Effects of thermal binders on chemical stabilities and tabletability of gabapentin granules prepared by twin-screw melt granulation

Nada Kittikunakorn, J. Joseph Koleng, Tony Listro, Changquan Calvin Sun, Feng Zhang

Research output: Contribution to journalArticlepeer-review

8 Scopus citations

Abstract

The effect of thermal binders on the physicochemical properties of gabapentin, a thermally labile drug, in granules prepared using twin-screw melt granulation was investigated in this study. Hydroxypropyl cellulose (HPC), a thermoplastic high molecular-weight binder, was compared against conventional low molecular-weight semi-crystalline thermal binders PEG 8000 and Compritol. Both the chemical degradation and polymorph form change of gabapentin were analyzed. The effects of particle size and molecular weight of HPC on the properties of granules were also studied. To overcome the high melt viscosity of HPC, higher barrel temperatures and higher specific mechanical energy were required to attain suitable granules. As a result, higher levels of gabapentin degradant were observed in HPC-based formulations. However, gabapentin form change was not observed in all formulations. Smaller particle size and lower molecular weight of HPC led to faster granule growth. The tabletability of granules was insensitive to the variations in particle size and molecular weight of HPC. Gabapentin crystal size reduction, HPC size reduction, and HPC enrichment on granule surface were observed for HPC-based granules.

Original languageEnglish (US)
Pages (from-to)37-47
Number of pages11
JournalInternational journal of pharmaceutics
Volume559
DOIs
StatePublished - Mar 25 2019

Bibliographical note

Funding Information:
The authors would like to thank Foster Delivery Science (Putnam, CT, USA) for the financial support of this study.

Publisher Copyright:
© 2019 Elsevier B.V.

Keywords

  • Continuous manufacturing
  • Gabapentin
  • Hydroxypropyl cellulose
  • Tabletability
  • Twin-screw melt granulation

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