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J Clin Pharmacol 1997 Jan;37(1):31-7
TRIAL - Bio-availability of sublingual
buprenorphine.
CONDUCTED BY - Mendelson J, Upton RA, Everhart ET, Jacob P 3rd, Jones RT
CONDUCTED AT
- Drug Dependence Research Center, Langley Porter Psychiatric Institute, University of California, San Francisco 94143-0984, USA.
Buprenorphine administered sublingually is a promising treatment for opiate dependence. Utilizing a new, sensitive, and specific gas chromatographic electron-capture detector assay, the absolute bio-availability of sublingual buprenorphine was determined in 6 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 analysed by analysis of variance; bio-equivalence was evaluated by the Schuirmann two-sided test. The 3- and 5-minute sublingual exposures each allowed 29 +/- 10% bio-availability (area under the plasma concentration-time curve unextrapolated) and were bio-equivalent. 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 bio-availability 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.
PMID:
9048270,
UI: 97200335
RUSAN
II ADDNOK