Skip to main content
SpringerLink
Log in

Development and Evaluation of a Novel Modified-Release Pellet-Based Tablet System for the Delivery of Loratadine and Pseudoephedrine Hydrochloride as Model Drugs

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

Abstract

Modified-release multiple-unit tablets of loratadine and pseudoephedrine hydrochloride with different release profiles were prepared from the immediate-release pellets comprising the above two drugs and prolonged-release pellets containing only pseudoephedrine hydrochloride. The immediate-release pellets containing pseudoephedrine hydrochloride alone or in combination with loratadine were prepared using extrusion–spheronization method. The pellets of pseudoephedrine hydrochloride were coated to prolong the drug release up to 12 h. Both immediate- and prolonged-release pellets were filled into hard gelatin capsule and also compressed into tablets using inert tabletting granules of microcrystalline cellulose Ceolus KG-801. The in vitro drug dissolution study conducted using high-performance liquid chromatography method showed that both multiple-unit capsules and multiple-unit tablets released loratadine completely within a time period of 2 h, whereas the immediate-release portion of pseudoephedrine hydrochloride was liberated completely within the first 10 min of dissolution study. On the other hand, the release of pseudoephedrine hydrochloride from the prolonged release coated pellets was prolonged up to 12 hr and followed zero-order release kinetic. The drug dissolution profiles of multiple-unit tablets and multiple-unit capsules were found to be closely similar, indicating that the integrity of pellets remained unaffected during the compression process. Moreover, the friability, hardness, and disintegration time of multiple-unit tablets were found to be within BP specifications. In conclusion, modified-release pellet-based tablet system for the delivery of loratadine and pseudoephedrine hydrochloride was successfully developed and evaluated.

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

Similar content being viewed by others

References

  1. Bodmeier R. Tableting of coated pellets. Eur J Pharm Biopharm. 1997;43:1–8.

    Article  CAS  Google Scholar 

  2. Bechgaard H, Neilson GH. Controlled release multiple units and single-unit doses. Drug Dev Ind Pharm. 1978;4:53–67.

    Article  CAS  Google Scholar 

  3. Bechgaard H. Critical factors influencing gastrointestinal absorption—what is the role of pellets? Acta Pharm Technol. 1982;28(2):149–57.

    CAS  Google Scholar 

  4. Wilson CG, Washington C, Washington N. Overview of epithelial barriers and drug transport. In: Wilson CG, Washington N, editors. Physiological pharmaceutics: biological barriers to drug absorption. Chichester: Ellis Horwood Limited; 1989. p. 60–70.

    Google Scholar 

  5. Beckett AH. Proceedings of an International Symposium on Recent Advances in the Design, Development and Assessment of Sustained Release Drug Delivery Systems.1985; Liverpool.

  6. Wieslaw S, Rafal L. Compressibility of floating pellets with verapamil hydrochloride coated with dispersion Koollicoat SR 30 D. Eur J Pharm Biopharm. 2005;60:153–58.

    Article  Google Scholar 

  7. Tunon A, Borjesson E, Frenning G, Alderborn G. Drug release from reservoir pellets compacted with some excipients of different physical properties. Eur J Pharm Biopharm. 2003;20:469–79.

    CAS  Google Scholar 

  8. Dashevsky A, Kolter K, Bodmeier R. Compression of pellets coated with various aqueous polymer dispersions. Eur J Pharm Sci. 2004;279:19–26.

    CAS  Google Scholar 

  9. Zeeshan F, Peh KK, Tan YTF. Exploring the potential of a highly compressible microcrystalline cellulose as novel tabletting excipient in the compaction of extended-release coated pellets containing an extremely water-soluble model drug. AAPS PharmSciTech. 2009;10(3):850–57.

    Article  CAS  PubMed  Google Scholar 

  10. Connell JT. A novel method to assess antihistamine and decongestant efficacy. Ann Allergy. 1979;42:278–85.

    CAS  PubMed  Google Scholar 

  11. Falliers CJ, Redding MA. Controlled comparison of a new antihistamine–decongestant combination to its individual components. Ann Allergy. 1980;45:75–80.

    CAS  PubMed  Google Scholar 

  12. Connell JT, Williams BO, Allen S, Cato A, Perkins JG. A double- blind controlled evaluation of Actifed and its individual constituents in allergic rhinitis. J Int Med Res. 1982;10:341–47.

    CAS  PubMed  Google Scholar 

  13. Sznitowska M, Cal K, Kupiec K. Development of modified-release dosage forms containing loratadine and pseudoephedrine sulphate. Acta Pol Pharm. 2004;61:72–4.

    CAS  PubMed  Google Scholar 

  14. Schaefer T, Worts O. Control of fluidized bed granulation: effects of spray angle, nozzle height and starting materials on granule size and size distribution. Arch Pharm Chem Sci. 1977;5:51–60.

    CAS  Google Scholar 

  15. Tan YTF, Heng PWS, Wan LSC. Mixed polymer coating for modified release from coated spheroids. Pharm Dev Technol. 1999;5(4):561–70.

    Article  Google Scholar 

  16. British Pharmacopoeia. Vol IV. London, UK: British Pharmacopoeia Commission Office; 2008: Appendix XII C A303-5.

  17. British Pharmacopoeia. Vol IV. London, UK: British Pharmacopoeia Commission Office; 2008: Appendix XVII H A423-4.

  18. British Pharmacopoeia. Vol IV. London, UK: British Pharmacopoeia Commission Office; 2008: Appendix XII A A283-4.

  19. Laakso L, Kristoffersson E, Marvola M. Bi-exponential first-order release kinetics of indomethacin from tablets containing polysorbate 80. Eur J Pharm Sci. 1984;19:35–42.

    CAS  Google Scholar 

  20. Lippold BC, Monells Pagés R. Control and stability of drug release from diffusion pellets coated with the aqueous quaternary polymethacrylate dispersion Eudragit RS 30 D. Pharmazie. 2001;56(6):477–83.

    CAS  PubMed  Google Scholar 

  21. Nisar ur Rahman, Yuen KH, Khan NA, Wong JW. Drug–polymer mixed coating: a new approach for controlling drug release rates in pellets. Pharm Dev Technol. 2006;11(1):71–7.

    Article  CAS  PubMed  Google Scholar 

  22. Chen S, Zhu J, Cheng J. Preparation and in vitro evaluation of a novel combined multiparticulate delayed-onset sustained-release formulation of diltiazem hydrochloride. Pharmazie. 2007;62(12):907–13.

    CAS  PubMed  Google Scholar 

  23. Huang HF, Lu Y, He HB, Tang X. Preparation and bioavailability of sustained-release doxofylline pellets in beagle dogs. Drug Dev Ind Pharm. 2008;34(7):676–82.

    Article  CAS  PubMed  Google Scholar 

  24. Ghaffari A, Avadi MR, Moghimi HR, Oskoui M, Bayati K, Rafiee-Tehrani M. Mechanistic analysis of drug release from theophylline pellets coated by films containing pectin, chitosan and Eudragit RS. Drug Dev Ind Pharm. 2008;34(4):390–02.

    Article  CAS  PubMed  Google Scholar 

  25. Mikatos A, Panderi I. Determination of the carboxylic acid metabolite of clopidogrel in human plasma by liquid chromatography–electrospray ionisation mass spectrometry. Analytica Chim Acta. 2004;505:107–14.

    Article  Google Scholar 

  26. Zahirul M, Khan I, Dragica Raušl, et al. Classification of loratadine based on the biopharmaceutics drug classification concept and possible in vitro–in vivo correlation. Biol Pharm Bull. 2004;27:1630–35.

    Article  Google Scholar 

  27. Flament MP, Leterme P, Gayot A, Gendrot E, Bruna E, Cousin G. Development and industrial scale-up of tablets containing modified-release pellets. Pharm Technol Eur. 1994;2:19–25.

    Google Scholar 

  28. Vergote GJ, Kiekens F, Vervaet C, Remon JP. Wax beads as cushioning agents during the compression of coated diltiazem pellets. Eur J Pharm Sci. 2002;17:145–51.

    Article  CAS  PubMed  Google Scholar 

  29. Celik M. Compaction of multiparticulate oral dosage forms. In: Ghebre-Sellasie, editor. Multiparticulate oral drug delivery. New York: Marcel Dekker; 1994. p. 181–15.

    Google Scholar 

Download references

Declaration of interest

The authors report no declaration of interest.

Author information

Authors and Affiliations

  1. Department of Pharmaceutical Technology, School of Pharmacy and Allied Health Sciences, International Medical University, Bukit Jalil, 57000, Kuala Lumpur, Malaysia

    Farrukh Zeeshan & Nadeem Irfan Bukhari

Authors
  1. Farrukh Zeeshan
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Nadeem Irfan Bukhari
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Farrukh Zeeshan.

Rights and permissions

Reprints and permissions

About this article

Cite this article

Zeeshan, F., Bukhari, N.I. Development and Evaluation of a Novel Modified-Release Pellet-Based Tablet System for the Delivery of Loratadine and Pseudoephedrine Hydrochloride as Model Drugs. AAPS PharmSciTech 11, 910–916 (2010). https://doi.org/10.1208/s12249-010-9456-2

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1208/s12249-010-9456-2

Key words

Search

Navigation