Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2014 Jul;53(4):387-91.

Pharmacokinetic comparison of sustained-release and standard buprenorphine in mice

Tannia S Clark  1 , David D Clark  2 , Robert F Hoyt Jr  3
Affiliations

Pharmacokinetic comparison of sustained-release and standard buprenorphine in mice

Tannia S Clark et al. J Am Assoc Lab Anim Sci. 2014 Jul.

Abstract

Effective pain medication is important for animal stewardship and valid research results. We compared the pharmacokinetic assessments of standard, immediate-release buprenorphine (Bup IR) and a sustained-release buprenorphine formulation (Bup SR Lab) in male C57BL/6J mice, a mouse strain commonly used in biomedical research. We postulated that the administration of Bup SR Lab would achieve a more persistent blood drug concentration (>1 ng/mL) compared with single-dose Bup IR. The study assumed a blood buprenorphine concentration of 1 ng/mL as the minimum that may result in adequate analgesia, as previously reported. The 7 experimental groups included Bup IR (0.03, 0.05, 0.1, and 2 mg/kg), Bup SR Lab (0.3 and 1.2 mg/ kg), and saline placebo (0.7 mL/100 g). Blood sampling occurred at 0.5, 1, 3, 6, 12, 24, 48, and 72 h for evaluation by using a forensic ELISA. Bup IR at 0.03 and 0.05 mg/kg and Bup SR Lab at 0.3 mg/kg failed to obtain maximal blood concentrations (Cmax) above 1 ng/mL. All other doses (0.1 and 2 mg/kg Bup IR and 1.2 mg/kg Bup SR Lab) reached a Cmax above 1 ng/mL within 3 h after injection. In addition, 1.2 mg/kg Bup SR Lab and 2 mg/kg Bup IR provided blood concentrations above 1 ng/mL for up to 12 h, and 0.1 mg/kg Bup IR achieved this criterion for as long as 3 h. In conclusion, Bup SR Lab at 1.2 mg/kg and Bup IR at 0.1 or 2.0 mg/kg achieve or surpass the published threshold for adequate analgesia in mice.

PubMed Disclaimer

Figures

Figure 1.
Figure 1.
Notional representation of randomly presented test group sampled at 8 time points after injection.
Figure 2.
Figure 2.
Notional representation of randomly presented test group, sampled at 6 time points after injection.
Figure 3.
Figure 3.
This graph plots the buprenorphine concentration in blood of different buprenorphine formulations over 48 h. Horizontal dashed lines represent therapeutic threshold (1 ng/mL) and lower limit of quantitation (0.33 ng/mL). Values below the lower limit of quantification are extrapolated values.
See this image and copyright information in PMC

References

    1. Carbone ET, Lindstrom KE, Diep S, Carbone L. 2012. Duration of action of sustained-release buprenorphine in 2 strains of mice. J Am Assoc Lab Anim Sci 51:815–819 - PMC - PubMed
    1. Carbone L. 2012. Pain management standards in the eighth edition of the Guide for the Care and Use of Laboratory Animals J Am Assoc Lab Anim Sci 51:322–328. - PMC - PubMed
    1. Catbagan DL, Quimby JM, Mama KR, Rychel JK, Mich PM. 2011. Comparison of the efficacy and adverse effects of sustained-release buprenorphine hydrochloride following subcutaneous administration and buprenorphine hydrochloride following oral transmucosal administration in cats undergoing ovariohysterectomy. Am J Vet Res 72:461–466 - PubMed
    1. Chawarski MC, Schottenfeld RS, O'Connor PG, Pakes J. 1999. Plasma concentrations of buprenorphine 24 to 72 hours after dosing. Drug Alcohol Depend 55:157–163 - PubMed
    1. Christoph T, Kogel B, Schiene K, Meen M, De Vry J, Friderichs E. 2005. Broad analgesic profile of buprenorphine in rodent models of acute and chronic pain. Eur J Pharmacol 507:87–98 - PubMed