Systematic screening of compressed ODT excipients: cellulosic versus non-cellulosic

Curr Drug Deliv. 2014;11(4):486-500. doi: 10.2174/1567201811666140323201650.

Abstract

The successful development of compressed ODTs utilises low compression forces to create a porous structure whereby excipients are added to enhance wicking/swelling action or provide strength to the fragile tablet framework. In this work, a systematic investigation comparing materials from two different categories was employed to understand their functionality in binary mixture tablets of the most commonly used diluent mannitol. Cellulose based excipients such as HPC (SSL-SFP), L-HPC (NBD-022) and MCC (Avicel PH-102) were compared with non-cellulosic materials such as PEO (POLYOX WSR N-10) and Crospovidone (XL-10). Pure excipient properties were studied using Heckel Plot, compressibility profile, SEM and XRPD, whereas the prepared binary mixture compacts were studied for hardness, disintegration time and friability. Results from our investigation provide insight into differences encountered in product performance of ODT upon inclusion of additional materials. For example, non-cellulosic excipients Polyox and Crospovidone showed higher plasticity (Py values 588 and 450MPa) in pure form but not in binary mixtures of mannitol. Cellulosic excipients, nonetheless, offer faster disintegration (<30 sec) specifically L-HPC and MCC tablets. Disintegration time for tablets with fully substituted-HPC was prolonged (200-500 sec) upon increasing concentration between 1-10% due to gelation/ matrix formation. It can be concluded that despite the reasonably good plasticity of both cellulosic and noncellulosic excipients in pure form, the mechanical strength in binary mixtures is negatively impacted by the fragmentation/ fracture effect of mannitol.

Publication types

  • Comparative Study
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Cellulose / chemistry*
  • Cellulose, Oxidized
  • Drug Compounding
  • Drug Delivery Systems* / trends
  • Excipients / chemistry*
  • Hardness
  • Humans
  • Kinetics
  • Pharmaceutical Preparations / administration & dosage*
  • Pharmaceutical Preparations / chemistry
  • Solubility
  • Surface Properties
  • Tablets

Substances

  • Cellulose, Oxidized
  • Excipients
  • Pharmaceutical Preparations
  • Tablets
  • Cellulose