A new deferiprone controlled release system obtained by ultrasound-assisted compression

Pharm Dev Technol. 2014 Sep;19(6):728-34. doi: 10.3109/10837450.2013.829091. Epub 2013 Aug 28.

Abstract

Objectives: This study implements the design of an innovative dosage form using ultrasound-assisted compression of thermoplastic polymers and the development of controlled release tablets for the oral administration of deferiprone in two doses per day.

Methods: Binary matrix tablets containing deferiprone and thermoplastic polymers have been prepared using an ultrasound-assisted tableting machine. Scanning electron microscopy has been employed to determine a sintering phenomenon of the excipients. Water uptake and drug release studies have been carried out to evaluate the ability of the polymers to control the drug release.

Results: SEM micrographs showed that some polymers underwent the sintering process and the in vitro dissolution test showed good fit of the release data from these tablets to the zero-order kinetic model.

Conclusions: Carbopol 974P and 971P have been selected as matrix forming polymers for the final formulation. The polymer percolation threshold has been exceeded with 15% w/w of polymer. Therefore, sustained release tablets have been developed with only 15% of excipient. This implies that matrix tablets containing 750 mg of API, intended for two administrations a day, can be obtained with a similar weight to those existing in the market containing 500 mg of API for three administrations a day.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Deferiprone
  • Delayed-Action Preparations / chemistry*
  • Dosage Forms
  • Drug Compounding / methods
  • Excipients / chemistry
  • Kinetics
  • Polymers / chemistry
  • Pyridones / chemistry*
  • Tablets / chemistry
  • Ultrasonics / methods
  • Water / chemistry

Substances

  • Delayed-Action Preparations
  • Dosage Forms
  • Excipients
  • Polymers
  • Pyridones
  • Tablets
  • Water
  • Deferiprone