Skip to main content
SpringerLink
Log in

Effect of Plasticizer on Release Kinetics of Diclofenac Sodium Pellets Coated with Eudragit RS 30 D

  • Research Article
  • Published:
AAPS PharmSciTech Aims and scope Submit manuscript

Abstract

The present study was designed to investigate the effect of two plasticizers, i.e., triethyl citrate (TEC) and polyethylene glycol 6000 (PEG 6000) on the in vitro release kinetics of diclofenac sodium from sustained-release pellets. Ammonio methacrylate copolymer type B (Eudragit RS 30 D) is used as the release-retarding polymer. Both plasticizers were used at 10% and 15% (w/w) of Eudragit RS 30 D. Pellets were prepared by powder layering technology and coated with Eudragit RS 30 D by air suspension technique. Thermal properties of drug and drug-loaded beads were studied using differential scanning calorimeter (DSC). DSC thermogram represented the identity of raw materials and exhibited no interaction or complexation between the active and excipients used in the pelletization process. Dissolution study was performed by using USP apparatus 1. No significant difference was observed among the physical properties of the coated pellets of different batches. When dissolution was performed as pure drug, about 8.22% and 90% drug was dissolved at 2 h in 0.1 N HCl and at 30 min in buffer (pH 6.8), respectively. From all formulations, the release of drug in acid media was very negligible (maximum 1.8 ± 0.08% at 2 h) but in buffer only 12% and 30% drug was released at 10 h from coated pellets containing TEC and PEG 6000, respectively, indicating that Eudragit RS 30 D significantly retards the drug release rate and that drug release was varied according to the type and amount of plasticizers used. The amount of TEC in coating formulation significantly effected drug release (p < 0.001), but the effect of PEG 6000 was not significant. Formulations containing PEG 6000 released more drug (98.35 ± 2.35%) than TEC (68.01 ± 1.04%) after 24 h. Different kinetic models like zero order, first order, and Higuchi were used for fitting drug release pattern. Zero order model fitted best for diclofenac release in all formulations. Drug release mechanism was derived with Korsmeyer equation.

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

Access this article

Log in via an institution

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

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6

Similar content being viewed by others

References

  1. B. C. Andrew, and L. Shargel. Applied Biopharmaceutics and Pharmacokinetics, Appleton & Lange, Connecticut, 1941, pp. 225–264.

    Google Scholar 

  2. D. Bidah, and J. M. Vergnaud. Dosage forms with a polymer matrix and a swelling polymer. Int. J. Pharm. 77:81–87 (1991).

    Article  CAS  Google Scholar 

  3. S. A. Bravo, M. C. Lamas, and C. J. Salamon. In-vitro studies of diclofenac sodium controlled-release from biopolymeric hydrophilic matrices. J. Pharm. Pharm. Sci. 53:213–219 (2002).

    PubMed  CAS  Google Scholar 

  4. J. L. Ford, A. R. Rajabi-Siahboomi, M. H. Rubinstein, and F. Sadeghi. Comparative study of drug release from pellets coated with HPMC or Surelease. Drug Dev. Ind. Pharm. 266:651–660 (2000).

    Article  PubMed  Google Scholar 

  5. G. Jayasagar, Y. M. Rao, and J. K. Veni. Formulation and evaluation of diclofenac sodium using hydrophilic matrices. Drug Dev. Ind. Pharm. 278:759–766 (2001).

    Article  PubMed  Google Scholar 

  6. W. Chuanbin, and W. M. James. Influence of ibuprofen as a solid-state plasticizer in Eudragit® RS 30 D on the physicochemical properties of coated beads. AAPS PharmSciTech. 2(4) article 24 (2001).

    Google Scholar 

  7. L. L. Augsburger, A. Lin, N. A. Muhammad, and D. Pope. Effect of curing and storage conditions on drug release from pellets coated with Eudragit NE30D. AAPS Annual Meeting Supplement 2(4) (2000).

  8. D. Dreher, and K. Lehmann. The use of aqueous synthetic polymer dispersions for coating pharmaceutical dosage forms. Drugs Made Ger. 16:126–136 (1973).

    Google Scholar 

  9. C. E. Obi, and R. S. Okor. Drug release through aqueous-based film coatings of acrylate-methacrylate, a water-insoluble copolymer. Int. J. Pharm. 58:89–91 (1990).

    Article  Google Scholar 

  10. G. Cole (eds.), Pharmaceutical Coating Technology, Taylor & Francis Ltd., London, 2001, pp. 27–31.

  11. J. W. McGinity (eds.), Aqueous Polymeric Coating for Pharmaceutical Dosage Forms, Marcel Decker Inc., New York, 1996, pp. 101–174.

  12. K. Lehmann. Practical Course in Film Coating of Pharmaceutical Dosage Forms with Eudragit, Pharma Polymers, Darmstadt, 2001, pp. 8–15.

    Google Scholar 

  13. Pharmaceutical Coatings Bulletin. Influence of Citrate Ester Plasticizers on the Properties of Acrylic Resin Polymers, Morflex, Inc., 1993, p. 102.

  14. Pharmaceutical Coatings Bulletin. Physical and Mechanical Properties of Acrylic and Cellulosic Polymers Plasticized with Citrate Esters. Morflex, Inc., 1994, p. 102.

  15. USP 23/NF 18. Triethyl Citrate-Official Monograph, 1995, p. 2316.

  16. C. Tapia, Z. Escobar, E. Costa et al. Comparative studies on polyelectrolyte complexes and mixture of chitosan-alginate and chitosan-carrageenan as prolonged diltiazem clorhydrate release system. Eur. J. Pharm. Biopharm. 57:65–75 (2004).

    Article  PubMed  CAS  Google Scholar 

  17. A. G. Gilman, T. W. Rail, A. S. Nies, and P. Taylor. The Pharmacological Basis of Therapeutics, Pergamon Press, New York, 1990.

    Google Scholar 

  18. D. M. Morkhade, S. V. Fulzele, P. M. Satturwar, and S. B. Joshi. Gum copal and gum damar: novel matrix forming materials for sustained drug delivery. Ind. J. Pharm. Sci. 68:53–58 (2006).

    Article  CAS  Google Scholar 

  19. T. Higuchi. Mechanism of sustained action medication. Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J. Pharm. Sci. 52:1145–1149 (1963).

    Article  PubMed  CAS  Google Scholar 

  20. R. W. Korsmeyer, R. Gurny, E. Doelker, P. Buri, and N. A. Peppas. Mechanisms of solute release from porous hydrophilic polymers. Int. J. Pharm. 15:25–35 (1983).

    Article  CAS  Google Scholar 

  21. Y. Zhu, K. A. Mehta, and J. W. McGinity. Influence of plasticizer level on the drug release from sustained release film coated and hot-melt extruded dosage forms. Pharm. Dev. Tech. 11:285–294 (2006).

    Article  CAS  Google Scholar 

  22. G. Kibria, and R. Jalil. The effect of the ratio of two acrylic polymers on the in-vitro release kinetics of ketoprofen from pellets prepared by extrusion and spheronisation technique. Pak. J. Pharm. Sci. 212:92–97 (2008).

    PubMed  CAS  Google Scholar 

  23. M. F. Saettone, G. Perini, P. Rijli, L. Rodriguez, and M. Cini. Effect of different polymer-plasticizer combinations on in vitro release of theophylline from coated pellets. Int. J. Pharm. 126:83–88 (1995).

    Article  CAS  Google Scholar 

Download references

Acknowledgements

The authors would like to thank Eskayef Bangladesh Ltd. (formerly, SmithKline & French, UK) for providing the raw materials as well as manufacturing facilities, Bangladesh Council of Scientific and Industrial Research (BCSIR), and Renata Ltd. Bangladesh (formerly, Pfizer, USA) for providing the scanning electron micrograph and the DSC thermogram, respectively.

Author information

Authors and Affiliations

  1. Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Dhaka, Dhaka, 1000, Bangladesh

    Golam Kibria, Monzurul Amin Roni, Mohammad Shahriarul Absar & Reza-ul Jalil

Authors
  1. Golam Kibria
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Monzurul Amin Roni
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Mohammad Shahriarul Absar
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Reza-ul Jalil
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Golam Kibria.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Kibria, G., Roni, M.A., Absar, M.S. et al. Effect of Plasticizer on Release Kinetics of Diclofenac Sodium Pellets Coated with Eudragit RS 30 D. AAPS PharmSciTech 9, 1240–1246 (2008). https://doi.org/10.1208/s12249-008-9163-4

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-008-9163-4

Key words

Search

Navigation