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AAPS PharmSciTech

, Volume 12, Issue 4, pp 1241–1247 | Cite as

Effect of Different Excipients on the Physical Characteristics of Granules and Tablets with Carbamazepine Prepared with Polyethylene Glycol 6000 by Fluidized Hot-Melt Granulation (FHMG)

  • Radosław Kraciuk
  • Malgorzata Sznitowska
Research Article Theme: Advanced Technologies for Oral Controlled Release

Abstract

The objective of this study was to investigate the properties of granules and tablets with carbamazepine which were prepared employing a fluidized hot-melt granulation (FHMG) technique. The FHMG process was carried out at 65°C. Macrogol 6000 (PEG 6000) was used as a binder at the content 10% (w/w) of the granulated mass. Granules containing up to 70% (w/w) of the drug and 20–90% (w/w) of a filler (lactose, mannitol, calcium hydrogen phosphate (Di-Cafos), pregelatinized starch, and microcrystalline cellulose (MCC)) were produced. When the drug content was 30% (w/w), the yield of the process was satisfying (>95%) and flowability of the granules was better than placebo granules or drug-loaded granules prepared by wet granulation. Type of a filler had strong impact on physical properties of granules, and size distribution of the particles was the most homogenous when lactose or Di-Cafos were used. The FHMG technique enabled preparation of granules with better compressability compared with the wet-granulated product or with non-granulated powders. Tablets with shorter disintegration time than 10 min were obtained with 2.0% crospovidone added as a disintegrant. In comparison to tablets prepared from the wet-granulated mass, employment of the FHMG method resulted in tablets with faster dissolution of carbamazepine (more than 80% of the drug released within 15 min). This was achieved with mannitol or lactose/MCC, as fillers.

KEY WORDS

carbamazepine dissolution fluidized hot-melt granulation macrogol tablets 

REFERENCES

  1. 1.
    Parikh DM, Bonck JA, Maogavero M. Batch fluid bed granulation. In: Parikh DM, editor. Handbook of pharmaceutical granulation technology. New York: Marcel Dekker; 1997. p. 227–302.Google Scholar
  2. 2.
    Tousey MD. The granulation process 101. Basic technologies for tablet making. Pharm Technol. 2002;8–13.Google Scholar
  3. 3.
    Holm P. High Shear Mixer granulators. In: Parikh DM, editor. Handbook of pharmaceutical granulation technology. New York: Marcel Dekker; 1997. p. 194–8.Google Scholar
  4. 4.
    Abberger T, Seo A, Schaefer T. The effect of droplet size and powder particle size on the mechanisms of nucleation and growth in fluid bed melt agglomeration. Int J Pharm. 2002;249:185–97.PubMedCrossRefGoogle Scholar
  5. 5.
    Walker GM, Holland CR, Ahmad MMN, Craig DQM. Influence of process parameters on fluidized hot-melt granulation and tablet pressing of pharmaceutical powders. Chem Eng Sci. 2005;60:3867–77.CrossRefGoogle Scholar
  6. 6.
    Kidokoro M, Haramiishi Y, Sagasaki S, Shimizu T, Yamamoto Y. Application of fluidized hot-melt granulation (FHMG) for the preparation of granules for tableting; properties of granules and tablets prepared by FHMG. Drug Dev Ind Pharm. 2002;28:67–76.PubMedCrossRefGoogle Scholar
  7. 7.
    Craig DQM. The mechanism of drug release from solid dispersions in water-soluble polymers. Int J Pharm. 2002;231:131–44.PubMedCrossRefGoogle Scholar
  8. 8.
    Passerini N, Calogera G, Albertini B, Rodriguez L. Melt granulation of pharmaceutical powders: a comparison of high-shear mixer and fluidised bed processes. Int J Pharm. 2010;391:177–86.PubMedCrossRefGoogle Scholar

Copyright information

© American Association of Pharmaceutical Scientists 2011

Authors and Affiliations

  1. 1.Pharmaceutical Works Polpharma SAStarogard GdańskiPoland
  2. 2.Department of Pharmaceutical TechnologyMedical University of GdańskGdańskPoland

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