Evaluation of a sustained-release formulation of buprenorphine for analgesia in rats

J Am Assoc Lab Anim Sci. 2011 Mar;50(2):198-204.

Abstract

Preventing and minimizing pain in laboratory animals is a basic tenet of biomedical research and is warranted for ethical, legal, and scientific reasons. Postoperative analgesia is an important facet of pain management. A sustained-release formulation of buprenorphine was tested in rats for analgesic efficacy and plasma concentration over a 72-h time period. Rats were injected subcutaneously with either 1.2 mg/kg sustained-release formulation (Bup-SR), 0.2 mL/kg buprenorphine HCl (Bup-HCl), or an equivalent volume of sustained-release vehicle and tested in a thermal nociception model or a surgical postoperative pain model. In both models, Bup-SR showed evidence of providing analgesia for 2 to 3 d. Thermal latency response in rats that received the sustained-release formulation increased 28.4% and 15.6% compared with baseline values on days 1 and 2, respectively. Rats with a unicortical tibial defect and treated with Bup-SR showed similar willingness to bear weight on the hindlimbs as did negative-control animals (no surgery), demonstrated by counting vertical raises; rats treated with Bup-HCl had significantly fewer vertical raises than did control rats for 5 d after surgery. Plasma concentrations of buprenorphine remained over 1 ng/mL for 72 h after a single dose of Bup-SR. Taken together, the results indicate that this formulation of buprenorphine may be a viable option for treating postsurgical pain in laboratory rats.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesia / methods
  • Analgesia / veterinary*
  • Analgesics, Opioid / blood
  • Analgesics, Opioid / pharmacology*
  • Animals
  • Buprenorphine / blood
  • Buprenorphine / pharmacology*
  • Delayed-Action Preparations / pharmacology
  • Drug Combinations
  • Injections, Subcutaneous / veterinary
  • Male
  • Pain Measurement / veterinary*
  • Pain, Postoperative / drug therapy
  • Pain, Postoperative / veterinary*
  • Rats*
  • Rats, Sprague-Dawley

Substances

  • Analgesics, Opioid
  • Delayed-Action Preparations
  • Drug Combinations
  • Buprenorphine