| Autor: |
Richard BM; Clinical Research and Drug Safety Assessment, Pacira Pharmaceuticals, Inc., 10450 Science Center Drive, San Diego, CA 92121, USA., Newton P, Ott LR, Haan D, Brubaker AN, Cole PI, Ross PE, Rebelatto MC, Nelson KG |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of drug delivery [J Drug Deliv] 2012; Vol. 2012, pp. 962101. Date of Electronic Publication: 2012 Jan 17. |
| DOI: |
10.1155/2012/962101 |
| Abstrakt: |
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 C(max) 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: |
MEDLINE |
| Externí odkaz: |
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