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BJA Advance Access published online on March 5, 2004
British Journal of Anaesthesia, doi:10.1093/bja/aeh126
© 2004 by The Board of Management and Trustees of the British Journal of Anaesthesia
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Accepted December 5, 2003

Laboratory Investigation

Antinociceptive effect of a novel long-acting nalbuphine preparation{dagger}

K. S. Liu 1, O. Y. P. Hu 2, S. T. Ho 3, J. I. Tzeng 4, Y. W. Chen 4, J. J. Wang 4*

1 Department of Medical Research, Chi-Mei Medical Center, Tainan, Taiwan; Department of Chemistry, National Cheng Kung University, Tainan, Taiwan
2 Department of Research and Education, National Defense Medical Center, Taipei, Taiwan
3 Department of Anesthesiology, Tri-Service General Hospital, Taipei, Taiwan
4 Department of Medical Research, Chi-Mei Medical Center, Tainan, Taiwan

* To whom correspondence should be addressed. E-mail: 400002{at}mail.chimei.org.tw.


  Abstract

Background. A long-acting analgesic may be particularly desirable in patients suffering from long-lasting pain. The aim of the study was to evaluate the antinociceptive effect of a novel nalbuphine preparation and to determine its duration of action.

Methods. The antinociceptive effects of i.m. nalbuphine HCl in saline and nalbuphine base in sesame oil were evaluated in rats. The in vitro drug-releasing profiles of nalbuphine HCl and base in different preparations were also evaluated.

Results. We found that i.m. nalbuphine HCl 25, 50 and 100 µmol kg-1 produced dose-related antinociceptive effects with a duration of action of 1.5, 2 and 3 h, respectively. I.M. nalbuphine base 100, 200 and 400 µmol kg-1 also produced dose-related antinociceptive effects but with longer durations of action: 27, 49 and 55 h, respectively. In vitro studies demonstrated that nalbuphine base in sesame oil had the slowest drug-releasing profile of the different preparations.

Conclusions. I.M. injection of an oil formulation of nalbuphine base produced a long-lasting antinociceptive effect.

Keywords: Keywords: analgesics opioid, nalbuphine; nerve, long-acting antinociception


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