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Bioavailability of sublingual buprenorphine
J Mendelson1, R A Upton, E T Everhart
1Drug Dependence Research Center, Langley Porter Psychiatric Institute, University of California, San Francisco 94143-0984, USA.
Journal of Clinical Pharmacology
|January 1, 1997
Summary
Sublingual buprenorphine, a treatment for opiate dependence, shows approximately 30% bioavailability. Exposure times of 3 to 5 minutes yield equivalent results, but saliva measurements can overestimate bioavailability.
Area of Science:
- Pharmacology
- Pharmacokinetics
Background:
- Sublingual buprenorphine is a key treatment for opiate dependence.
- Accurate bioavailability data is crucial for optimizing treatment efficacy.
Purpose of the Study:
- To determine the absolute bioavailability of sublingual buprenorphine.
- To evaluate the impact of sublingual exposure time on bioavailability.
- To assess the accuracy of bioavailability estimations using saliva measurements.
Main Methods:
- Developed a sensitive gas chromatographic electron-capture detector assay.
- Administered 2 mg sublingual and 1 mg intravenous buprenorphine to healthy volunteers.
- Measured buprenorphine concentrations in plasma and saliva over time.
- Analyzed pharmacokinetic parameters and evaluated bioequivalence.
Main Results:
- Sublingual buprenorphine bioavailability was approximately 29% +/- 10% for both 3- and 5-minute exposures.
- These exposure times were found to be bioequivalent.
- Saliva measurements underestimated recovery, with 52-55% of the dose recovered, and were influenced by saliva pH.
Conclusions:
- Sublingual buprenorphine bioavailability is around 30% with 3-5 minute exposure times.
- Saliva measurements can lead to significant overestimation of sublingual buprenorphine bioavailability.
- Optimized sublingual administration protocols are essential for effective opiate dependence treatment.