Novel sustained-release fast-disintegrating multi-unit compressed tablets of lornoxicam containing Eudragit RS coated chitosan-alginate beads

Pharm Dev Technol. 2011 Aug;16(4):316-30. doi: 10.3109/10837451003692595. Epub 2010 Mar 23.

Abstract

Novel fast-disintegrating multi-unit tablets (FDMUTs) were prepared to modify the release of lornoxicam (a potent non-steroidal anti-inflammatory drug with a short half-life) as well as to combine the advantages of multi-unit systems with the cost-effectiveness of compressed tablets. The proposed FDMUTs consisted of sustained-release lornoxicam beads directly compressed with fast-disintegrating component, containing amorphous solid dispersion of lornoxicam, anticipating rapid drug release that starts in the stomach to rapidly alleviate the painful symptoms and continues in the intestine to maintain extended analgesic effect. Initially, calcium-alginate and chitosan-alginate beads containing lornoxicam were prepared. Then, the erosion of selected beads formulation was suppressed by treatment with Eudragit RS either through polymer-reinforcement or beads coating. The beads, which elicited appropriate sustainment of lornoxicam release, were directly compressed with fast-disintegrating components to form FDMUTs. The release characteristics of the original beads were maintained after compression which indicates that the adopted compression process did not induce mechanical damage to the beads or coating. All of the prepared FDMUTs demonstrated acceptable physical properties that complied with compendial requirements. Release studies, performed in simulated gastric and intestinal fluids used in sequence to mimic the gastrointestinal transit, illustrate that the FDMUTs containing 8?mg lornoxicam equally distributed between the sustained-release beads and the fast-release component, showed the desired release profile.

MeSH terms

  • Acrylic Resins / administration & dosage*
  • Alginates / administration & dosage
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Chemical Phenomena
  • Chitosan / administration & dosage
  • Delayed-Action Preparations / chemistry*
  • Drug Carriers / chemistry
  • Drug Compounding / methods
  • Drug Stability
  • Excipients / administration & dosage
  • Excipients / chemistry
  • Gastric Juice / metabolism
  • Gastrointestinal Transit
  • Glucuronic Acid / administration & dosage
  • Hexuronic Acids / administration & dosage
  • Humans
  • Hydrogen-Ion Concentration
  • Intestinal Secretions / metabolism
  • Piroxicam / administration & dosage
  • Piroxicam / analogs & derivatives*
  • Piroxicam / pharmacokinetics
  • Solubility
  • Tablets

Substances

  • Acrylic Resins
  • Alginates
  • Anti-Inflammatory Agents, Non-Steroidal
  • Delayed-Action Preparations
  • Drug Carriers
  • Excipients
  • Hexuronic Acids
  • Tablets
  • Piroxicam
  • Eudragit RS
  • Glucuronic Acid
  • Chitosan
  • lornoxicam