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.
Background
Orally disintegrating tablets (ODTs) promote patient compliance due to their great convenience in use. ODTs are palatable, in terms of taste and mouth feel and no water is needed for swallowing. The FDA recommends that ODTs should disintegrate rapidly in the mouth in 30 seconds or less and ODTs should weigh less than 500 mg. Excipients selection is critical in reaching the main design attributes.
Ready to use ODT platforms have been developed to accelerate the formulation process for new APIs. Hydrophilic filler and the superdisintegrant are co-processed in ODT-platforms so that the formulator has to add only the API and the lubricant. However, the stability of the API can be affected by pharmaceutical excipients that react directly with the drug or contain reactive impurities such as peroxides, formaldehyde, formic acid, antioxidants, organic acids, reducing sugars.
Polyvinylpyrrolidone excipients (povidone, crospovidone, copovidone, Kollidon) that are components of many commercially available ODT platforms often contain peroxides or other oxidative impurities like formaldehyde or formic acid.