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Controlled Release Gel of Ibuprofen and Lidocaine in Epidural Use—Analgesia and Systemic Absorption in Pigs

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Abstract

Purpose. Reduction of the frequency of injections and localization of the absorption of drug molecules to the injection site would be of great advantage in epidural pain treatment. The epidural use of a controlled release gel of lidocaine and ibuprofen was studied.

Methods. The effect of a poloxamer gel (25%) containing 2% lidocaine ⋅HC1 and 2% ibuprofen ⋅ Na on the duration of analgesia after epidural administration to pigs was compared with drug in solution. Analgesia was assessed by observing the motor function and the nociceptive reflex-withdrawal response to painful pressure stimulation on the feet. Pharmacokinetic and histological examinations were performed.

Results. Analgesia lasted significantly longer after epidural lidocaine gel injection in comparison with the solution. The gel prolonged the systemic absorption, thereby increasing the epidural availability of lidocaine for spinal analgesia. Although the absorption of ibuprofen was prolonged after epidural gel injection, the duration of analgesia as compared with the solution was not prolonged. After epidural injection, only slight inflammatory changes were observed in the tissue structures of the epidural space, but none in the spinal cord.

Conclusions. These results demonstrate poloxamer gel to be a promising controlled-release, injectable epidural formulation for the management of pain.

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Authors and Affiliations

  1. Department of Pharmacy, Pharmaceutical Technology Division, University of Helsinki, Bio-center 2, P.O. Box 56, Helsinki, 00014, Finland

    Anne Paavola & Jouko Yliruusi

  2. Department of Anaesthesia, Helsinki University Central Hospital, Helsinki, Finland

    Pekka Tarkkila, Mei Xu & Per Rosenberg

  3. Department of Pathology, Haartman Institute, University of Helsinki, Helsinki, Finland

    Torsten Wahlström

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  1. Anne Paavola
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  2. Pekka Tarkkila
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  3. Mei Xu
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  4. Torsten Wahlström
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  5. Jouko Yliruusi
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  6. Per Rosenberg
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Paavola, A., Tarkkila, P., Xu, M. et al. Controlled Release Gel of Ibuprofen and Lidocaine in Epidural Use—Analgesia and Systemic Absorption in Pigs. Pharm Res 15, 482–487 (1998). https://doi.org/10.1023/A:1011992702604

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