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Published on: July 4, 2014
Excipient interaction with cetylpyridinium chloride activity in tablet based lozenges
R M Richards1, J Z Xing, K M Mackay
1School of Pharmacy, Robert Gordon University, Schoolhill, Aberdeen, United Kingdom.
Tablet excipients, particularly magnesium stearate, significantly reduce the antimicrobial activity of cetylpyridinium chloride (CPC) in lozenges. To maintain CPC efficacy, limit magnesium stearate to 0.3% w/w in tablet formulations.
Area of Science:
- Pharmaceutical Sciences
- Microbiology
Background:
- Cetylpyridinium chloride (CPC) is an antiseptic agent used in oral hygiene products.
- Tablet excipients can potentially affect the stability and efficacy of active pharmaceutical ingredients.
Purpose of the Study:
- To investigate the impact of tablet excipients on the antimicrobial activity of cetylpyridinium chloride (CPC).
- To determine the interaction between specific excipients and CPC.
Main Methods:
- Developed an analytical assay to assess CPC-excipient interactions.
- Conducted in vivo studies with human volunteers to measure oropharyngeal microbial reduction.
- Performed in vitro antimicrobial activity tests against Staphylococcus aureus, Streptococcus pyogenes, and Candida albicans, evaluating excipient and pH effects.
Main Results:
- Tablet-based lozenges showed significantly reduced antimicrobial activity compared to candy-based lozenges or aqueous CPC solutions.
- Magnesium stearate was found to adsorb CPC, leading to a substantial decrease in antimicrobial activity at concentrations of 0.4% lozenge weight and higher.
Conclusions:
- Reduced CPC activity in tablet lozenges is attributed to its adsorption by magnesium stearate, decreasing its availability in solution.
- For tablet lozenges containing CPC at 250 µg/ml, magnesium stearate content should not exceed 0.3% w/w to prevent significant reduction in antimicrobial efficacy.
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