Therapeutic role of nimesulide in acute pain: from formulation to in vivo study
Abstract
Nimesulide, a selective cyclooxygenase-2 (COX-2) inhibitor, is a promising therapeutic agent for acute pain management owing to its rapid onset of action, favorable pharmacokinetics, and improved safety profile compared to conventional non-steroidal anti-inflammatory drugs (NSAIDs). The present study aimed to develop and evaluate Nimesulide tablets, focusing on their Preformulation, formulation, and pharmacological performance. Pre-compression and post-compression parameters confirmed acceptable flow and compressibility properties, with tablets demonstrating uniform weight, optimal hardness, low friability, and rapid disintegration. Drug content analysis revealed >98% uniformity, while in vitro release studies showed nearly complete drug release within 30 minutes, suggesting suitability for immediate pain relief. UV-spectrophotometric calibration confirmed linearity in the 6–28 µg/mL range (R² > 0.99). Solubility studies indicated poor aqueous solubility but better solubility in ethanol and acidic media. In vivo evaluation using the tail flick method in Wistar rats demonstrated a significant increase in pain threshold, with latency times increasing from 2 seconds (baseline) to 27 seconds at 1-hour post-administration, confirming a potent analgesic effect. Overall, the results validate Nimesulide’s role as an effective and well-tolerated analgesic for acute pain management, supporting its clinical relevance in modern therapeutics.
Keywords:
Nimesulide, Acute pain management, COX-2 inhibitor, Analgesic activity, Tablet formulation, In vitro drug release, Tail flick test, NSAIDsDOI
https://doi.org/10.22376/References
1. Vane JR, Botting RM. Mechanism of action of anti-inflammatory drugs. Int J Tissue React. 1998;20(1–2):3–15.
2. Bianchi M, Broggini M, Balzarini P, Vaira D, Frigo GM. Nimesulide: a selective cyclooxygenase-2 inhibitor with fast onset of action. Drugs Today. 1997;33(Suppl A):9–14.
3. Leone R, Conforti A, Di Fiore G, Moretti U, Velo G. Nimesulide: a review of its clinical pharmacology and therapeutic use. Pharmacol Res. 1999;39(1):1–13.
4. Bombardier C, Laine L, Reicin A, Shapiro D, Burgos-Vargas R, Davis B, et al. Comparison of upper gastrointestinal toxicity of rofecoxib and naproxen in patients with rheumatoid arthritis. N Engl J Med. 2000;343(21):1520–8.
5. Lombardo M, et al. Nimesulide in the treatment of acute pain: A clinical overview. Drugs. 2001;61(6):817–36.
6. Peloso PM, Fort JG, Vrooman HA, Mehlisch DR, Brown CR, Hubbard RC. A double-blind, randomized, placebo-controlled comparison of the analgesic efficacy of nimesulide, naproxen sodium, and placebo in patients with acute musculoskeletal disorders. Clin Ther. 2001;23(8):1239–54.
7. Bannwarth B, Netter P, Lapicque F, Gillet P, Péré P, Boccard E, et al. Plasma concentrations and analgesic effects of nimesulide. Br J Clin Pharmacol. 1995;40(5):431–3.
8. Rainsford KD, Kean WF, Ehrlich GE. Review of the pharmaceutical properties and clinical effects of nimesulide, a preferential COX-2 inhibitor. Inflammopharmacology. 2008;16(1):3–36.
9. Ong CK, Seymour RA, Lirk P, Merry AF. Combining paracetamol (acetaminophen) with nonsteroidal anti-inflammatory drugs: a qualitative systematic review of analgesic efficacy for acute postoperative pain. Anesth Analg. 2010;110(4):1170–9.
10. Kokki H, Kokki M, Sjövall J. Nimesulide for the treatment of acute pain in children: a systematic review. Paediatr Drugs. 2012;14(4):251–61.
11. Gan TJ. Nonsteroidal anti-inflammatory drugs in pain management. In: Miller RD, editor. Miller’s Anesthesia. 8th ed. Philadelphia: Elsevier; 2015. p. 1810–25.
12. Laine L. Gastrointestinal effects of NSAIDs and coxibs. J Pain Symptom Manage. 2003;25(2 Suppl):S32–40.
13. Farhan A, Khan NU, Ali SM. Assessment of efficacy of nimesulide in the treatment of COVID-19 infection. J Pharm Res Int. 2022;34(39B):35–42.
14. Tiwaskar M, Charde S, Balankhe N, Hegde A, Deodhar M, Gondane A, et al. Nimesulide: Critical appraisal of safety and efficacy in acute pain. J Assoc Physicians India. 2025;73(3):e22–8.
Published
Abstract Display: 256 
PDF Downloads: 204 How to Cite
Issue
Section
This work is licensed under a Creative Commons Attribution-NonCommercial-ShareAlike 4.0 International License.
How to Cite
.