Diclofenac Sodium Injection (Dyloject®)
- 188 Downloads
▲ A new formulation of the nonselective NSAID diclofenac sodium suitable for intravenous bolus injection has been developed using hydroxypropyl β-cyclodextrin as a solubility enhancer (HPβCD diclofenac).
▲ HPβCD diclofenac intravenous bolus injection was shown to be bioequivalent to the existing parenteral formulation of diclofenac containing propylene glycol and benzyl alcohol as solubilizers (PG-BA diclofenac), which is relatively insoluble and requires slow intravenous infusion over 30 minutes.
▲ Single-dose HPβCD diclofenac 3.75, 9.4, 18.75, 25, 37.5, 50 and 75 mg administered by intravenous bolus injection produced significantly greater responses than placebo for total pain relief (TOTPAR) over 6 hours or pain intensity at 4 hours in the treatment of moderate or severe postoperative dental pain in randomized, double-blind trials. HPβCD diclofenac 37.5 and 75 mg were similar in efficacy to intravenous bolus ketorolac 30 mg.
▲ In a well controlled trial, single-dose HPβCD diclofenac 75 mg intravenous bolus injection was shown to be superior to PG-BA diclofenac 75 mg intravenous infusion with respect to TOTPAR over 4 hours, indicating faster onset of analgesia in the treatment of moderate or severe postoperative dental pain. Both HPβCD diclofenac and PG-BA diclofenac were superior to placebo.
▲ HPβCD diclofenac was generally well tolerated during single-dose treatment of postoperative pain. The tolerability profile was similar to that of PG-BA diclofenac, but with a lower incidence of thrombophlebitis.
KeywordsPain Intensity Ketorolac Thrombophlebitis Intramuscular Administration Intravenous Bolus Injection
- 4.National Pharmaceutical Council. Pain: current understanding of assessment, management, and treatments [online]. Available from URL: http://www.npcnow.org/resources/PDFs/painmonograph.pdf [Accessed 2007 Jun 5]
- 6.Barden J, Edwards J, Moore RA, et al. Single dose oral diclofenac for postoperative pain. Cochrane Database Syst Rev 2004; (2): CD004768Google Scholar
- 11.Javelin Pharmaceuticals Inc. A phase 1, randomized, analytically blind, fasted, single-dose, four-way crossover study of the bioavailability of one dose level of parenteral DIC075V (diclofenac sodium 75 mg/2 ml), administered intramuscularly and intravenously, vs. parenteral Voltarol® (diclofenac sodium 75 mg/3 ml) administered intramuscularly and intravenously in healthy adult volunteers. New York: Javelin Pharmaceuticals Inc., 2004. (Data on file)Google Scholar
- 13.Javelin Pharmaceuticals Inc. A randomized, double-blind, placebo- and comparator-controlled, single-dose, parallel-group comparison of the analgesic efficacy and safety of intravenous DIC075V (diclofenac sodium injection), ketorolac tromethamine and placebo following surgery. New York: Javelin Pharmaceuticals Inc., 2006. (Data on file)Google Scholar
- 14.Data on file, Javelin Pharmaceuticals Inc., 2007Google Scholar
- 15.Wallerstein K. A cost minimization analysis of IV bolus versus IV infusion diclofenac in post-operative pain [abstract and poster]. 10th Annual European Congress of the International Society for Pharmacoeconomics and Outcomes Research; 2007 Oct 20–23; DublinGoogle Scholar
- 17.Novartis Pharmaceuticals UK Ltd. Voltarol ampoules: summary of product characteristics [online]. Available from URL: http://emc.medicines.org.uk [Accessed 2007 May 30]
- 18.Javelin Pharmaceuticals Inc. Javelin Pharmaceuticals receives marketing authorization approval for Dyloject® in the United Kingdom [media release]. 2007 Oct 31Google Scholar