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Stability of Benzocaine Formulated in Commercial Oral Disintegrating Tablet Platforms

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Abstract

Pharmaceutical excipients contain reactive groups and impurities due to manufacturing processes that can cause decomposition of active drug compounds. The aim of this investigation was to determine if commercially available oral disintegrating tablet (ODT) platforms induce active pharmaceutical ingredient (API) degradation. Benzocaine was selected as the model API due to known degradation through ester and primary amino groups. Benzocaine was either compressed at a constant pressure, 20 kN, or at pressure necessary to produce a set hardness, i.e., where a series of tablets were produced at different compression forces until an average hardness of approximately 100 N was achieved. Tablets were then stored for 6 months under International Conference on Harmonization recommended conditions, 25°C and 60% relative humidity (RH), or under accelerated conditions, 40°C and 75% RH. Benzocaine degradation was monitored by liquid chromatography–mass spectrometry. Regardless of the ODT platform, no degradation of benzocaine was observed in tablets that were kept for 6 months at 25°C and 60% RH. After storage for 30 days under accelerated conditions, benzocaine degradation was observed in a single platform. Qualitative differences in ODT platform behavior were observed in physical appearance of the tablets after storage under different temperature and humidity conditions.

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ACKNOWLEDGMENTS

This investigation was conducted in a facility constructed with support from Research Facilities Improvement Program Grant C06 RR15482 from the National Centre for Research Resources, NIH. This research was funded in part by Roquette America, Inc. The authors would like to thank Dr. Jerry White and Bryan Zahakaylo of UIC-RRC Mass Spectrometry Facility for significant help with LC-MS.

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Authors and Affiliations

  1. Department of Biopharmaceutical Sciences, University of Illinois, Chicago, Illinois, 60612-7231, USA

    Melanie Köllmer & Richard A. Gemeinhart

  2. Roquette America Inc., Geneva, Illinois, 60134, USA

    Carmen Popescu, Prashanth Manda & Leon Zhou

  3. Department of Pharmaceutics, University of Mississippi, University, Mississippi, 38677, USA

    Prashanth Manda

  4. Department of Bioengineering, University of Illinois, Chicago, Illinois, 60607-7052, USA

    Richard A. Gemeinhart

  5. Department of Ophthalmology and Visual Sciences, University of Illinois, Chicago, Illinois, 60612-4319, USA

    Richard A. Gemeinhart

Authors
  1. Melanie Köllmer
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  2. Carmen Popescu
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  3. Prashanth Manda
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  4. Leon Zhou
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  5. Richard A. Gemeinhart
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Correspondence to Richard A. Gemeinhart.

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Köllmer, M., Popescu, C., Manda, P. et al. Stability of Benzocaine Formulated in Commercial Oral Disintegrating Tablet Platforms. AAPS PharmSciTech 14, 1333–1340 (2013). https://doi.org/10.1208/s12249-013-0015-5

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  • DOI: https://doi.org/10.1208/s12249-013-0015-5

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