The Safety of EXPAREL ® (Bupivacaine Liposome Injectable Suspension) Administered by Peripheral Nerve Block in Rabbits and Dogs
| Autor: | Marlon C. Rebelatto, Phaedra I. Cole, Paul E. Ross, Brigitte M. Richard, Abram N. Brubaker, Keith Nelson, Dean Haan, Laura R. Ott, Paul E. Newton |
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| Rok vydání: | 2012 |
| Předmět: |
Bupivacaine
medicine.medical_specialty Article Subject Nerve root Clinical pathology business.industry medicine.medical_treatment lcsh:RS1-441 Adipose tissue Surgery lcsh:Pharmacy and materia medica Pharmacokinetics Anesthesia medicine Histopathology business Saline Brachial plexus Research Article medicine.drug |
| Zdroj: | Journal of Drug Delivery Journal of Drug Delivery, Vol 2012 (2012) |
| ISSN: | 2090-3022 2090-3014 |
| Popis: | A sustained-release DepoFoam injection formulation of bupivacaine (EXPAREL, 15 mg/mL) is currently being investigated for postsurgical analgesia via peripheral nerve block (PNB). Single-dose toxicology studies of EXPAREL (9, 18, and 30 mg/kg), bupivacaine solution (Bsol, 9 mg/kg), and saline injected around the brachial plexus nerve bundle were performed in rabbits and dogs. The endpoints included clinical pathology, pharmacokinetics, and histopathology evaluation on Day 3 and Day 15 (2/sex/group/period). EXPAREL resulted in a nearly 4-fold lower Cmax versus Bsol at the same dose. EXPAREL was well tolerated at doses up to 30 mg/kg. The only EXPAREL-related effect seen was minimal to mild granulomatous inflammation of adipose tissue around nerve roots (8 of 24 rabbits and 7 of 24 dogs) in the brachial plexus sites. The results indicate that EXPAREL was well tolerated in these models and did not produce nerve damage after PNB in rabbits and dogs. |
| Databáze: | OpenAIRE |
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