Ϫ Indicates absence. ϩ, ϩϩ, ϩϩϩ Indicate level of abundance.

Glidants play a vital role in tablet formulation. This study aimed to examine the impact of glidants on the compaction and tableting properties of paracetamol granules prepared by wet granulation. Three formulations of paracetamol granules were prepared to consist of either talc, colloidal silicon dioxide (CSD) or a combination of both in equal proportion (1:1) as glidants added extragranularly. The granules were characterised by measuring the particle size, angle of repose, bulk and tapped densities, true densities, and moisture content. Compaction studies on the granules were carried out using the Heckel, Kawakita, Walker, and compressibility-tabletability-compactibility (CTC) models. Tablets were prepared from the granules for each formulation and evaluated according to USP requirements. The results of the granule analysis revealed that granule properties were similar across the formulations irrespective of the type of glidant used. Compaction studies revealed that talc granules exhibited a greater degree of plasticity and compressibility compared to the other formulations. However, CSD granules and granules containing the two glidants in equal proportion were found to have better compactibility and tabletability, resulting in tablets with relatively better properties. This study has underscored the impact of glidants on the compaction and tableting properties of paracetamol granules.

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The functionality of a co-processed excipient is usually derived from its composition and the proportion of each excipient that is incorporated to yield a composite excipient. The aim of this study was to assess the impact of binder as a formulation variable on the material and tableting properties of developed co-processed excipients containing gelatin (SGS) and microcrystalline cellulose (SMS) as binders respectively in the same proportion. Two co-processed excipients, SGS and SMS were generated by combining tapioca starch (90%), gelatin or microcrystalline cellulose (7.5%) and colloidal silicon dioxide (2.5%) using the co-fusion method. Particle size analysis and morphological assessment were carried out by light microscopy and scanning electron microscopy (SEM) respectively. DSC analysis was performed to evaluate the thermal behaviour of both materials and flow properties were assessed by measuring parameters like angle of repose, bulk and tapped densities, Carr's index and Hausner's ratio. Compaction behaviour of both materials was determined using Heckel and Walker equations and the compressibility-tabletability-compactibility (CTC) profile for each material was obtained. Particulate and bulk-level properties of SGS and SMS revealed spherical-shaped, free-flowing powders characterized by a glass transition event typical of amorphous polymers. Compaction analysis demonstrated greater degree of plastic deformation with SMS resulting in better tableting properties with respect to tensile strength and disintegration time. The outcome of the study shows that the choice of binder used in the formulation of a co-processed excipient plays a crucial role in defining the material and tableting properties of the co-processed excipient.

Background Computer-aided formulation design is gaining fantastic attention in chemical engineering of high functionality pharmaceutical materials for dosage form manufacture. To accelerate development of novel formulations in a quality-by-design perspective, SeDeM Expert System preformulation algorithm was developed as a tool for the design of solid drug delivery systems and for prediction of direct compression manufacturability of solid formulations. This research aims to integrate SeDeM Expert System into particle engineering design space of co-processing of solid excipients to develop novel composites with optimum direct compression propensity, using corn starch and microcrystalline cellulose powders as model primary excipients. Result The data and information generated from the expert system have elucidated the bulk-level characteristics of the primary excipients, enabled computation of the optimum co-processing ratio of the ingredients, and validated the impact of co-processing on material functionality. The experimental flowability (7.78±0.17), compressibility functions (5.16±0.14), parameter profile (0.92), and parametric profile index (6.72±0.27) of the engineered composites, were within the acceptable thresholds. With a reliability constant of 0.961, the net direct compression propensity of the composites expressed as Good Compression Index (6.46±0.26) was superior to that of the primary excipients, but comparable to reference co-processed materials, StarLac® (6.44±0.14) and MicroceLac®100 (6.58±0.03). Conclusion Application of SeDeM Expert System in particle engineering via co-processing has provided an accelerated upstream proactive mechanism for designing directly compressible co-processed excipients in a quality-by-design fashion. A four-stage systematic methodology of co-processing of solid excipients was postulated. Stage I entails the characterization of CMAs of both defective and corrective excipients, and elucidation of their physicomechanical limitations using SeDeM diagrams. Stage II involves computation of loading capacity of the corrective excipient using dilution potential equation. Stage III entails the selection of co-processing technique based on desired Critical Material Attributes as revealed by the information obtained from Stage I. Stage IV evaluates the impact of co-processing by monitoring the critical behavior of the engineered composites with a decision on either to accept or reject the product.