Sustained release of hydrophobic and hydrophilic drugs from a floating dosage form

Int J Pharm. 2007 May 4;336(1):159-65. doi: 10.1016/j.ijpharm.2006.11.060. Epub 2006 Dec 3.

Abstract

Floating dosage forms enable the sustained delivery of drugs in the gastro-intestinal tract. In this study, a type of multi-unit floating gel bead was synthesized with calcium alginate, sunflower oil, and a drug of interest through an emulsification/gelation process. The alginate beads with oil addition were able to continuously float over the medium for 24h under constant agitation while the non-oily beads could not. Three kinds of drugs with different hydrophilicities, ibuprofen, niacinamide and metoclopramide HCl, were tested in the study. The hydrophobic drug ibuprofen was released in a sustained manner for 24h, due to the oil partitioning. With suitable modification, the beads were able to also release the hydrophilic drugs, niacinamide and metoclopramide HCl, for a similar duration. Therefore a floating dosage form that is able to sustain release both hydrophobic and hydrophilic drugs within its extended gastric retention time has been developed.

MeSH terms

  • Alginates / chemistry
  • Delayed-Action Preparations / chemistry*
  • Delayed-Action Preparations / pharmacokinetics
  • Gastric Juice / chemistry
  • Gels
  • Glucuronic Acid / chemistry
  • Hexuronic Acids / chemistry
  • Ibuprofen / chemistry*
  • Ibuprofen / pharmacokinetics
  • Metoclopramide / chemistry*
  • Metoclopramide / pharmacokinetics
  • Microscopy, Electron, Scanning
  • Niacinamide / chemistry*
  • Niacinamide / pharmacokinetics
  • Particle Size
  • Plant Oils / chemistry
  • Polymethacrylic Acids / chemistry
  • Polyvinyl Alcohol / chemistry
  • Sunflower Oil
  • Water / analysis
  • Water / chemistry

Substances

  • Alginates
  • Delayed-Action Preparations
  • Gels
  • Hexuronic Acids
  • Plant Oils
  • Polymethacrylic Acids
  • Sunflower Oil
  • Water
  • methylmethacrylate-methacrylic acid copolymer
  • Niacinamide
  • Glucuronic Acid
  • Polyvinyl Alcohol
  • Metoclopramide
  • Ibuprofen