Related Experiment Video
Updated: Aug 9, 2026

Intravascular Delivery of Biologics to the Rat Kidney
Published on: September 1, 2016
Novel depots of buprenorphine prodrugs have a long-acting antinociceptive effect
Kuo-Sheng Liu1, Jann-Inn Tzeng, Yu-Wen Chen
1Department of Anesthesiology and Medical Research, Chi-Mei Medical Center, Tainan, Taiwan.
Abstract:
An analgesic with a prolonged duration may be desirable in patients with long-lasting pain. In this study, we evaluated the antinociceptive effects and durations of action of three novel depots of buprenorphine esters buprenorphine propionate, enanthate, and decanoate given by IM injection, in rats. The pharmacokinetic profiles of buprenorphine in blood after IM injection of these depots were also evaluated. Antinociception was evaluated using the plantar test. Buprenorphine concentrations in blood were assayed using high-performance liquid chromatography. We found that the traditional form of buprenorphine HCl (in saline) produced a dose-related antinociceptive effect. A dose of 0.6 micromol/kg buprenorphine HCl (in saline) produced a significant antinociceptive effect lasting 5 h. The same dose of buprenorphine base, propionate, enanthate, and decanoate (in oil) also produced a significant antinociceptive effect with longer durations of action of 26, 28, 52, and 70 h, respectively. The pharmacokinetic studies demonstrated that all the buprenorphine esters were prodrugs of buprenorphine. We conclude that the novel depots of buprenorphine prodrugs: buprenorphine propionate, enanthate, and decanoate produced a long-acting antinociceptive effect after IM injection in rats.
Related Concept Videos
Opioid Analgesics: Synthetic and Semisynthetic Opioids
Analgesia and Pain Management
Oral Drug Delivery Systems: Continuous-Release Systems
Opioid Analgesics: Morphine and Other Natural Cogeners
Opioid Receptors: Overview
Nondepolarizing (Competitive) Neuromuscular Blockers: Pharmacokinetics
Instead, they are transported by the blood to different tissues. Muscles with a greater blood supply (arteries) and blood flow receive more...

