Formulation and Functional Characterization of a Novel Co-Processed Excipient for Direct Compression: Evaluation by the SeDeM Expert System

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Abstract
Background/Objectives: Although pharmaceutical formulations on the market are more varied than in previous decades, developing tablets remains a continuing interest due to increased patient compliance. Simultaneously, the development of multifaceted excipients has remained a requirement of the pharmaceutical industry. This study aimed to develop a granular co-processed excipient for tablets and to evaluate it using the SeDeM expert system. Methods: Six granule formulations (obtained via wet layering granulation) were developed using different binder concentrations, fillers, and core types. The binders’ concentration (AquaPolish® STA) varied on three levels: 10%, 15%, and 20%. Three formulations used microcrystalline cellulose as the filler, while the remaining three replaced it with lactose (six formulations coded E1-E6). The granules obtained were evaluated using the SeDeM expert system for all 12 characteristic parameters, encompassing six incidence factors. The unloaded granules were compressed to yield uncoated tablets, which were verified for dimensional parameters, mechanical properties, and disintegration ability in accordance with the in-force European Pharmacopoeia requirements. Results: The binder concentration influenced particle size, with a 20% AquaPolish® STA concentration yielding large granules. It has been observed that the type of core used to prepare the granules played an important role in establishing mechanical strength; thus, the formulation in which Cellets® was used exhibited lower resistance than those in which sugar was used. During the SeDeM evaluation, it was observed that two formulations (E4 and E5) exhibited good results in terms of the parameter index (PI), parameter profile index (PPI), and Good Compressibility Index (GCI). The recorded disintegration times were less than 15 minutes for all the tablets obtained from the formulated granules. Conclusions: For granule development, binder concentration had the greatest influence on particle size, mechanical strength, and lubricity; also, the type of core used played an important role in tablet mechanical strength. With the help of the SeDeM expert system, the excipients most suitable for developing uncoated tab-lets were highlighted.

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