Skip to main content
Log in

Efficacy of gastro-retentive forms of ecabet sodium in the treatment of gastric ulcer in rats

  • Research Article
  • Published:
Archives of Pharmacal Research Aims and scope Submit manuscript

Abstract

The purpose of the present study is to investigate the influence of gastric retention of ecabet sodium (ECS) on its mucoprotective effect in rat ulcer models. Mini-tablets containing 9 mg ECS were prepared using the direct compression method. The release rates of ECS mini-tablets were controlled by the amount and viscosity grade of hydroxypropylmethyl cellulose incorporated. Gastric retention of ECS mini-tablets after oral administration to rats was visually confirmed using a fluorescence imaging system. Because ECS mini-tablets exhibited size-dependent gastric retention, their gastric retention time was prolonged as the release rate decreased. In the in vivo efficacy study, gastro-retentive dosage forms of ECS did not influence the mucoprotective effect in the immediate irritation model but enhanced the effect in the delayed irritation model compared with ECS suspension. This finding indicates that the duration of the mucoprotective effect of ECS can be extended by the employment of gastro-retentive dosage formulations and provides a rationale for development of ECS gastro-retentive dosage forms.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7
Fig. 8
Fig. 9

Similar content being viewed by others

References

  • Adachi, K., S. Ishihara, T. Hashimoto, K. Hirakawa, N. Ishimura, M. Niigaki, T. Kaji, A. Kawamura, H. Sato, and H. Fujishiro. 2001. Efficacy of ecabet sodium for Helicobacter pylori eradication triple therapy in comparison with a lansoprazole-based regimen. Alimentary Pharmacology and Therapeutics 15: 1187–1191.

    Article  CAS  PubMed  Google Scholar 

  • Baumgartner, S., J. Kristl, and N.A. Peppas. 2002. Network structure of cellulose ethers used in pharmaceutical applications during swelling and at equilibrium. Pharmaceutical Research 19: 1084–1090.

    Article  CAS  PubMed  Google Scholar 

  • Berenguer, B., L. Sánchez, A. Quilez, M. López-Barreiro, O. De Haro, J. Galvez, and M. Martin. 2006. Protective and antioxidant effects of Rhizophora mangle L. against nsaid-induced gastric ulcers. Journal of Ethnopharmacology 103: 194–200.

    Article  CAS  PubMed  Google Scholar 

  • Brzozowski, T., P. Konturek, S. Konturek, S. Kwiecień, D. Drozdowicz, W. Bielanski, R. Pajdo, A. Ptak, A. Nikiforuk, and W. Pawlik. 2004. Exogenous and endogenous ghrelin in gastroprotection against stress-induced gastric damage. Regulatory Peptides 120: 39–51.

    Article  CAS  PubMed  Google Scholar 

  • Cao, Q.R., Y.W. Choi, J.H. Cui, and B.J. Lee. 2005. Formulation, release characteristics and bioavailability of novel monolithic hydroxypropylmethylcellulose matrix tablets containing acetaminophen. Journal of Controlled Release 108: 351–361.

    Article  CAS  PubMed  Google Scholar 

  • Conti, S., L. Maggi, L. Segale, E. Ochoa Machiste, U. Conte, P. Grenier, and G. Vergnault. 2007. Matrices containing nacmc and hpmc: 2. Swelling and release mechanism study. International Journal of Pharmaceutics 333: 143–151.

    Article  CAS  PubMed  Google Scholar 

  • De Barros, M.P., J.P.B. Sousa, J.K. Bastos, and S.F. De Andrade. 2007. Effect of brazilian green propolis on experimental gastric ulcers in rats. Journal of Ethnopharmacology 110: 567–571.

    Article  PubMed  Google Scholar 

  • Evangelista, S., C.A. Maggi, and A. Meli. 1987. Influence of peripherally-administered peptides on ethanol-induced gastric ulcers in the rat. General Pharmacology 18: 647–649.

    Article  CAS  PubMed  Google Scholar 

  • Ito, Y., T. Fukushima, Y. Sugawara, O. Takaiti, and S. Nakamura. 1991. Metabolic fate of a new anti-ulcer drug (+)-(1R, 4aS, 10aR)-1,2,3,4,4a,9,10,10a-octahydro-1,4a-dimethyl-7-(1-methylethyl)-6-sulfo-1-phenanthrenecarboxylic acid 6-sodium salt pentahydrate (TA-2711). I. Disposition, metabolism and protein binding in rats and dogs. Journal of Pharmacobio-Dynamics 14: 533–546.

    Article  CAS  PubMed  Google Scholar 

  • Ito, Y., Y. Onoda, S. Nakamura, K. Tagawa, T. Fukushima, Y. Sugawara, and O. Takaiti. 1993. Effects of the new anti-ulcer drug ecabet sodium (TA-2711) on pepsin activity. II: Interaction with substrate protein. Japanese Journal of Pharmacology 62: 175–181.

    Article  CAS  PubMed  Google Scholar 

  • Ito, Y., K. Shibata, A. Hongo, and M. Kinoshita. 1998. Ecabet sodium, a locally acting antiulcer drug, inhibits urease activity of Helicobacter pylori. Euro J Pharmacol 345: 193–198.

    Article  CAS  Google Scholar 

  • Kim, H.W., G.H. Kim, J.Y. Cheong, U.S. Yang, S.K. Park, C.S. Song, D.H. Kang, and G.A. Song. 2008. H. pylori eradication: A randomized prospective study of triple therapy with or without ecabet sodium. World Journal of Gastroenterology 14: 908–912.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • Kinoshita, M., M. Endo, A. Yasoshima, N. Saito, K. Yamasaki, S. Chishima, and H. Narita. 1999. Ecabet sodium, a novel locally-acting anti-ulcer agent, protects the integrity of the gastric mucosal gel layer from pepsin-induced disruption in the rat. Alimentary Pharmacology and Therapeutics 13: 687–694.

    Article  CAS  PubMed  Google Scholar 

  • Kinoshita, M., H. Iwasaki, A. Yasoshima, and H. Tamaki. 1993. Effects of ecabet sodium (TA-2711), a new antiulcer agent, on gastrointestinal mucosal prostanoid production and morphology in rats. Biological and Pharmaceutical Bulletin 16: 1220–1225.

    Article  CAS  PubMed  Google Scholar 

  • Kinoshita, M., E. Kume, and H. Tamaki. 1995a. Roles of prostaglandins, nitric oxide and the capsaicin-sensitive sensory nerves in gastroprotection produced by ecabet sodium. Journal of Pharmacology and Experimental Therapeutics 275: 494–501.

    CAS  PubMed  Google Scholar 

  • Kinoshita, M., K. Yamasaki, Y. Kokusenya, and H. Tamaki. 1995b. Relationship between gastroprotective effect of locally acting antiulcer agent ecabet sodium and its binding to gastric mucosa in rats. Digestive Diseases and Sciences 40: 661–667.

    Article  CAS  PubMed  Google Scholar 

  • Oh, T.Y., G.J. Ahn, S.M. Choi, B.O. Ahn, and W.B. Kim. 2005. Increased susceptibility of ethanol-treated gastric mucosa to naproxen and its inhibition by DA-9601, an artemisia asiatica extract. World Journal of Gastroenterology 11: 7450–7456.

    CAS  PubMed  Google Scholar 

  • Onoda, Y., T. Magaribuchi, and H. Tamaki. 1990. Effects of the new anti-ulcer agent 12-sulfodehydroabietic acid monosodium salt on duodenal alkaline secretion in rats. Arznei-Forschung 40: 576–578.

    CAS  Google Scholar 

  • Pan, L., Q. Tang, Q. Fu, B. Hu, J. Xiang, and J. Qian. 2005. Roles of nitric oxide in protective effect of berberine in ethanol-induced gastric ulcer mice. Acta Pharma Sinica 26: 1334–1338.

    Article  CAS  Google Scholar 

  • Pearson, J., and N. Roberts. 2001. Mucosal protective effects of ecabet sodium: Pepsin inhibition and interaction with mucus. Clinical Science 100: 411–417.

    Article  CAS  PubMed  Google Scholar 

  • Saphier, S., A. Rosner, R. Brandeis, and Y. Karton. 2010. Gastro intestinal tracking and gastric emptying of solid dosage forms in rats using X-ray imagining. International Journal of Pharmaceutics 388: 190–195.

    Article  CAS  PubMed  Google Scholar 

  • Sibilia, V., G. Rindi, F. Pagani, D. Rapetti, V. Locatelli, A. Torsello, N. Campanini, R. Deghenghi, and C. Netti. 2003. Ghrelin protects against ethanol-induced gastric ulcers in rats: Studies on the mechanisms of action. Endocrinology 144: 353–359.

    Article  CAS  PubMed  Google Scholar 

  • Siepmann, J., and N. Peppas. 2001. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Advanced Drug Delivery Reviews 48: 139–157.

    Article  CAS  PubMed  Google Scholar 

Download references

Acknowledgments

This study was supported by a grant of the Korean Health Technology R&D Project, Ministry for Health, Welfare & Family Affairs, Republic of Korea (A092018).

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Eun-Seok Park.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Kim, JY., Bae, HJ., Choi, J. et al. Efficacy of gastro-retentive forms of ecabet sodium in the treatment of gastric ulcer in rats. Arch. Pharm. Res. 37, 1053–1062 (2014). https://doi.org/10.1007/s12272-013-0278-0

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s12272-013-0278-0

Keywords

Navigation