Pharmacokinetics, bioavailability and opioid effects of liquid versus tablet buprenorphine
Pharmacokinetics, bioavailability and opioid effects of liquid versus tablet buprenorphine
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DOI：
10.1016/j.drugalcdep.2005.08.005
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发表时间：
2006-03-15
影响因子：
4.2
通讯作者：
Chiang, N
中科院分区：
文献类型：
--
作者：
Compton, P;Ling, W;Chiang, N
Aims: Two tablet formulations of buprenorphine (a buprenorphine mono-product, subutex(R), and a buprenorphine/naloxone combination product, Suboxone(R)) are available for use in the treatment of opioid addiction; however, the bulk of the clinical studies supporting its approval by the US Food and Drug Administration (FDA) were conducted with a sublingual liquid preparation. To assist the clinician in interpreting the relevant literature in establishing dosing parameters for prescription of tablet buprenorphine, this Study was designed to compare the steady state: (1) pharmacokinetics and bioavailability, and (2) physiological, subjective and objective opiate effects of two 8 mg buprenorphine tablets (16 mg) to those of 1 ml (8 mg/ml) buprenorphine solution based upon early reports Suggesting that the bioavailability of the tablet was approximately 50% of that of the liquid.Design: Randomized, open-label, two-way crossover Study.Setting: Inpatient hospitalization for 21 days.Participants: Twenty-four male and females in general good health and meeting DSM-IV criteria for opiate dependence.Intervention: Subjects received one of the two buprenorphine formulations in the first 10-day period, and the other for the second 10-day period with no washout.Measurements: Pharmacokinetic analyses, opiate effects and adverse events.Findings: Drug steady state was reached by Day 7 of each 10-day period, area under the Curve for 16 mg (two 8 mg) tablets was higher than the solution. The only non-kinetic statistically significant difference observed between the formulations was in changes in total opioid agonist score.Conclusions: The serum concentration achieved by 16 mg of tablet buprenorphine is higher than that of the 8 mg Solution, although differences between physiologic, subjective and objective opioid effects were not noted. The relative bioavailability of tablet versus solution is estimated to be 0.71; thus, with respect to dosing parameters for the tablet, clinicians should consider using less than 16 mg to achieve bioequivalence to the 8 mg solution. (C) 2005 Elsevier Ireland Ltd. All rights reserved.
