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Evaluation of Alternative Metallic Stearates as Lubricants in Pharmaceutical Tablet Formulation

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Abstract

Magnesium stearate (MgSt) is perhaps one of the most frequently used lubricants in tablet formulation due to its superior lubrication capacity, yet it could also negatively affect the critical quality attributes of pharmaceutical products. Therefore, we provided a rather comprehensive evaluation of another two FDA-approved metallic stearates, sodium stearate (NaSt) and calcium stearate (CaSt), as alternative tablet lubricants. The primary objective of the present study is to comparatively evaluate the physicochemical properties and lubrication efficiency of the three metallic stearates. In addition, it was also aimed to specify the most influential factor for ranking and differentiating the lubricity of various lubricants using principal component analysis. Unit ejection force could be used herein as a simple and the most powerful parameter to evaluate the lubrication performance instead of the friction coefficient. The results suggested that CaSt, MgSt, and NaSt had similar impacts on the mechanical strength of tablets. However, CaSt exhibited insufficient lubrication effects as the formulations containing CaSt showed low pressure transmission ratios, high unit ejection forces, and high friction coefficients. In contrast, both MgSt and NaSt displayed satisfactory lubrication efficiency without negatively impacting tabletability. Notably, the lubrication performance of the formulation containing 0.5 wt% NaSt was almost identical to that of the formulation with 1 wt% MgSt, indicating that NaSt had a remarkable lubrication capability probably due to its high specific surface area. In summary, the findings of this investigation should provide practical information and feasible methodologies to readily determine the lubricity and to sensibly select alternative lubricants for pharmaceutical tablet formulations.

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Acknowledgements

The authors would like to thank Drs. Gerard Klinzing, Meng Li, Jiaying Liu, and Christopher John for providing helpful scientific discussions. Drs. Ting Xu and Jie Ren are specially acknowledged for technical/experimental contributions and data processing. D.Y. is grateful to the visiting scholar opportunity provided by the Center for Materials Science and Engineering at Merck & Co., Inc.

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Authors and Affiliations

  1. Department of Pharmaceutical Sciences, University of Maryland, Baltimore, MD, USA

    Dongyue Yu

  2. Center for Materials Science and Engineering, Merck & Co., Inc., 770 Sumneytown Pike, , West Point, PA, 19486, USA

    Dongyue Yu & Haichen Nie

  3. Department of Industrial and Physical Pharmacy, Purdue University, 575 Stadium Mall Drive, West Lafayette, IN, 47907, USA

    Haichen Nie

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  1. Dongyue Yu
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Contributions

Dongyue Yu: Methodology, formal analysis, writing — original draft.

Haichen Nie: Conceptualization, methodology, formal analysis, investigation, resources, visualization, project administration, writing — review and editing, visualization.

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Correspondence to Haichen Nie.

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Yu, D., Nie, H. Evaluation of Alternative Metallic Stearates as Lubricants in Pharmaceutical Tablet Formulation. AAPS PharmSciTech 23, 200 (2022). https://doi.org/10.1208/s12249-022-02338-1

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