Processing challenges with solid dosage formulations containing vitamin E TPGS

Pharm Dev Technol. 2013 Feb;18(1):296-304. doi: 10.3109/10837450.2012.737807. Epub 2012 Nov 9.

Abstract

The objective of this study is to investigate processing challenges associated with the incorporation of Vitamin E TPGS (d-α tocopheryl polyethylene glycol 1000 succinate) into solid pharmaceutical dosage forms. For this work, a wet granulation process (high-shear and fluid bed) was used and Vitamin E TPGS was added as part of the binder solution during granulation. It was shown that Vitamin E TPGS can be incorporated into a prototype formulation at 10% w/w concentration without any significant processing challenges. However, the resulting granulations could only be compressed successfully at low tablet press speeds (dwell time ~100 ms). When compressed at low dwell times (<20 ms) representative of commercial tablet manufacturing, a significant loss in compactability was observed. In addition, several other tablet defects were observed. It was shown that intragranular incorporation of Aeroperl(®) 300, a granulated form of colloidal silicon dioxide, was able to overcome these compaction problems. The formulation consisting of Aeroperl(®) 300 showed significantly lower granule particle size, higher granule porosity and higher compactability as compared to the formulation without Aeroperl(®) 300.

Publication types

  • Comparative Study

MeSH terms

  • Colloids
  • Drug Compounding / methods*
  • Excipients / chemistry*
  • Particle Size
  • Polyethylene Glycols / chemistry
  • Porosity
  • Silicon Dioxide / chemistry*
  • Tablets
  • Time Factors
  • Vitamin E / analogs & derivatives*
  • Vitamin E / chemistry

Substances

  • Colloids
  • Excipients
  • Tablets
  • Vitamin E
  • Polyethylene Glycols
  • Silicon Dioxide
  • tocophersolan