpus ID: 31735116

Bioavailability of Sublingual Buprenorphine

@article{Mendelson1997BioavailabilityOS,
  title={Bioavailability of Sublingual Buprenorphine},
  author={John E. Mendelson and Robert A. Upton and E. Thomas Everhart and Peyton Jacob Iii and Reese T. Jones},
  journal={The Journal of Clinical Pharmacology},
  year={1997},
  volume={37}
}

• J. Mendelson, R. Upton, +2 authors Reese T. Jones
• Published 1 January 1997
• Medicine, Biology
• The Journal of Clinical Pharmacology

Buprenorphine administered sublingually is a promising treatment for opiate dependence. Utilizing a new, sensitive, and specific gas chromatographic electron‐capture detector assay, the absolute bioavailability of sublingual buprenorphine was determined in six healthy volunteers by comparing plasma concentrations after 3‐ and 5‐minute exposures to 2 mg sublingual and 1 mg intravenous buprenorphine. The amount of unabsorbed buprenorphine in saliva was measured after 2‐, 4‐, and 10‐minute exposures to 2 mg sublingual buprenorphine in 12 participants. Pharmacokinetic parameters were analyzed by analysis of variance; bioequivalence was evaluated by the Schuirmann two‐sided test. The 3‐ and 5‐ minute sublingual exposures each allowed 29 ± 10% bioavailability (area under the plasma concentration—time curve unextrapolated) and were bioequivalent. Buprenorphine recovered from saliva after 2‐, 4‐, and 10‐minute exposures was, on average, 52% to 55% of dose. Increased saliva pH was correlated with decreased recovery from saliva. Study results indicate that bioavailability of sublingual buprenorphine is approximately 30%. Sublingual exposure times between 3 and 5 minutes produce equivalent results. Buprenorphine remaining in saliva causes an almost twofold overestimation of bioavailability.