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Powder adhesion or sticking onto punches is one of the outstanding issues in pharmaceutical tablet manufacturing. We show in this work that, at comparable particle sizes, the acesulfame potassium exhibited pronouncedly reduced propensity to punch sticking than acesulfame. Detailed analyses revealed strong correlation between sticking propensity and crystal mechanical properties and surface chemistry. The free acid was highly plastic with high cohesive strength while the salt form was brittle. During compaction, surfaces of acesulfame in contact with punch face are abundant in electronegative functional groups while those of the salt consists of mainly hydrophobic groups. Thus, acesulfame underwent stronger interactions with the electron deficient punch. Consequently, the strikingly different onset and severity of sticking propensity between the two solid forms of acesulfame could be clearly explained based on their different crystal mechanical property and surface characteristics. By providing molecular insight into an outstanding problem in pharmaceutical tablet manufacturing, this work expands the list of pharmaceutical properties that can benefit from crystal engineering by including punch sticking.
This article was published in the following journal.
Name: Molecular pharmaceutics
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Enzyme complexes that catalyze the formation of PROSTAGLANDINS from the appropriate unsaturated FATTY ACIDS, molecular OXYGEN, and a reduced acceptor.