Comparative analgesic efficacy of nimesulide and diclofenac gels after topical application on the skin.

作者: S. Sengupta , T. Velpandian , P. Sapra , P. Mathur , S.K. Gupta

DOI: 10.1159/000029837

关键词:

摘要: Nimesulide is a newer non-steroidal anti-inflammatory drug (NSAID) with selective cyclo-oxygenase (COX)-2 blocking property and has demonstrated potent analgesic activity on oral rectal administration. However, the Cmax through both these routes reached only after 3 h of Dose-dependent gastrointestinal side effects also limit concentration that can be achieved at site inflammation when administered routes. The present study was conducted to evaluate antinociception induced by new gel formulation nimesulide applied skin. Efficacy topical 1% (w/w) studied mice in acetic-acid-induced writhing, tail flick latency (TFL) test formalin-induced pain models. antinociceptive effect compared diclofenac (1% w/w). Both drugs dose-dependent analgesia peak seen between 90 120 min treatment. Greater (expressed as percent maximum possible effect) writhing than TFL test, indicating peripheral action drugs. evidenced significant protection first phase modulation nociceptors unlike other conventional NSAIDs. This suggests COX-2 may primary contributor afferent evoked increase prostanoid-mediated changes processing. Antinociception following application skin lower intraperitoneal administration, localised application. findings suggest transgel provides topically.

参考文章(18)
Vinod P. Shah, Charan R. Behl, Gordon L. Flynn, William I. Higuchi, Hans Schaefer, Brian W. Barry, Charan R. Behl, Dale P. Conners, C.Carnot Evans, Gordon L. Flynn, Thomas J. Franz, Eugene H. Gans, William I. Higuchi, Nicholas Kail, Gerald G. Krueger, James Leyden, Howard I. Maibach, A.Waseem Malick, Sargio Nacht, Shirley Ng, Carl C. Peck, Lynn K. Pershing, Russell O. Potts, Boyd J. Poulsen, Hans Schaefer, Robert C. Scott, Joel A. Seqeira, Vinod P. Shah, Dinesh Sharma, Jerome P. Skelly, Maw-Sheng Wu, Principles and criteria in the development and optimization of topical therapeutic products. Sponsored by the American Association of Pharmaceutical Scientists (AAPS) and U.S. Food and Drug Administration (FDA) International Journal of Pharmaceutics. ,vol. 82, pp. 21- 28 ,(1992) , 10.1016/0378-5173(92)90067-C
Vinod P. Shah, Charan R. Behl, Gordon L. Flynn, William I. Higuchi, Hans Schaefer, Principles and criteria in the development and optimization of topical therapeutic products. Pharmaceutical Research. ,vol. 9, pp. 1107- 1112 ,(1992) , 10.1023/A:1015831201020
A.F. Schärli, K. Brülhart, T. Monti, Pharmacokinetics and therapeutic study with nimesulide suppositories in children with post-operative pain and inflammation. Journal of International Medical Research. ,vol. 18, pp. 315- 321 ,(1990) , 10.1177/030006059001800408
S. K. Gupta, J. Prakash, L. Awor, S. Joshi, T. Velpandian, S. Sengupta, Anti-inflammatory activity of topical nimesulide gel in various experimental models. Inflammation Research. ,vol. 45, pp. 590- 592 ,(1996) , 10.1007/BF02312040
Steinar Hunskaar, Ole Bernt Fasmer, Kjell Hole, Formalin test in mice, a useful technique for evaluating mild analgesics Journal of Neuroscience Methods. ,vol. 14, pp. 69- 76 ,(1985) , 10.1016/0165-0270(85)90116-5
C. J. Grossman, J. Wiseman, F. S. Lucas, M. A. Trevethick, P. J. Birch, Inhibition of constitutive and inducible cyclooxygenase activity in human platelets and mononuclear cells by NSAIDS and Cox 2 inhibitors Inflammation Research. ,vol. 44, pp. 253- 257 ,(1995) , 10.1007/BF01782978
Sanford H. Roth, NSAID Gastropathy Archives of Internal Medicine. ,vol. 156, pp. 1623- 1628 ,(1996) , 10.1001/ARCHINTE.1996.00440140039003