Approaches to developing fast release pellets via wet extrusion-spheronization

Pharm Dev Technol. 2018 Jun;23(5):432-441. doi: 10.1080/10837450.2016.1265556. Epub 2016 Dec 9.

Abstract

Microcrystalline cellulose (MCC) is widely regarded as the excellent choice to manufacture pellets via wet extrusion-spheronisation (ES) process due to its excellent water uptake capability, water holding capacity, desirable rheological properties, cohesiveness and plasticity etc. Nevertheless, in spite of all these advantages, limitations associated with the application of MCC also have been reported. The most prevailing limitation is prolonged or incomplete drug release profile due to the lack of disintegration as pellet contracts significantly during the drying process, especially when in combination with poorly soluble drug at a high level. This characteristic limits the application of MCC in immediate release formulations. Over the years, many approaches have been tried to overcome this disadvantage, such as modifying MCC, incorporation of superdisintegrant, increasing the porosity of pellet, partial or complete substitution for MCC, enhancing the solubility of poorly soluble drug (e.g. solid dispersion, self-emulsifying drug-delivery system), etc. In this review, we will provide an updated and integrated discussion of current approaches to prepare fast release pellets via wet ES.

Keywords: Pellet; extrusion-spheronization; fast release; porosity; solubility.

Publication types

  • Review

MeSH terms

  • Cellulose / chemistry*
  • Delayed-Action Preparations / chemistry*
  • Drug Compounding / methods*
  • Emulsions / chemistry
  • Excipients / chemistry*
  • Particle Size
  • Pharmaceutical Preparations / chemistry
  • Porosity
  • Solubility
  • Water / chemistry

Substances

  • Delayed-Action Preparations
  • Emulsions
  • Excipients
  • Pharmaceutical Preparations
  • Water
  • Cellulose
  • microcrystalline cellulose