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RETRACTED ARTICLE: Meloxicam Taste-Masked Oral Disintegrating Tablet with Dissolution Enhanced by Ion Exchange Resins and Cyclodextrin

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This article was retracted on 04 February 2014

Abstract

The purpose of this study was to develop taste-masked oral disintegrating tablets (ODTs) using the combination of ion exchange resin and cyclodextrin, to mask the bitter taste and enhance drug dissolution. Meloxicam (MX) was selected as a model drug with poor water solubility and a bitter taste. Formulations containing various forms of MX (free drug, MX-loaded resin or resinate, complexes of MX and 2-hydroxypropyl-β-cyclodextrin (HPβCD) or MX/HPβCD complexes, and a mixture of resinate and MX/HPβCD complexes) were made and tablets were prepared by direct compression. The ODTs were evaluated for weight variation, thickness, diameter, hardness, friability, disintegration time, wetting time, MX content, MX release, degree of bitter taste, and stability. The results showed that thickness, diameter, weight, and friability did not differ significantly for all of these formulations. The tablet hardness was approximately 3 kg/in.2, and the friability was less than 1%. Tablets formulated with resinate and the mixture of resinate and MX/HPβCD complexes disintegrated rapidly within 60 s, which is the acceptable limit for ODTs. These results corresponded to the in vivo disintegration and wetting times. However, only tablets containing the mixture of resinate and MX/HPβCD complexes provided complete MX dissolution and successfully masked the bitter taste of MX. In addition, this tablet was stable at least 6 months. The results from this study suggest that the appropriate combination of ion exchange resin and cyclodextrin could be used in ODTs to mask the bitter taste of drug and enhance the dissolution of drugs that are weakly soluble in water.

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REFERENCES

  1. Sastry SV, Nyshadham JR, Fıx JA. Recent technological advances in oral drug delivery—a review. Pharm Sci Technol Today. 2000;3(4):138–45.

    Article  CAS  PubMed  Google Scholar 

  2. Hirani JJ, Rathod DA, Vadalia KR. Orally disintegrating tablets: a review. Trop J Pharm Res. 2009;8:161–72.

    Article  CAS  Google Scholar 

  3. Mohapatra A, Parikh RK, Gohel MC. Formulation, development and evaluation of patient friendly dosage forms of metformin, part—I: orally disintegrating tablets. Asian J Pharm. 2008;2:167–71.

    Article  Google Scholar 

  4. Bhise K, Shaikh S, Bora D. Taste Mask, design and evaluation of an oral formulation using ion exchange resin as drug carrier. AAPS PharmSciTech. 2008;9(2):557–62.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  5. Anand V, Kandarapu R, Garg S. Ion-exchange resins: carrying drug delivery forward. Drug Discov Today. 2001;6:905–14.

    Article  CAS  PubMed  Google Scholar 

  6. Burke GM, Mendes RW, Jambhekar SS. Investigation of the application of ion exchange resins as a sustained release drug delivery system for propranolol hydrochloride. Drug Dev Ind Pharm. 1986;12:713–32.

    Article  CAS  Google Scholar 

  7. Leea CW, Kima SJ, Youna YS, Widjojokusumoa E, Leea YH, Kimb J, et al. Preparation of bitter taste masked cetirizine dihydrochloride/β-cyclodextrin inclusion complex by supercritical antisolvent (SAS) process. J Supercrit Fluid. 2010;5(1):348–57.

    Article  Google Scholar 

  8. Brewster ME, Loftsson T. Cyclodextrins as pharmaceutical solubilizers. Advanced Drug Delivery Reviews. 2007;59:645–66.

    Article  CAS  PubMed  Google Scholar 

  9. Loftsson T, Brewster ME. Pharmaceutical applications of cyclodextrins. 1. Drug solubilization and stabilization. J Pharm Sci. 1996;85:1017–25.

    Article  CAS  PubMed  Google Scholar 

  10. The United State Pharmacopoeia XXXII/National FormulationXXVII. The United States Pharmacopoeial Convention. Rockville, MD; 2009.

  11. Kunin R. Ion exchange resins. New York: Wiley; 1963.

    Google Scholar 

  12. Sriwongjanya M, Bodmeier R. Entrapment of drug-loaded ion-exchange particles within polymeric microparticles. Int J Pharm. 1997;158:29–38.

    Article  CAS  Google Scholar 

  13. Samprasit W, Rojanarata T, Akkaramongkolporn P, Ngawhirunpat T, Sila-On W, Opanasopit P. Improvement of drug loading onto ion exchange resin by cyclodextrin inclusion complex. Drug Dev Ind Pharm. 2013. doi:10.3109/03639045.2012.729593.

  14. Job P. Job’s plot analyses for the 2-CG and 3-CG complexes were consistent with 1:1 stoichiometry. Ann Chim. 1928;9:113–34.

    CAS  Google Scholar 

  15. Guo X, Chang RK, Hussain MA. Ion-exchange resins as drug delivery carriers. J Pharm Sci. 2009;98(11):3886–902.

    Article  CAS  PubMed  Google Scholar 

  16. Gohel M, Patel M, Amin A, Agrawal R, Dave R, Bariya N. Formulation design and optimization of mouth dissolve tablets of nimesulide using vacuum drying technique. AAPS PharmSciTech. 2004;36:1–6.

    Google Scholar 

  17. Bi Y, Sunada H, Yonezawa Y, Danjo K, Otsuka A, Iida K. Preparation and evaluation of a compressed tablet rapidly disintegrating in the oral cavity. Chem Pharm Bull. 1996;44:2121–7.

    Article  CAS  PubMed  Google Scholar 

  18. Luger P, Daneck K, Trummlitz WEG, Wagner K. Structure and physicochemical properties of meloxicam, a new NSAID. Eur J Pharm Sci. 1996;4:175–87.

    Article  CAS  Google Scholar 

  19. Pisal S, Zainnuddin R, Nalawade P, Mahadik K, Kadam S. Molecular properties of ciprofloxacin-Indion 234 complexes. AAPS PharmSciTech. 2004;5(4):1–8.

    Article  Google Scholar 

  20. Sriwongjanya M, Bodmeier R. Entrapment of drug-loaded ion-exchange particles within polymeric microparticles. Int J Pharm. 1997;158:29–38.

    Article  CAS  Google Scholar 

  21. Dowex product literature. http://www.dow.com. Accessed 26 Nov 2012.

  22. Jeong SH, Park K. Drug loading and release properties of ion-exchange resin complexes as a drug delivery matrix. Int J Pharm. 2008;361:26–32.

    Article  CAS  PubMed  Google Scholar 

  23. Higuchi T, Kristiansen H. Binding specificities between small organic solutes in aqueous solutions: classification of some solutes onto two groups according to binding tendencies. J Pharm Sci. 1970;59:1601–8.

    Article  CAS  PubMed  Google Scholar 

  24. Obaidat AA, Khanfar RA, Khawam MN. The effect of β-cyclodextrin on the solubility and dissolution rate of meloxicam and investigation of the driving force for complexation using molecular modeling. J Incl Phenom Macrocycl Chem. 2009;63:273–9.

    Article  CAS  Google Scholar 

  25. Sinko PJ. Martin’s physical pharmacy and pharmaceutical sciences. London: Lippincott Williams & Wilkins; 2011. p. 197–222.

    Google Scholar 

  26. Jug M, Bećirević-Laćan M. Influence of hydroxypropyl-β-cyclodextrin complexation on piroxicam release from buccoadhesive tablets. Eur J Pharm Sci. 2004;21:251–60.

    Article  CAS  PubMed  Google Scholar 

  27. Sheshala R, Khan N, Chitneni M, Darwis Y. Formulation and in vivo evaluation of ondansetron orally disintegrating tablets using different superdisintegrants. Arch Pharm Res. 2011;34(11):1945–56.

    Article  CAS  PubMed  Google Scholar 

  28. Fenyresi E, Shirankura O, Szejtli J, Nagai T. Properties of cyclodextrin polymer as a tableting aid. Chem Pharm Bull. 1984;32:665–9.

    Article  Google Scholar 

  29. Ghorab MM, Abdel-Salam HM, El-Sayad MA, Mekhel MM. Tablet formulation containing meloxicam and β-cyclodextrin: mechanical characterization and bioavailability evaluation. AAPS PharmSciTech. 2004;5(4):1–6.

    Article  Google Scholar 

  30. Rudnic EM, Rhodes CT, Welsh S, Bernardo P. Evaluation of the mechanism of disintegrant action. Drug Dev Ind Pharm. 1982;8:87–109.

    Article  CAS  Google Scholar 

  31. Amberlite product literature. http://www.rohmhaas.com. Accessed 26 Nov 2012.

  32. Akkaramongkolporn P, Ngawhirunpat T, Nunthanid J, Opanasopit P. Effect of a pharmaceutical cationic exchange resin on the properties of controlled release diphenhydramine hydrochloride matrices using Methocel K4M or Ethocel 7cP as matrix formers. AAPS PharmSciTech. 2008;9(3):899–908.

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  33. Sriwongjanya M, Bodmeier R. Effect of ion exchange resins on the drug release from matrix tablets. Eur J Pharm Biopharm. 1998;46:321–7.

    Article  CAS  PubMed  Google Scholar 

  34. Pattarakan N, Opanasopit P, Ngawhirunpat T, Akkaramongkolporn P. Application of ion exchange resins as tablet disintegrants. The 26th Annual Research Conference in Pharmaceutical Science. 04 December 2009. Bangkok, Thailand.

  35. Kornblum SS, Stoopak SB. A new tablet disintegrating agent: cross-linked polyvinylpyrrolidone. J Pharm Sci. 1973;62(1):43–9.

    Article  CAS  PubMed  Google Scholar 

  36. Jivraj M, Martini LG, Thomson CM. An overview of the different excipients useful for the direct compression of tablets. Pharm Sci Tech Today. 2000;3:58–62.

    Article  CAS  Google Scholar 

  37. Narazaki R, Harada T, Takami N, Kato Y, Ohwaki T. A new method for disintegration studies of rapid disintegrating tablet. Chem Pharm Bull. 2004;52(6):704–7.

    Article  CAS  PubMed  Google Scholar 

  38. Bi Y, Hisakadzu S. Preparation and evaluation of a compressed tablet rapidly disintegrating in the oral cavity. Chem Pharm Bull. 1996;44:2121–7.

    Article  CAS  PubMed  Google Scholar 

  39. Fenyresi E, Shirankura O, Szejtli J, Nagai T. Properties of cyclodextrin polymer as a tableting aid. Chem Pharm Bull. 1984;32:665–9.

    Article  Google Scholar 

  40. Jinichi F, Etsuo Y, Yasuo Y, Terada K. Evaluation of rapidly disintegrating tablets containing glycine and carboxymethylcellulose. Int J Pharm. 2006;310:101–9.

    Article  Google Scholar 

  41. Akkaramongkolporn P, Yononemochi E, Terada K. Molecular state of chlorpheniramine in resinates. Chem Pharm Bull. 2000;48(2):231–4.

    Article  CAS  PubMed  Google Scholar 

  42. Dahiya S, Pathak K. Influence of amorphous cyclodextrin derivatives on aceclofenae release from directly compressible tablets. Pharmazie. 2007;62:278–83.

    CAS  PubMed  Google Scholar 

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ACKNOWLEDGMENTS

The authors wish to thank the Commission of Higher Education (Thailand), the Thailand Research Funds through the Golden Jubilee PhD Program (Grant No. PHD/0001/2553) and the Silpakorn University Research and Development Institute for financial support (Grant No. SURDI 55/02/2555).

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Correspondence to Praneet Opanasopit.

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This article was retracted at the request of the authors because of an error in data compilation.

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Samprasit, W., Akkaramongkolporn, P., Ngawhirunpat, T. et al. RETRACTED ARTICLE: Meloxicam Taste-Masked Oral Disintegrating Tablet with Dissolution Enhanced by Ion Exchange Resins and Cyclodextrin. AAPS PharmSciTech 14, 1118–1128 (2013). https://doi.org/10.1208/s12249-013-0001-y

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  • DOI: https://doi.org/10.1208/s12249-013-0001-y

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