Processing challenges with solid dosage formulations containing vitamin E TPGS

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.

Keywords::

• Wet granulation
• vitamin E TPGS
• compaction
• dwell time
• colloidal silicon dioxide
• Aeroperl^® 300

Acknowledgements

The authors would like to thank Elena Zour, Munir Hussain, David Buckley, and Robert Jerzewski for their support and guidance during this work.

Declaration of Interest

The authors declare no conflicts of interest.