ArticleJournal of the American Association for Laboratory Animal Science : JAALAS2021
Pharmacokinetic and Histopathologic Study of an Extended-Release, Injectable Formulation of Buprenorphine in Sprague-Dawley Rats.
Article in Journal of the American Association for Laboratory Animal Science : JAALAS, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 29 citations in OpenAlex.
- Pharmacokinetics of a Single Subcutaneous Extended-Release Buprenorphine (Ethiqa XR) in Healthy Beagles.Journal of veterinary pharmacology and therapeutics · 2026Article
- Evaluation of a human slow-release buprenorphine formulation in rats - tactile sensitivity and plasma concentration.Laboratory animal research · 2026Article
- Efficacy and Pharmacokinetics of 3 Sustained-Release Buprenorphine Formulations in Cairo Spiny Mice (Acomys cahirinus).Journal of the American Association for Laboratory Animal Science : JAALAS · 2026Article
- Serum Pharmacokinetics of a Highly Concentrated Buprenorphine Formulation in Older Female Sprague-Dawley Rats (Rattus norvegicus).Journal of the American Association for Laboratory Animal Science : JAALAS · 2025Article
- Pharmacokinetic Analysis of Sustained-Release Buprenorphine Formulations in Owl Monkeys (Aotus spp.).Journal of the American Association for Laboratory Animal Science : JAALAS · 2025Article
- Pharmacokinetics of Extended-release Buprenorphine and Clinical Efficacy for Postoperative Pain Management in the Domestic Ferret (Journal of the American Association for Laboratory Animal Science : JAALAS · 2024Article
- Pharmacokinetic Evaluation of a Topical Extended-release Analgesic in Mice.Journal of the American Association for Laboratory Animal Science : JAALAS · 2024Article
- Evaluation and comparison of pharmacokinetic profiles and safety of two extended-release buprenorphine formulations in common marmosets (Callithrix jacchus).Scientific reports · 2023Article
- Long-Acting Opioid Analgesics for Acute Pain: Pharmacokinetic Evidence Reviewed.Veterinary sciences · 2023Review
- A Review of Long-acting Parenteral Analgesics for Mice and Rats.Journal of the American Association for Laboratory Animal Science : JAALAS · 2022Review
- Efficacy of 3 Buprenorphine Formulations for the Attenuation of Hypersensitivity after Plantar Incision in Immunodeficient NSG Mice.Journal of the American Association for Laboratory Animal Science : JAALAS · 2022Article
- Pharmacokinetics of Sustained-release and Extended-release Buprenorphine in Mice after Surgical Catheterization.Journal of the American Association for Laboratory Animal Science : JAALAS · 2022Article
- Assessment of the Safety and Efficacy of Pre-emptive Use of Extended-release Buprenorphine for Mouse Laparotomy.Journal of the American Association for Laboratory Animal Science : JAALAS · 2022Article
- Effectiveness of two extended-release buprenorphine formulations during postoperative period in neonatal rats.PloS one · 2022Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A novel buprenorphine (BUP) extended-release formulation (BUP-XR) produced as a lipid-encapsulated, low viscosity BUP suspension for SC injection to control pain was evaluated for pharmacokinetics and safety in Sprague-Dawley rats given either 0.65 mg/kg (low dose) or 1.30 mg/kg (high dose). The 2 dosage groups each contained 6 male and 6 female rats to determine whether BUP-XR behaved differently in male or female animals. Blood samples were obtained from each animal before BUP-XR administration and at 6, 24, 48, 72, 96, and 168 h after administration. For necropsy and injection-site histopathology evaluation, 3 animals of each sex from each test group were euthanized on day 8, with the remaining animals euthanized on day 15. Mean plasma BUP concentration peaked from 6 to 24 h in all test groups, then declined in a linear fashion. Quantifiable plasma BUP was measured in all male rats at all time points except for one low dose group sample taken at 168 h. Female rats had quantifiable plasma BUP at all time points except for 1 low dose group sample at 72 and 96 h, and 2 low dose group samples at 168 h. The low dose groups, whether male or female, had lower mean plasma BUP levels at all time points as compared with their high dose counterparts, and female rats had lower mean plasma BUP levels than male rats at all time points. Results indicate that a single BUP-XR dose at either dose concentration can reliably provide plasma levels of BUP reported in the literature to be therapeutically relevant for up to 72 h, although lower plasma BUP levels can be anticipated in female rats compared with male counterparts. Mild to moderate injection-site granulomatous inflammation was observed in 6 of 12 rats in the low dose group and 7 of 12 in the high dose group. This reaction is characteristic of lipid material designed to persist in situ.
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