THE SUBLINGUAL BIOAVAILABILITY OF BUPRENORPHINE AT ANALGESIC
DOSES
P. L. T. Bevan, M. A. Zinny, and D. M. O’Donnell
Reckitt & Colman Products Ltd, Hull HU8 7DS, UK and Medical and Technical Research Associates
Inc., Boston, Massachusetts
This was an open, single dose, randomised four-way crossover bioavailability study of buprenorphine, 0.3mg
IV and 0.2 mg, 0.4 mg and 0.8 mg SL with a one week washout between doses. Safety evaluations were
undertaken after each dose. The study was carried out in 24 male healthy volunteers aged 19-39 (mean 27.7)
years; 19 subjects completed the study. Blood samples, obtained up to 24 hours were analyzed using a
partially-specific radioimmunoassay in which the antibody is known to cross-react with N-dealkyl
buprenorphine. Mean peak plasma buprenorphine immunoreactivity concentrations of 0.28, 0.47 and
0.83ng/ml were attained at mean times of 96,91 and 91 minutes after administration of the 0.2 mg, 0.4 mg and
0.8 mg sublingual doses respectively and showed a highly significant extent of dose proportionality. Area
under the curve (0-24 hrs) was calculated from the area to the time of the last detectable plasma concentration
plus an estimate of the residual area up to 24 hours based on the terminal elimination rate. Based on mean AUC
values the % bioavailability relative to the 0.3 mg intravenous dose for the 0.2 mg, 0.4 mg and 0.8 mg
sublingual doses was 32%, 47% and 79% respectively, again showing dose proportionality. The best estimate
of the fraction (F) of buprenorphine sublingually bioavailable was 0.35 obtained using data from the 0.4mg and
0.8mg sublingual doses.
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