Controlled release ibuprofen-poloxamer gel for epidural use - A pharmacokinetic study using microdialysis in pigs

Show full item record



Permalink

http://hdl.handle.net/10138/229644

Citation

Paavola , A , Bernards , C M & Rosenberg , P H 2016 , ' Controlled release ibuprofen-poloxamer gel for epidural use - A pharmacokinetic study using microdialysis in pigs ' , European Journal of Pharmaceutics and Biopharmaceutics , vol. 108 , pp. 180-186 . https://doi.org/10.1016/j.ejpb.2016.09.006

Title: Controlled release ibuprofen-poloxamer gel for epidural use - A pharmacokinetic study using microdialysis in pigs
Author: Paavola, Anne; Bernards, Christopher M.; Rosenberg, Per H.
Other contributor: University of Helsinki, Clinicum


Date: 2016-11
Language: eng
Number of pages: 7
Belongs to series: European Journal of Pharmaceutics and Biopharmaceutics
ISSN: 0939-6411
DOI: https://doi.org/10.1016/j.ejpb.2016.09.006
URI: http://hdl.handle.net/10138/229644
Abstract: In order to avoid the risks of sideeffects of epidural local anesthetics and opioids, the use of nonsteroidal anti-inflammatory drugs (NSAIDs) epidurally would be an interesting option of analgesic therapy. The fairly short duration of action of spinally administered NSAIDs, e.g., ibuprofen, may be prolonged by using controlled release poloxamer gel formulation. Using a microdialysis technique we studied the epidural and intrathecal pharmacokinetics of ibuprofen after its epidural administration as a poloxamer 407 formulation or a solution formulation. In addition, plasma ibuprofen concentrations were analyzed from central venous blood samples. Ibuprofen concentrations in the epidural space were significantly higher and longer lasting after the epidural gel injection compared with the epidural solution injection. The epidural AUC of ibuprofen was over threefold greater after epidural ibuprofen gel injection compared with the ibuprofen solution injection (p <0.001). The systemic absorption of ibuprofen from 25% poloxamer 407 gel was very low. The in situ forming poloxamer gel acted as a reservoir allowing targeted ibuprofen release at the epidural injection site and restricted ibuprofen molecules to a smaller spinal area. Ibuprofen diffusion from the epidural space to the intrathecal space was steady and prolonged. These results demonstrate that the use of epidurally injectable poloxamer gel can increase and prolong ibuprofen delivery from epidural space to the CSF enhancing thus ibuprofen entry into the central neuroaxis for spinal analgesia. Further toxicological and dose-finding studies are justified. (C) 2016 Elsevier B.V. All rights reserved.
Subject: Controlled release
Epidural
Intrathecal
Ibuprofen Na
Injectable
Microdialysis
Poloxamer 407 gel
NONSTEROIDAL ANTIINFLAMMATORY DRUGS
CEREBROSPINAL-FLUID
SPINAL-CORD
COPOLYMER MICELLES
AQUEOUS-SOLUTION
HUMAN-PLASMA
RAT
BUPIVACAINE
LIDOCAINE
MORPHINE
317 Pharmacy
3126 Surgery, anesthesiology, intensive care, radiology
Rights:


Files in this item

Total number of downloads: Loading...

Files Size Format View
1_s2.0_S0939641116305343_main.pdf 533.3Kb PDF View/Open

This item appears in the following Collection(s)

Show full item record