Gastroretentive Extended-Release Floating Granules Prepared Using a Novel Fluidized Hot Melt Granulation (FHMG) Technique

H. Zhai, D. S. Jones, C. P. McCoy, A. M. Madi, Yiwei Tian, G. P. Andrews*

*Corresponding author for this work

Research output: Contribution to journalArticle

8 Citations (Scopus)

Abstract

The objective of this work was to investigate the feasibility of using a novel granulation technique, namely, fluidized hot melt granulation (FHMG), to prepare gastroretentive extended-release floating granules. In this study we have utilized FHMG, a solvent free process in which granulation is achieved with the aid of low melting point materials, using Compritol 888 ATO and Gelucire 50/13 as meltable binders, in place of conventional liquid binders. The physicochemical properties, morphology, floating properties, and drug release of the manufactured granules were investigated. Granules prepared by this method were spherical in shape and showed good flowability. The floating granules exhibited sustained release exceeding 10 h. Granule buoyancy (floating time and strength) and drug release properties were significantly influenced by formulation variables such as excipient type and concentration, and the physical characteristics (particle size, hydrophilicity) of the excipients. Drug release rate was increased by increasing the concentration of hydroxypropyl cellulose (HPC) and Gelucire 50/13, or by decreasing the particle size of HPC. Floating strength was improved through the incorporation of sodium bicarbonate and citric acid. Furthermore, floating strength was influenced by the concentration of HPC within the formulation. Granules prepared in this way show good physical characteristics, floating ability, and drug release properties when placed in simulated gastric fluid. Moreover, the drug release and floating properties can be controlled by modification of the ratio or physical characteristics of the excipients used in the formulation.

Original languageEnglish
Pages (from-to)3471-3483
Number of pages13
JournalMolecular Pharmaceutics
Volume11
Issue number10
Early online date08 Aug 2014
DOIs
Publication statusPublished - Oct 2014

Keywords

  • gastroretention
  • floating granules
  • granulation
  • FMHG
  • oral drug delivery
  • metronidazole
  • CONTROLLED DRUG-DELIVERY
  • HELICOBACTER-PYLORI
  • MATRIX TABLETS
  • DOSAGE FORMS
  • SOLID DISPERSIONS
  • GASTRO-RETENTION
  • ALGINATE BEADS
  • CITRIC-ACID
  • IN-VITRO
  • SYSTEMS

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