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Influence of ibuprofen as a solid-state plasticizer in eudragit® RS 30 D on the physicochemical properties of coated beads

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Abstract

The purpose of this study was to investigate the physicochemical properties of nonpareil beads coated with Eudragit® RS 30 D containing ibuprofen as a multifunctional agent. The influence of the concentration of ibuprofen in the film coating and the effect of the coating level on drug release from coated beads was determined in pH 7.2 phosphate buffer solution. The influence of storage time at 23°C and 60°C on the release of ibuprofen from coated beads was also investigated. The thermal properties of the films were determined using a differential scanning calorimeter. Scanning electron microscopy was employed to image the surface morphology of the coated beads. Infrared spectroscopy was used to study the interaction of Eudragit RS 30 D and ibuprofen. Results from the dissolution studies demonstrated that increasing the amount of ibuprofen in the polymeric film reduced the rate of drug release, mainly because of a more complete coalescence of the polymeric particles of the latex dispersion. The glass transition temperature (Tg) of Eudragit RS 30 D films decreased and the surface of the coated beads became smoother as the concentration of ibuprofen was increased. Hydrogen bonding between the polymer and ibuprofen was demonstrated by Fourier transform infrared spectroscopy. No significant differences were found in drug dissolution between the coated beads stored at 23°C for 12 months and those stored at 60°C for 12 hours. The results of this study demonstrated that the ibuprofen plasticized the Eudragit RS 30 D. Furthermore, the dissolution rate of ibuprofen can be controlled and changes in the drug release rate can be minimized by using the drug-induced plasticization technique with this polymer.

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References

  1. Gutierrez-Rocca JC, McGinity JW. Influence of water soluble and insoluble plasticizers on the physical and mechanical properties of acrylic resin copolymers. Int J Pharm. 1994;103:293–301.

    Article  CAS  Google Scholar 

  2. Wesseling M, Kuppler F, Bodmeier R. Tackiness of acrylic and cellulosic polymer films used in the coating of solid dosage forms. Eur J Pharm Biopharm. 1999;47:73–78. [PUBMED]

    Article  CAS  PubMed  Google Scholar 

  3. Bianchini R, Bruni G, Gazzaniga A, Veccio C. d-Indobufen extended-release pellets prepared by coated with aqueous polymer dispersions. Drug Dev Ind Pharm. 1993;19(16):2021–2041.

    Article  CAS  Google Scholar 

  4. Guo JH. A theoretical and experimental study of additive effects of physical aging and antiplasticization on the water permeability of polymer film coatings. J Pharm Sci. 1994;83(3):447–449. [PUBMED]

    Article  CAS  PubMed  Google Scholar 

  5. Amighi K, Moes A. Influence of plasticizer concentration and storage conditions on the drug release rate from Eudragit® RS 30 D film-coated sustained-release theophylline pellets. Eur J Pharm Biopharm. 1996;42:29–35.

    CAS  Google Scholar 

  6. Chowhan ZT, Amaro AA, Chi LH. Comparative evaluations of aqueous film coated tablet formulations by high humidity aging. Drug Dev Ind Pharm. 1982;8(5):713–737.

    Article  CAS  Google Scholar 

  7. Al-Gohary OM, Al-Gamel SS, Hammad A, Molokhia AM. Effect of storage on tabletted microencapsulated aspirin granules. Int J Pharm. 1989;55:47–52.

    Article  CAS  Google Scholar 

  8. Munday DL, Fassihi AR. Changes in drug release rate: effect of stress storage conditions on film coated mini-tablets. Drug Dev Ind Pharm. 1991;17(15):2135–2143.

    Article  CAS  Google Scholar 

  9. Fukumori Y, Yamaoka Y, Ichikawa H, Takeuchi Y, Fukuda T, Osako Y. Coating of pharmaceutical powders by fluidized bed process. IV. Softening temperature of acrylic copolymers and its relation to film formation in aqueous coating. Chem Pharm Bull. 1988;36(12):4927–32.

    Article  CAS  PubMed  Google Scholar 

  10. Arwidsson H, Hjelstuen O, Ingason D, Graffner C. Properties of ethyl cellulose films for extended release. Part 2. Influence of plasticizer content and coalescence conditions when using aqueous dispersions. Acta Pharm Nordica. 1991;3(2):65–70.

    CAS  Google Scholar 

  11. Bodmeier R, Paeratakul O. Leaching of water-soluble plasticizers from polymeric films prepared from aqueous colloidal polymer dispersions. Drug Dev Ind Pharm. 1992;18(17):1865–1882.

    Article  CAS  Google Scholar 

  12. Wu C, McGinity JW. Non-traditional plasticization of polymeric films. Int J Pharm. 1999;177:15–17.

    Article  CAS  PubMed  Google Scholar 

  13. O'Donnell PB, Wu C, Wang J, Oshlach B, Chasin M, Bodmeier R, McGinity JW. An aqueous based pseudolatex of zein protein for film coating of solid dosage forms. Eur J Pharm Biopharm. 1997;43:83–89.

    Article  Google Scholar 

  14. Wu C, McGinity JW. Influence of relative humidity on the mechanical and drug release properties of acrylic polymer coated beads using methylparaben as a non-traditional plasticizer. Eur J Pharm Biopharm. 2000;50(2):277–284.

    Article  CAS  PubMed  Google Scholar 

  15. Gardon JL. Cohesive-energy density. In: Mark HF, Gaylord NG, Bikales NM, eds. Encyclopedia of Polymer Science and Technology. Volume 3. New York, NY: Interscience; 1965:833–863.

    Google Scholar 

  16. Sears JK, Touchette NW. Plasticizers. In: Krostwitch JI, ed. Concise Encyclopedia of Polymer Science and Engineering. New York, NY: John Wiley & Sons; 1990;734–744.

    Google Scholar 

  17. Heinamaki JT, Lehtola VM, Nikuppaavo P, Yliruusi JK. The mechanical and moisture permeability properties of aqueous-based hydroxypropyl methylcellulose coating systems plasticized with polyethylene glycol. Int J Pharm. 1994;112:191–196.

    Article  Google Scholar 

  18. Siew LF, Basit AW, Netwton JM. The potential of organic-based amylose-ethylcellulose film coatings as oral colon-specific drug delivery systems. AAPS PharmSciTech. 2000;1(3):article 22. Available from: http://www.aapspharmaceutica.com/scientificjournal s/pharmscitech/volume issue3/028/manuscript.htm

  19. Wouessidjewe D, Devissaguet JP, Carstensen JT. Effect of multiple film coverage in sustained release pellets. Drug Dev Ind Pharm. 1991;17(1):7–25.

    Article  CAS  Google Scholar 

  20. Goodhart FW, Harris MR, Murthy KS, Nesbitt RU. An evaluation of aqueous film-forming dispersions for controlled release. Pharm Tech. 1984;8:64–71.

    CAS  Google Scholar 

  21. Wheatley TA, Steuernagel CR. Latex emulsions for controlled drug delivery. In: McGinity JW, ed. Aqueous Polymeric Coatings for Pharmaceutical Dosage Forms. New York, NY: Marcel Dekker; 1996:1–54.

    Google Scholar 

  22. Banker GS, Peck GE. New water-based colloidal dispersions, Pharm Tech. 1981;5:55–60.

    CAS  Google Scholar 

  23. Yoo JN, Sperling LH, Glinka CJ, Klein A. Characterization of film formation from polystyrene latex particles via SANS. 1. Moderate molecular weight. Macromolecules. 1990;23:3926–3967.

    Article  Google Scholar 

  24. Miller RA, Vadas EB. The physical stability of tablets coated using an aqueous dispersion of ethylcellulose. Drug Dev Ind Pharm. 1984;10:1565–1585.

    Article  CAS  Google Scholar 

  25. Harris MR, Ghebre-Sellassie I, Nesbitt RU. A water-based coating process for sustained release. Pharm Tech. 1986;10:102–107.

    CAS  Google Scholar 

  26. Gilligan CA, Li Wan Po A. Factors affecting drug release from a pellet system coated with an aqueous colloidal dispersion. Int J Pharm. 1991;73:51–68.

    Article  CAS  Google Scholar 

  27. Li SO, Jhawar R, Mehta GN, Harwood RJ, Grim WM. Preparation and in vitro evaluation of a controlled-release drug delivery system of theophylline using an aqueous acrylic resin dispersion. Drug Dev Ind Pharm. 1989;15:1231–1242.

    Article  CAS  Google Scholar 

  28. Amighi K, Moës AJ. Influence of curing conditions on the drug release rate from Eudragit® NE30D film coated sustained-release theophylline pellets. STP Pharma Sci. 1997;7(2):141–147.

    CAS  Google Scholar 

  29. Fisher DG, Rowe RC. The adhesion of film coating to tablet surfaces-instrumentation and preliminary evaluation. J Pharm Pharmacol. 1976;28(2):886–889.

    Article  CAS  PubMed  Google Scholar 

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Authors and Affiliations

  1. Division of Pharmaceutics, College of Pharmacy, The University of Texas at Austin, 78712, Austin, TX

    Chuanbin Wu & James W. McGinity

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  1. Chuanbin Wu
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  2. James W. McGinity
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Correspondence to Chuanbin Wu.

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Published: November 26, 2001

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Wu, C., McGinity, J.W. Influence of ibuprofen as a solid-state plasticizer in eudragit® RS 30 D on the physicochemical properties of coated beads. AAPS PharmSciTech 2, 24 (2001). https://doi.org/10.1208/pt020424

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