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Buprenorphine pharmacokinetics: relative bioavailability of sublingual tablet and liquid formulations

Nath, R.P.; Upton, R.A.; Everhart, E.T.; Cheung, P.; Shwonek, P.; Jones, R.T.; Mendelson, J.E.

Journal of Clinical Pharmacology 39(6): 619-623

1999


ISSN/ISBN: 0091-2700
PMID: 10354966
DOI: 10.1177/00912709922008236
Accession: 010260393

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Buprenorphine is an effective new treatment for opiate dependence. This study compared the bioavailability of buprenorphine from a tablet to that from a reference solution. Six men experienced with, but not dependent on, opiates (DSM-III-R) were each administered 7.7 mg of buprenorphine in liquid form and 8 mg in tablet form 1 week apart in a balanced crossover design. Plasma levels were measured by electron capture capillary gas chromatography (GC), and concentration-time curves were constructed. Pharmacokinetic data were analyzed by analysis of variance. The bioavailability from the tablet was approximately 50% that from the liquid and was not affected by saliva pH. Lower bioavailability from the tablet may be due to slow dissolution.

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