Buprenorphine pharmacokinetics: relative bioavailability of sublingual tablet and liquid formulations.
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.
Nath
R P
RP
Drug Dependence Research Center, Langley Porter Psychiatric Institute, University of California, San Francisco 94143-0984, USA.
Upton
R A
RA
Everhart
E T
ET
Cheung
P
P
Shwonek
P
P
Jones
R T
RT
Mendelson
J E
JE
D000286:Administration, Sublingual; D000328:Adult; D000701:Analgesics, Opioid / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D002047:Buprenorphine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D006339:Heart Rate / Q000187:drug effects; D006801:Humans; D008297:Male; D009294:Narcotics / Q000009:adverse effects; D019999:Pharmaceutical Solutions; D013375:Substance Withdrawal Syndrome / Q000503:physiopathology; D013607:Tablets
D000701:Analgesics, Opioid; D009294:Narcotics; D019999:Pharmaceutical Solutions; D013607:Tablets; D002047:Buprenorphine