The aspects that describe the pre-clinical studies of aceclofenac, as an instrument of registration of a generic drug

Abstract


The paper presents the aspects of the toxicity, specific activity, pharmacokinetics and pharmacodynamics of aceclofenac, given in various sources describing its preclinical studies.

The search for information sources for the study was carried out using domestic and international databases: elibrary and PubMed using contextual queries, including terms of the international nonproprietary name, preclinical studies of pharmacokinetics, pharmacodynamics, and animal species.

Aceclofenac is one of the most prescribed drugs for acute and chronic pain. It refers to non-steroidal anti-inflammatory drugs, considered as drugs of first choice in the treatment of inflammation and pain.

On the pharmaceutical market of the Russian Federation, aceclofenac is presented in the form of tablets, powder for suspension preparation, cream for external use, which allows it to be prescribed for various diseases. It has shown itself to be highly effective in the symptomatic treatment of diseases of the musculoskeletal system, for the relief of acute and chronic pain.

A review of preclinical studies materials cited in various literature sources and including aspects of studying the toxicity, specific activity, pharmacokinetics and pharmacodynamics of aceclofenac, in our opinion, will allow using the data obtained in our study as one of the tools for further registration of generics.


About the authors

Natalia A. Anisimova

Saint Petersburg State Chemical and Pharmaceutical University, Saint Petersburg, Russia

Email: natalia.anisimova@pharminnotech.com

Russian Federation, 197376, St. Petersburg, Professora Popova st., 14

PhD in Biological Sciences at the Department of Pharmacology and Clinical Pharmacology

Natalia O. Selizarova

Saint Petersburg State Chemical and Pharmaceutical University, Saint Petersburg, Russia

Email: natalia.selizarova@pharminnotech.com

Russian Federation, 197376, St. Petersburg, Professora Popova st., 14

PhD in Medicine at the Department of Pharmacology and Clinical Pharmacology

Grigory A. Plisko

Saint Petersburg State Chemical and Pharmaceutical University, Saint Petersburg, Russia

Email: grigoriy.plisko@pharminnotech.com

Russian Federation, 197376, St. Petersburg, Professora Popova st., 14

Junior Researcher, Center for Experimental Pharmacology

Evgeny D. Semivelichenko

Saint Petersburg State Chemical and Pharmaceutical University, Saint Petersburg, Russia

Email: semivelichenko@pharminnotech.com

Russian Federation, 197376, St. Petersburg, Professora Popova st., 14

Junior Researcher, Center for Experimental Pharmacology

Svetlana M. Napalkova

Saint Petersburg State Chemical and Pharmaceutical University, Saint Petersburg, Russia

Author for correspondence.
Email: svetlana.napalkova@pharminnotech.com
SPIN-code: 7311-2841

Russian Federation, 197376, St. Petersburg, Professora Popova st., 14

PhD in Biological Sciences, Professor, Professor at the Department of Pharmacology and Clinical Pharmacology

References

  1. Goldstein JL, Larson LR, Yamashita BD and Boyd MS: Management of NSAID induced gastropathy: an economic decision analysis. Clinical therapeutics 1997: 19 (6): 1496-1509.;
  2. Lindbury P, Vojnovic I, Warner T: COX-2/COX-1 selectivity of aceclofenac in comparison with celecoxib and rofecoxib in the human whole blood assay. Osteoarthr. Cartil. (2000) 8(Suppl. B):S40-S41.;
  3. Patel N. J., Joshi B. P., Prajapati K. S., Patil V. M. Pathomorphological changes of aceclofenac toxicity in layer chicks. Veterinary World, EISSN: 2231-0916. Available at www.veterinaryworld.org/Vol.7/Feb-2014/10.pdf.
  4. Sharma, R. and Vegad, J. L. (2010) Avian gout: causes, treatment and prevention. Poultry line. 10 (8):19-21.;
  5. Ghanvat, D. P. (2012) M.V. Sc. thesis. Toxicopathological studies of ketoprofen in layer chicks, Anand Agricultural University, Anand
  6. Peloso PM: Strategies and practice for use of nonsteroidal anti-inflammatory drugs. Scandinavian Journal of Rheumatology 1996; 1 (105): 29-43;
  7. Senthilkumar, K. and Thirumurugan, R. (2005) Visceral gout in a Bengal vulture. Indian Vet. J. 82(7):795-796.;
  8. Bort R, Ponsoda X, Carrasco E, Gomez-Lechon MJ, Castell JV. Comparative metabolism of the nonsteroidal anti-inflammatory drug, aceclofenac, in the rat, monkey and human. Drug Metab Dispos 24(9): 969-975, 1996.;
  9. Henrotin Y, de Leval X, Mathy-Hartet M, Mouithys-Mickalad, A, Deby-Dupont G, Dogne JM, Delarge J and Reginster JY: In vitro effects of aceclofenac and its metabolites on the production by chondrocytes of inflammatory mediators. Inflammation Research 2001; 50 (8): 391-399.;
  10. Musmade P, Subramanian G, Srinivasan KK. High performance liquid chromatography and pharmacokinetics of aceclofenac in rats. Analytica Chimica Acta 585: 103-109, 2007.;
  11. Aydin G, Gokcimen A, Oncu M, Cicek E, Karahan N, and Gokalp O: Histopathological changes in liver and renal tissues induced by different doses of diclofenac sodium in rats. Turkish Journal of Veterinary and Animal Sciences 2003; 27: 1131-1140.;
  12. Aceclofenac. British Pharmacopoeia 1: 36-38, 2004
  13. Aceclofenac. European Pharmacopoeia 6.2: 3685-3686, 2008
  14. Gowda KV, Rajan DS, Mandal U, Selvan PS, Sam Solomon WD , Bose A, Sarkar AK, Pal TK. Evaluation of bioequivalence of two formulations containing 100 milligrams of aceclofenac. Drug Dev Ind Pharm 32: 1219-1225, 2006.;
  15. Dingle JT, Parker M: NSAID stimulation of human cartilage matrix synthesis. Clin. Drug Invest. (1997) 14:353-362
  16. Dooley M, Spencer CM, Dunn CJ: Aceclofenac. A reappraisal of its use in the management of pain and rheumatic disease. Drugs (2001) 61:1351-1378
  17. Akimoto H, Yamazaki R, Hashimoto S et al.: 4’-Hydroxyaceclofenac suppresses the interleukin-1-induced production of promatrix metalloproteinases and release of sulfated-glycosaminoglycans from rabbit articular chondrocytes. Eur. J. Pharmacol. (2000) 401:429-436.;
  18. Yamazaki R, Kawai S, Mizushima Y et al.: A major metabolite of aceclofenac, 4’-hydroxy aceclofenac, suppresses the production of interstitial pro-collagenase/proMMP 1 and pro-stromyelsin-1/proMMP-3 by human rheumatoid synovial cells.Inflamm. Res. (2000) 49:133-138.;
  19. Lindbury P, Vojnovic I, Warner T: COX-2/COX-1 selectivity of aceclofenac in comparison with celecoxib and rofecoxib in the human whole blood assay. Osteoarthr. Cartil. (2000) 8(Suppl. B):S40-S41.;
  20. Arañó A, Zapatero MI, Basi N, Duque A, Gropper S: Comparison of the anti-inflammatory effect and gastrointestinal tolerability of aceclofenac and diclofenac. Arzneim-Forsch (1996) 46:398-400;
  21. Grau M, Guasch J, Montero J et al.: Pharmacology of the potent new non-steroidal anti-inflammatory agent aceclofenac. Arzneim-Forsch (1991) 41:1265-1276.;
  22. Kulkarni S.K., Handbook of experimental pharmacology, 2nd revised and enlarged edition, Vallabh Prakashan, India, 1997. pp. 52–56.;
  23. Mutalik S., K. Paridhavi, R.C. Mallikarjuna, N. Udupa, Analgesic and antipyretic effect of Solanum melongena, Indian J. Pharmacol. 35 (2003) 312–315.;
  24. Musmade P, Subramanian G, Srinivasan KK. High performance liquid chromatography and pharmacokinetics of aceclofenac in rats. Analytica Chimica Acta 585: 103-109, 2007.;
  25. Bort R, Ponsoda X, Carrasco E, Gomez-Lechon MJ, Castell JV. Comparative metabolism of the nonsteroidal anti-inflammatory drug, aceclofenac, in the rat, monkey and human. Drug Metab Dispos 24(9): 969-975, 1996.;
  26. Noh Keumhan, Shin Beom Soo, Kwon Kwang-il et.al. Absolute bioavailability and metabolism of aceclofenac in rats/Arch. Pharm. Res. Опубл. онлайн 18.03.2014;
  27. Shanmugam S. Bioequivalence Study of Aceclofenac Formulations in Animal Model/ Asian Journal of Chemistry. Vol. 22, No. 10 (2010), 8249-8251;
  28. Rajesh Sehgal, Pallavi Bhatia, Pramjit Arora. Sub-chronic toxicological evaluation of aceclofenac in rats. www.pharmasm.com Vol-2, Issue-3, July-2011/ 62-72;
  29. Tamta, A., Payasi, A., Chaudhari, M., Ahmed, A. and Dwivedi V. (2009) Sub acute toxicity of aceclofenac drug in albino rat. Iranian Journal of Toxicology. 2 (3): 240-245.;
  30. Patel N. J., Joshi B. P., Prajapati K. S., Patil V. M. Pathomorphological changes of aceclofenac toxicity in layer chicks. Veterinary World, EISSN: 2231-0916. Available at www.veterinaryworld.org/Vol.7/Feb-2014/10.pdf.
  31. Oaks, J. L., Gilbert, M., Virani, M. Z., Watson, R. T., Meteyer, C. U., Rideout, B., Shivaprasad, H. L., Ahmed, S., Chaudhry, M. J., Arshad, M., Mahmood, S., Ali, A. and Khan, A. A. (2004) Diclofenac residues as the cause of vulture population decline in Pakistan. Nature. 427: 630-633.;
  32. Gajera, A. B. (2006) M.V. Sc. thesis. Pathological studies on experimental feeding of diclofenac sodium in broilers, Anand Agricultural University, Anand.;
  33. Irtaza, H., Khan, M. Z., Khan, A., Ijaz, J. and Kashif, M. S. (2008) Toxicological effects of diclofenac in four avian species. Avian Pathol. 37(3): 315-321.;
  34. Senthilkumar, K. and Thirumurugan, R. (2005) Visceral gout in a Bengal vulture. Indian Vet. J. 82(7):795-796.;
  35. Sharma, R. and Vegad, J. L. (2010) Avian gout: causes, treatment and prevention. Poultry line. 10 (8):19-21.;
  36. Jana, S., Mukhopadhayay, S. K., Niyogi, D., Damodar Singh, Y. and Thiyagaseelan, C. (2009) Epidemio-pathological studies of gout in broiler birds in West Bengal. Indian J. Vet. Pathol. 33(2): 222-224.;
  37. Senthilkumar, K. and Thirumurugan, R. (2005) Visceral gout in a Bengal vulture. Indian Vet. J. 82(7):795-796.;
  38. Mir, M. S., Darzi, M. M., Khan, A. A., Ganaie, N. A., Gupta, S., Nashiruddullah, N. and Kamil, S. A. (2005) Investigation of an outbreak of gout in Kashmir Favorella poultry. Indian. J. Vet. Pathol. 29(1): 35-37.;
  39. Patel, A. K. (2005) M.V.Sc. thesis. Epidemiological and experimental studies on etiology of visceral gout in broiler chicks, Anand Agricultural University, Anand.;
  40. Shultz, S., Baral, H. S., Charman, S., Cunningham, A. A., Das, D., Ghalsasi, G. R., Goudar, M. S., Green, R. E., Jones, A., Nighot, P., Pain, D. J. and Vibhu Prakash (2004) Diclofenac poisoning is widespread in declining vulture populations across the Indian subcontinent. Crossmark. 271(6): 458-460.;
  41. Achutha Nayak Usha, Srinivas Mutalik, Meka Sreenivasa Reddy, Averineni Kumar Ranjith, Pralhad Kushtagi, Nayanabhirama Udupa. Preparation and, in vitro, preclinical and clinical studies of aceclofenac spherical agglomerates / European Journal of Pharmaceutics and Biopharmaceutics 70 (2008) 674–683.;
  42. Mutalik S., B. Sulochana, M. Chetana, N. Udupa, P. Uma Devi, Preliminary studies on acute and subacute toxicity of an antidiabetic herbal preparation, Dianex, Indian J. Exptl. Biol. 41 (2003) 316–320.;
  43. Tamta, A., Payasi, A., Chaudhari, M., Ahmed, A. and Dwivedi V. (2009) Sub acute toxicity of aceclofenac drug in albino rat. Iranian Journal of Toxicology. 2 (3): 240-245.;
  44. Hooper L, Brown TJ, Elliott RA, et al. The effectiveness of five strategies for the prevention of gastrointestinal toxicity induced by non-steroidal anti-inflammatory drugs: systematic review. The British Medical Journal. 2004;329(7472):948–952
  45. Heyneman CA, Lawless-Liday C, Wall GC. Oral versus topical NSAIDs in rheumatic diseases: a comparison. Drugs. 2000;60(3):555–574
  46. J. J. G. Bujan, G. M. G. Alvarez-Eire, W. Martinez, et al. Photoallergic contact dermatitis from aceclofenac, Contact Dermatitis, vol. 45, no. 3, p. 170, 2001
  47. Public Assessment Report Decentralised Procedure ACECLOFENAC 100 mg film-coated tablets UK/H/3717/001/DC UK Licence No: PL 23088/0008 ASTRON RESEARCH LIMITED 19th August 2011

Statistics

Views

Abstract - 50

PDF (Russian) - 2

Cited-By


Article Metrics

Metrics Loading ...

PlumX

Dimensions

Refbacks

  • There are currently no refbacks.

Copyright (c) 2020 Pharmacy Formulas

Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.

This website uses cookies

You consent to our cookies if you continue to use our website.

About Cookies