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Relative Bioavailability of Different Buprenorphine Formulations Under Chronic Dosing Conditions

Relative Bioavailability of Different Buprenorphine Formulations Under Chronic Dosing Conditions

Eric C Strain, David E Moody, Kenneth B Stoller, Sharon L Walsh, George E Bigelow

Drug Alcohol Depend. 2004 Apr 9;74(1):37-43.

PMID: 15072805

Abstract:

Background:
Buprenorphine is an approved medication for the treatment of opioid dependence. Three sublingual formulations have been used at various times during its development-a solution containing alcohol, tablets containing buprenorphine alone, and tablets containing buprenorphine plus naloxone. This study compared the relative buprenorphine bioavailability of these different formulations.
Methods:
Outpatient volunteers (N = 10) were maintained for 14 days of daily administration on each formulation; the dose of buprenorphine (8 mg) was constant across formulations. Blood samples were collected and tested for buprenorphine and norbuprenorphine concentrations after 7 and 14 days maintenance on each formulation. Serial samples were collected before and for 6 h after a daily dose of each formulation.
Results:
Peak buprenorphine concentrations (C(max)) and area under the curve (AUC) for the 6h interval (AUC(0-6)) were highest for the solution and lowest for buprenorphine alone tablets; values for combination tablets were more similar to those for solution. Differences between formulations were less pronounced at day 14 than day 7. There was considerable between-subject variability in concentrations produced.
Conclusions:
These results suggest there may be greater bioavailability of buprenorphine/naloxone versus buprenorphine alone tablets, and that the bioavailability of buprenorphine from the former is very similar to that seen with solution after 2 weeks of stabilization on each formulation.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AS271861	Norbuprenorphine glucuronide-D3 solution			Price

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