Background: The compaction of formulation blends is a critical stage in pharmaceutical tablet manufacturing, particularly when drug substances or functional excipients exhibit limited flowability and tabletability. Objectives: This study systematically examined the mechanical behaviour of viscoelastic microcrystalline cellulose (MCC) and brittle anhydrous dibasic calcium phosphate (DCPA), as well as their mixtures, to check how deformation mechanisms influence powder handling and tablet performance. Methods: A compaction simulator, mimicking a small rotary tablet press, was used to evaluate tablet weight variability, densification profiles, die-filling height, force–displacement behaviour, and in-die Heckel analysis. Additional assessments included compression times, breaking force, tensile strength, elastic recovery, as well as in-die and out-of-die tablet thickness across various compositions and compaction pressures. Results/Conclusions: Bulk density values from the simulator showed strong correlation with pharmacopeial measurements (R² ≥ 0.997). Measurable differences in true density and cohesiveness led to poor flowability for MCC and good flow for DCPA, with mixtures containing higher DCPA concentration displaying markedly improved flow characteristic. Compaction analyses confirmed extensive plastic deformation for MCC and fragmentation for DCPA. Increasing MCC content elevated die-fill height, compaction energy, and tablet weight variability, whereas higher DCPA fractions decreased apparent density of tablets and reduced energy demand. Tabletability and compressibility profiles reflected that MCC generated hard tablets but exhibited higher elastic recovery, while DCPA formed softer tablets with closer to linear strength–pressure relationships. Energy profiling demonstrated that MCC stored more elastic energy and required higher overall compression work, whereas DCPA reduced elastic accumulation. Overall, blending viscoelastic and brittle excipients offers a robust strategy for optimizing manufacturability, mechanical strength, and energy efficiency in tablet production.

Methods: Effervescent granules containing citric acid and sodium bicarbonate were successfully prepared for the first time via TS-MG using a polyol (sorbitol) as a melt binder. Results: Processing parameters, specifically granulation temperature and screw speed, were systematically varied to investigate their influence. The granulation efficiency, inversely related to the wt.% of fines, decreased in the following order across the tested conditions (granulation temperature–screw speed; ℃-rpm): 95-6 > 100-5 > 90-5 > 100-7 > 90-7. Granulation temperature had a minimal impact on the bulk and tapped densities of the uncalibrated granules, whereas increased screw speed led to higher densities, associated with a reduced proportion of fines. The tensile strength of the resulting effervescent tablets increased with granulation temperature and was generally higher for tablets derived from granules with higher granulation efficiency. The residence time within the TS-MG barrel decreased with increasing temperature and screw speed. Notably, the greatest effect of granulation temperature on tensile strength occurred between 90 and 95 °C, particularly under longer residence times. The disintegration time of the tablets was shortest for the 90 °C and 5 rpm condition, corresponding to the lowest tensile strength, while tablets across formulations showed consistent homogeneity as indicated by similar pH values post-disintegration. Conclusions: These findings underscore sorbitol’s suitability as a melt binder and highlight the interplay between TS-MG parameters and the physical characteristics of effervescent granules and tablets.

The bitter drug, warfarin, has a narrow therapeutic index (NTI) and is used in paediatrics and geriatrics. The aim of this feasibility study was to formulate the taste-masked warfarin-containing pellets to be applicable for dose personalisation and to improve patient compliance, as well as to investigate the effect of the core type (PharSQ^® Spheres M, CELPHERE™ CP-507, and NaCl) on the warfarin release from the Kollicoat^® Smartseal taste-masking-coated pellets. The cores were successfully drug-loaded and coated in a fluid-bed coater with a Wurster insert. An increase in particle size and particle size distribution was observed by optical microscopy. In saliva-simulated pH, at the Kollicoat^® Smartseal level of 2 mg/cm², none of the pellets demonstrated drug release, confirming their efficient taste-masking. However, in a stomach-simulated pH, a faster drug release was observed from PharSQ^® Spheres M- and CELPHERE™ CP-507-coated pellets in comparison with NaCl cores. Additional experiments allowed us to explain the slower drug release from NaCl-containing pellets because of the salting-out effect. Despite the successful taste masking, the drug release from pellets was relatively slow (not more than 91% per 60 min), allowing for further formulation improvements.

Background/Objectives: As a formulation strategy to produce fixed-dose combinations with amorphous solid dispersions of poorly soluble drugs, active coating of tablets is an under-investigated topic. Methods: In this study, ibuprofen, with a boiling point of 157 °C, was used as a model drug, and an ibuprofen–HPMCAS coating was loaded on the surface of placebo tablets using a widely used perforated laboratory pan-coater with a single two-component nozzle. Acetone, acetonitrile, and DMSO, with different boiling points and evaporation kinetics, were used as the organic solvents. HPMCAS solutions in the mentioned solvents demonstrated different viscosities due to different solvent–polymer interactions, as indicated by different solution turbidity. The concentrations of the organic solvent-containing coatings were selected based on desirable flow rates in comparison with the reference Opadry^® II coating dispersion. Coatings were applied at the same pan rotation speed, but atomising and pattern air pressure, as well as drying conditions, were different. Results: The content of residual solvents in coatings was determined with gas chromatography: low-boiling-point acetone and acetonitrile content was below the LOD, while the content of DMSO, with a boiling point of 189 °C, comprised 1.5 wt.%. A pharmacopoeial approach was utilised to assess uniformity of dosage units via uniformity of content. The accuracy of dosing decreased from acetone- and acetonitrile- to DMSO-based coatings. Because of the high boiling point of DMSO in comparison to ibuprofen, the DMSO-based coating process was the longest, and the amount of ibuprofen loss was the highest. In turn, the precision of dosing via active coating increased from acetone to acetonitrile and to DMSO. The R.S.D. of the uniformity of content decreased along with coating time and fit the power function well (R² = 0.9843). Conclusions: Therefore, to answer the main question of this study, proper drug dosing (in terms of accuracy and precision) using drug loading via tablet coating with this specific equipment is possible. Depending on the dose precision desired, the duration of the coating process can vary.

Background: Polyols are widely used as tablet diluents due to their high solubility, favourable taste, and ability to form robust tablets. Thus, commercially available polyols, such as mannitol and isomalt, can be considered for the preparation of low-drug-dose formulations with a high polyol load. Methods/Results: This study investigated spray-dried mannitol (Mannogem^® XL Opal SD and Pearlitol^® 200 SD) and fluid-bed granulated isomalt (galenIQ™ 720 and galenIQ™ 721) at magnesium stearate levels of 0.5 and 3.0 wt.% and consolidation pressures of 100 and 300 MPa. During the tableting of 100 consecutive tablets, materials displayed different ejection force profiles: galenIQ™ 720 and galenIQ™ 721 demonstrated low and stable ejection pressures; Mannogem^® displayed a lubricant- and compaction pressure-dependent profile, whereas Pearlitol^® produced the highest ejection forces, particularly at 0.5 wt.% magnesium stearate. To elucidate these differences, the used materials were characterised in terms of SEM imaging, moisture content, surface area and porosity analysis, particle size distribution, pXRD, and densification kinetics. Using a compaction simulator, key parameters including pressure–displacement profiles, mean yield pressure, and strain rate sensitivity of the unlubricated materials were experimentally determined, while pressure transmission, residual die-wall pressure, and friction coefficient were computed. Conclusions: The study concluded that variations in tableting properties were primarily governed by moisture content and, for mannitol grades, by manufacturing method-dependent differences in particle microstructure. These insights provide guidance for the rational selection of polyol excipients and appropriate lubrication levels in direct compression tablet formulations.